| Adenosine A3 receptor |
EC50 |
= |
303000.0 |
nM |
Agonist efficacy as effective concentration to stimulate binding of [35S]GTP-gamma-S, by activation of human A3AR receptor |
CHEMBL1134070 |
| Rattus norvegicus |
IC50 |
= |
160.0 |
nM |
In vitro inhibition of synaptic potential in the hippocampal formation (synaptic responses (fEPSPs) recorded in the CAI region of in vivo hippocampal slices in rat brain) |
CHEMBL1125345 |
| Adenosine A1 receptor |
Ki |
= |
10.3 |
nM |
Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor |
CHEMBL1125345 |
| Adenosine A3 receptor |
Agonist effect |
= |
100.0 |
% |
Inhibition of [35S]GTP gamma-S binding to CHO cell membranes expressing human A3 receptor at 1 uM |
CHEMBL1134734 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]-CCPA from CHO cells expressing human recombinant Adenosine A1 receptor |
CHEMBL1134734 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
[3H]NECA saturation binding in CHO cells expressing human recombinant A2A adenosine receptor |
CHEMBL1134734 |
| Adenosine A2b receptor |
EC50 |
= |
2400.0 |
nM |
Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor |
CHEMBL1134734 |
| Adenosine A3 receptor |
Ki |
= |
6.0 |
nM |
[3H]NECA saturation binding in CHO cells expressing human Adenosine A3 receptor |
CHEMBL1134734 |
| Adenosine A1 receptor |
Ki |
= |
13.3 |
nM |
Binding affinity towards adenosine A1 receptor in rat brain cortex |
CHEMBL1134790 |
| Adenosine A2a receptor |
Ki |
= |
12.4 |
nM |
Binding affinity towards adenosine A2A receptor in rat brain striatum |
CHEMBL1134790 |
| Adenosine A1 receptor |
IC50 |
= |
2460.0 |
nM |
Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding |
CHEMBL1124076 |
| Adenosine A1 receptor |
IC50 |
= |
2.4 |
nM |
Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding |
CHEMBL1124076 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. |
CHEMBL1124142 |
| Adenosine A2 receptor |
Ki |
= |
12.0 |
nM |
Binding affinity at adenosine A2 receptor from rat striatal membranes by [3H]NECA displacement. |
CHEMBL1124142 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
1.87 |
|
Ratio of binding affinity against A2 and A1 receptors |
CHEMBL1124142 |
| Adenosine A1 receptor |
Ki |
> |
200.0 |
nM |
Affinity for Adenosine A1 receptor by displacement of [3H]DPCPX from human cerebral cortex |
CHEMBL1133855 |
| Adenosine A2a receptor |
Ki |
= |
15.1 |
nM |
Affinity for A2a receptor by displacement of [3H]-CGS- 21680 from human striatum |
CHEMBL1133855 |
| Adenosine A3 receptor |
Ki |
= |
8.22 |
nM |
Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in CHO cells |
CHEMBL1133855 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Binding affinity for A1-adenosine receptor by the displacement of specific [3H]-PIA binding in rat brain was determined |
CHEMBL1127835 |
| Adenosine A2 receptor |
Ki |
= |
10.3 |
nM |
Binding affinity for A2-adenosine receptor by the displacement of specific [3H]-CGS- binding in rat striatal membranes was determined |
CHEMBL1127835 |
| Adenosine A3 receptor |
Ki |
= |
113.0 |
nM |
Binding affinity for recombinant rat A3-adenosine receptor by the displacement of specific [125I]APNEA or [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5'-N-methyluronamide |
CHEMBL1127835 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
0.071 |
|
Ratio of binding affinities for A1 receptor compared to that of A3 receptor |
CHEMBL1127835 |
| Unchecked |
Ratio |
= |
0.091 |
|
Ratio of binding affinities for A2 receptor compared to that of A3 receptor |
CHEMBL1127835 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine |
CHEMBL1124304 |
| Adenosine A2 receptor |
Ki |
= |
12.0 |
nM |
Binding affinity towards adenosine A2 receptor on rat striatal membrane using [3H]NECA as radioligand |
CHEMBL1124304 |
| Rattus norvegicus |
EC25 |
= |
21.0 |
nM |
Reduction of heart rate (A1 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Rattus norvegicus |
EC25 |
= |
1.1 |
nM |
Enhancement of coronary flow (A2 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
1.9 |
|
Ratio of Ki at adenosine A2 and A1 receptors |
CHEMBL1124304 |
| Adenosine A1 receptor |
Affinity constant |
= |
0.1 |
uM |
Affinity constant for inhibition of A1 receptor control of adenylate cyclase in adipocytes, heart and brain cells |
CHEMBL1122012 |
| Adenosine A2 receptor |
Affinity constant |
= |
2.0 |
uM |
Affinity constant for A2 receptor control of adenylate cyclase in adipocytes, heart and brain cells |
CHEMBL1122012 |
| Adenosine receptor |
Affinity constant |
|
|
|
Inhibition of adenyl cyclase via P site in adipocytes; Inactive |
CHEMBL1122012 |
| Adenosine A3 receptor |
IC50 |
= |
65600.0 |
nM |
Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor |
CHEMBL1148450 |
| Adenosine A3 receptor |
Efficacy |
= |
100.0 |
% |
Percent efficacy for inhibition of human adenosine A3 receptor activity |
CHEMBL1148450 |
| Adenosine A1 receptor |
Ki |
= |
10.4 |
nM |
Displacement of [3H]CHA from Adenosine A1 receptor of rat brain |
CHEMBL1129447 |
| Adenosine A2a receptor |
Ki |
= |
7.8 |
nM |
Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. |
CHEMBL1129447 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
1.3 |
|
Relative affinities for Adenosine A1 and A2A receptors |
CHEMBL1129447 |
| Adenosine A1 receptor |
EC50 |
= |
54.8 |
nM |
Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria |
CHEMBL1129447 |
| Adenosine A2a receptor |
EC50 |
= |
394.0 |
nM |
Vasorelaxation as Adenosine A2A receptor activity in rat aorta |
CHEMBL1129447 |
| Adenosine A2a receptor |
Ratio |
= |
1.0 |
|
Ratio of inhibition of ADP-induced rabbit platelet aggregation and Adenosine A2a receptor binding |
CHEMBL1129447 |
| Adenosine A1 receptor |
Ki |
= |
10.4 |
nM |
Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. |
CHEMBL1128307 |
| Adenosine A2a receptor |
Ki |
= |
7.8 |
nM |
Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. |
CHEMBL1128307 |
| Adenosine A1 receptor |
EC50 |
= |
54800.0 |
nM |
Functional activity against adenosine A1 receptor from rat atria. |
CHEMBL1128307 |
| Adenosine A2a receptor |
EC50 |
= |
394.0 |
nM |
Functional activity against adenosine A2a receptor from rat aorta. |
CHEMBL1128307 |
| Adenosine A2a receptor |
Potency ratio |
= |
1.0 |
|
Anti-aggregatory activity against adenosine A2A receptor from rabbit platelets. Potency ratio was reported with reference to the NECA IC50 of 0.2 uM. |
CHEMBL1128307 |
| ADMET |
k' |
= |
0.19 |
|
Hydrophobicity index (k'') (RP-HPLC pH 7.5) |
CHEMBL1128307 |
| Adenosine receptors; A1 & A2a |
Selectivity |
= |
1.3 |
|
Selectivity as the ratio of Ki value towards A1 receptor to that of A2a receptor. |
CHEMBL1128307 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA. |
CHEMBL1131059 |
| Adenosine A2a receptor |
Ki |
= |
10.3 |
nM |
Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680. |
CHEMBL1131059 |
| Adenosine A3 receptor |
Ki |
= |
113.0 |
nM |
Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-. |
CHEMBL1131059 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
0.071 |
|
Selectivity for binding affinity towards A1 adenosine receptor in rat brain membrane and rat A3 receptor expressed in CHO cells. |
CHEMBL1131059 |
| Adenosine receptor A2a and A3 |
Ratio |
= |
0.0091 |
|
Selectivity for binding affinity towards A2A adenosine receptor in rat striatal membrane and rat A3 receptor expressed in CHO cells. |
CHEMBL1131059 |
| Adenosine A2a receptor |
Ki |
= |
1.0 |
nM |
In vitro inhibition of human neutrophil activation via Adenosine A2A receptor. |
CHEMBL1133401 |
| Adenosine A1 receptor |
Ki |
= |
1.0 |
nM |
Ex vivo inhibition of guinea pig ileum twitch via Adenosine A1 receptor. |
CHEMBL1133401 |
| P3 purinoceptor |
Ki |
= |
37.0 |
nM |
Binding activity was evaluated on P3 purinoceptor-like protein from rat brain membranes by using [3H]NECA (40 nM). |
CHEMBL1131028 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Inhibition of [3H]- DPCPX binding to Adenosine A1 receptor ofrat brain membranes |
CHEMBL1131028 |
| Adenosine A2a receptor |
Ki |
= |
10.0 |
nM |
Inhibition of [3H]- CGS 21680 binding to Adenosine A2A receptor of rat brain membranes |
CHEMBL1131028 |
| Adenosine A2b receptor |
Ki |
= |
2600.0 |
nM |
Activity against Adenosine A2B receptor as cAMP production in VA-13 cells |
CHEMBL1131028 |
| Adenosine A3 receptor |
Ki |
= |
110.0 |
nM |
Inhibition of [125I]AB-MECA (0.15 nM) binding to Adenosine A3 receptor of RBL-2H3 cell membranes |
CHEMBL1131028 |
| Adenosine A1 receptor |
Ki |
= |
1257.0 |
nM |
Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine |
CHEMBL1124836 |
| Adenosine A2 receptor |
Ki |
= |
9.0 |
nM |
Binding to Adenosine A2 receptor was measured in ADA-pretreated rat striatal membranes using [3H]-CGS- 21680 |
CHEMBL1124836 |
| Rattus norvegicus |
EC25 |
= |
5.0 |
nM |
Effective concentration required for 25% increase in coronary flow(CF) in perfused working heart model was determined |
CHEMBL1124836 |
| Rattus norvegicus |
EC25 |
= |
60.0 |
nM |
Effective concentration required for 25% increase in heart rate in perfused working heart model was determined |
CHEMBL1124836 |
| Unchecked |
Ratio |
= |
0.5 |
|
Ratio of A1-receptor binding to that of A2-receptor binding |
CHEMBL1124836 |
| Adenosine A3 receptor |
Radioligand bound |
= |
100.0 |
% |
Percentage of [35S]GTP-gamma-S, binding to the human adenosine A3 receptor stimulated at 10E-4 M |
CHEMBL1132635 |
| Adenosine A3 receptor |
EC50 |
= |
89.0 |
nM |
Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor |
CHEMBL1132635 |
| Adenosine A3 receptor |
Inhibition |
= |
100.0 |
% |
Inhibition of forskolin-stimulated cAMP production mediated by human adenosine A3 receptor expressed in CHO cells at 10 uM |
CHEMBL1132635 |
| P3 purinoceptor |
Ki |
= |
37.0 |
nM |
Binding activity was evaluated on P3 purinoceptor-like protein from rat brain membranes by using [3H]NECA (40 nM). |
CHEMBL1131028 |
| Adenosine A1 receptor |
Ki |
= |
11.0 |
nM |
Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
650.0 |
nM |
Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
8.2 |
nM |
Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
22.0 |
nM |
Binding affinity against adenosine A2 receptor from rat striatal membranes with 50 nM CPA using [3H]-NECA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
70.0 |
nM |
Binding affinity against adenosine A2 receptor from human platelet membranes using [3H]NECA |
CHEMBL1126089 |
| Adenosine receptors; A1 & A2 |
A2 selectivity |
= |
0.5 |
|
Selectivity as A1 adenosine receptors(high affinity) using [3H]-DPCPX compared to A2 adenosine receptors using [3H]NECA in rat striatal membranes |
CHEMBL1126089 |
| Adenosine receptors; A1 & A2 |
A2 selectivity |
= |
0.4 |
|
Selectivity as A1 adenosine receptors(high affinity) using [3H]CCPA compared to A2 adenosine receptors using [3H]-NECA in rat striatal membranes |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
12.0 |
nM |
In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. |
CHEMBL1136764 |
| Adenosine A2a receptor |
Ki |
= |
60.0 |
nM |
Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand |
CHEMBL1136764 |
| Adenosine A3 receptor |
Ki |
= |
11.0 |
nM |
Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor |
CHEMBL1136764 |
| Adenosine A2b receptor |
Displacement |
= |
2200.0 |
% |
Percent displacement of [3H]DPCPX from human adenosine A2B receptor |
CHEMBL1136764 |
| Adenosine A1 receptor |
Relative potency |
= |
0.2 |
|
Relative potency for human adenosine A1 receptor (Ki value) |
CHEMBL1136764 |
| Adenosine A2a receptor |
Relative potency |
= |
3.5 |
|
Relative potency for human adenosine A2A receptor (Ki value) |
CHEMBL1136764 |
| Adenosine A3 receptor |
Relative potency |
= |
55.0 |
|
Relative potency for human adenosine A3 receptor (Ki value) |
CHEMBL1136764 |
| Adenosine receptors; A1 & A2a |
Selectivity |
= |
5.0 |
|
Selectivity against adenosine A1 and A2A receptors |
CHEMBL1136764 |
| Adenosine receptors; A1 & A3 |
Selectivity |
= |
0.9 |
|
Selectivity for adenosine A1 and A3 receptors |
CHEMBL1136764 |
| Adenosine A2a receptor |
Ki |
= |
21.6 |
nM |
Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells |
CHEMBL1130114 |
| Adenosine A2a receptor |
Ki |
= |
21.5 |
nM |
Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells |
CHEMBL1130114 |
| Adenosine A2a receptor |
Ki |
= |
5.24 |
nM |
Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells |
CHEMBL1130114 |
| Adenosine A2a receptor |
Ki |
= |
21.4 |
nM |
Binding affinity against WT human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 |
CHEMBL1144939 |
| Adenosine A2a receptor |
Displacement |
= |
20.0 |
% |
Binding affinity against T88D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 at 10 uM |
CHEMBL1144939 |
| Adenosine A2a receptor |
Displacement |
= |
0.0 |
% |
Binding affinity against T88E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 at 10 uM |
CHEMBL1144939 |
| Adenosine A2a receptor |
Ki |
= |
1.5 |
nM |
Binding affinity against Q89D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 |
CHEMBL1144939 |
| Adenosine A2a receptor |
Ki |
= |
29.2 |
nM |
Binding affinity against S277E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 |
CHEMBL1144939 |
| Adenosine A2a receptor |
Ki |
= |
19.1 |
nM |
Binding affinity against H278D human adenosine A2A receptor stably transfected in CHO cells using [3H]- ZM-241385 as radioligand. |
CHEMBL1144939 |
| Adenosine A2a receptor |
Ki |
= |
24.6 |
nM |
Binding affinity against H278E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 |
CHEMBL1144939 |
| Adenosine A3 receptor |
EC50 |
= |
155.0 |
nM |
Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor |
CHEMBL1133730 |
| Adenosine A3 receptor |
Max |
= |
100.0 |
% |
Maximum stimulation against human adenosine A3 receptor |
CHEMBL1133730 |
| Adenosine A1 receptor |
Ki |
= |
6.3 |
nM |
Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand |
CHEMBL1125572 |
| Adenosine A2 receptor |
Ratio |
= |
10.3 |
nM |
Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand |
CHEMBL1125572 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
1.6 |
|
Ratio of A2 to A1. |
CHEMBL1125572 |
| Canis familiaris |
PO2 |
= |
250.0 |
% |
Tested for percent increase in coronary sinus partial pressure of oxygen (PO2) in open chest anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Canis familiaris |
Duration |
= |
345.0 |
min |
Total time in minutes elapsed from the initiation of the change until return to the pretest value of oxygen partial pressure in coronary sinus of anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Canis familiaris |
BP |
= |
15.0 |
mmHg |
Tested for the percent increase in aortic blood pressure (BP) in open chest anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Canis familiaris |
Duration |
= |
120.0 |
min |
Total time in minutes elapsed from the initiation of the change until return to the pretest value of blood pressure in coronary sinus of anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Canis familiaris |
HR |
= |
73.0 |
% |
Tested for the percent increase in heart rate (HR) in open chest anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Canis familiaris |
Duration |
= |
345.0 |
min |
Total time in minutes elapsed from the initiation of the change until return to the pretest value of heart rate in coronary sinus of anesthetized dog at intravenous dosage of 0.01 mg/kg |
CHEMBL1121608 |
| Mus musculus |
LD50 |
= |
0.5 |
mg.kg-1 |
Lethal dose in mice after intraperitoneal administration |
CHEMBL1121608 |
| Mus musculus |
LD50 |
= |
5.0 |
mg.kg-1 |
Lethal dose in mice after peroral administration |
CHEMBL1121608 |
| Canis familiaris |
EC50 |
= |
150.0 |
nM |
Coronary vasoactivity in dogs |
CHEMBL1123491 |
| Adenosine A2 receptor |
EC50 |
= |
130.0 |
nM |
Potency against PC12 cell A2 adenosine receptor by adenylate cyclase activation |
CHEMBL1123491 |
| Adenosine A2 receptor |
EC50 |
= |
300.0 |
nM |
Potency against human platelet A2 adenosine receptor |
CHEMBL1123491 |
| Adenosine A1 receptor |
IC50 |
= |
10.2 |
nM |
Potency against rat brain adenosine A1 receptor |
CHEMBL1123491 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. |
CHEMBL1131221 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. |
CHEMBL1131221 |
| Adenosine A3 receptor |
Ki |
= |
49.0 |
nM |
Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
1.1 |
|
Inhibitory selectivity at Adenosine 2A receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
3.5 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
3.06 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 2A receptor. |
CHEMBL1131221 |
| Adenosine A1 receptor |
IC50 |
= |
17.0 |
nM |
Displacement of [125I]ABA from adenosine A1 receptor of chick cerebellar membrane |
CHEMBL1123754 |
| Adenosine A2 receptor |
IC50 |
= |
25.0 |
nM |
Displacement of [3H]-NECA from adenosine A2 receptor of rat striatal membrane |
CHEMBL1123754 |
| Unchecked |
Selectivity |
= |
1.5 |
|
Relative affinities for adenosine A2 and A1 receptors |
CHEMBL1123754 |
| Adenosine A3 receptor |
EC50 |
= |
26.0 |
nM |
Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor |
CHEMBL1135592 |
| Adenosine A3 receptor |
Efficacy |
= |
103.0 |
% |
Percent efficacy against human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
35.0 |
nM |
Affinity for human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
0.8 |
nM |
Binding affinity towards human Adenosine A3 receptor wild type |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
0.9 |
nM |
Binding affinity towards Adenosine A3 receptor (W243 A mutant receptor) |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
|
|
|
Binding affinity towards Adenosine A3 receptor (H95A mutant receptor); Not determined |
CHEMBL1135592 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes |
CHEMBL1134334 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane |
CHEMBL1134334 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX |
CHEMBL1134334 |
| Adenosine A1 receptor |
EC50 |
= |
87.2 |
nM |
[S]GTP gamma-S binding against adenosine A1 receptor in rat brain |
CHEMBL1131655 |
| Adenosine A1 receptor |
EC50 |
= |
59.0 |
nM |
Binding against human adenosine A1 receptor |
CHEMBL1131655 |
| Adenosine A1 receptor |
Ki |
= |
10.4 |
nM |
Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand |
CHEMBL1127534 |
| Adenosine A2 receptor |
Ki |
= |
7.8 |
nM |
Affinity for the adenosine A2 receptor was evaluated in a competition assay in rat striatum using [3H]-CGS- 21680 as radioligand |
CHEMBL1127534 |
| Adenosine A1 receptor |
EC50 |
= |
54.8 |
nM |
Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria |
CHEMBL1127534 |
| Adenosine A2 receptor |
EC50 |
= |
394.0 |
nM |
Negative chronotropic activity via A2 Adenosine receptor was tested monitoring vasodilation in rat aorta |
CHEMBL1127534 |
| Adenosine A2a receptor |
Ratio |
= |
1.0 |
|
Inhibition compared to inhibition by NECA (IC50 ratio) of rabbit platelet aggregation induced by ADP |
CHEMBL1127534 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
1.3 |
|
Ratio between Ki values of A1 and A2 receptors was determined |
CHEMBL1127534 |
| ADMET |
k' |
= |
0.19 |
|
Hydrophobicity index (k') (RP-HPLC) |
CHEMBL1127534 |
| Adenosine A3 receptor |
EC50 |
= |
84.8 |
nM |
Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells |
CHEMBL1148352 |
| Adenosine A1 receptor |
Ki |
= |
10.4 |
nM |
Displacement of [3H]CHA from Adenosine A1 receptor of rat brain |
CHEMBL1128544 |
| Adenosine A2a receptor |
Ki |
= |
7.8 |
nM |
Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum |
CHEMBL1128544 |
| Adenosine receptors; A1 & A2a |
Selectivity |
= |
1.3 |
|
Relative affinities for rat adenosine A1 and A2a receptors |
CHEMBL1128544 |
| Adenosine A1 receptor |
EC50 |
= |
55.0 |
nM |
Activity at Adenosine A1 receptor of rat atria |
CHEMBL1128544 |
| Adenosine A2a receptor |
EC50 |
= |
394.0 |
nM |
Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta |
CHEMBL1128544 |
| Adenosine A1 receptor |
Ki |
= |
13.3 |
nM |
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand |
CHEMBL1126140 |
| Adenosine A2 receptor |
Ki |
= |
12.4 |
nM |
Binding affinity against adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand |
CHEMBL1126140 |
| Rattus norvegicus |
ED30 |
= |
0.19 |
ug kg-1 |
Dose producing 30% decrease of blood pressure in anesthetized rats (SHR) |
CHEMBL1126140 |
| Rattus norvegicus |
ED10 |
= |
0.35 |
ug kg-1 |
Dose producing 10% decrease of heart rate in anesthetized rats (SHR) |
CHEMBL1126140 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
1.1 |
|
Selectivity against adenosine A1 to A2 receptors |
CHEMBL1126140 |
| G protein-coupled receptor 80 |
Ki |
= |
37.0 |
nM |
Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes |
CHEMBL1134608 |
| G protein-coupled receptor 80 |
Ki |
= |
27.0 |
nM |
Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes |
CHEMBL1134608 |
| Adenosine A1 receptor |
Ki |
= |
7.7 |
nM |
Binding activity against Adenosine A1 receptor from rat brain membranes using [3H]8-cyclopentyl-1,3-dipropylxanthine (DPCPX) |
CHEMBL1134608 |
| Adenosine A2a receptor |
Ki |
= |
4.13 |
nM |
Binding affinity for Adenosine A2A receptor in rat brain membranes using [3H]CGS-21680 |
CHEMBL1134608 |
| Adenosine A2b receptor |
Activity |
= |
100.0 |
|
Agonist activity as cAMP production in CHO cells expressing rat Adenosine A2B receptor at 100 uM |
CHEMBL1134608 |
| Adenosine A3 receptor |
Ki |
= |
412.0 |
nM |
Binding affinity for adenosine A3 receptor in CHO cell membranes using [125I]IB-MECA |
CHEMBL1134608 |
| Unchecked |
Ratio |
= |
0.29 |
|
Ratio of affinity for A1 AND P3LP receptor |
CHEMBL1134608 |
| Unchecked |
Ratio |
= |
0.152 |
|
Ratio of affinity for A2A and P3LP receptors |
CHEMBL1134608 |
| Unchecked |
Ratio |
= |
15.3 |
|
Ratio of affinity for A3 and P3LP receptors |
CHEMBL1134608 |
| Adenosine A3 receptor |
Ki |
= |
169.0 |
nM |
Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells |
CHEMBL1134644 |
| Adenosine A3 receptor |
Ki |
= |
3200.0 |
nM |
Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells |
CHEMBL1134644 |
| Adenosine A1 receptor |
Ki |
= |
12.0 |
nM |
Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX; Range = 9.6-15 nM |
CHEMBL1148363 |
| Adenosine A2a receptor |
Ki |
= |
60.0 |
nM |
Binding affinity against human adenosine A2A receptor expressed in HEK293 cells using [3H]ZM-241385 |
CHEMBL1148363 |
| Adenosine A3 receptor |
Ki |
= |
11.0 |
nM |
Binding affinity against human adenosine A3 receptor expressed on HEK293 cells using [125I]I-AB-MECA |
CHEMBL1148363 |
| Adenosine A2b receptor |
EC50 |
= |
104.0 |
nM |
Agonistic activity against human adenosine A2B receptor expressed in CHO cells |
CHEMBL1148363 |
| Adenosine A1 receptor |
IC50 |
= |
16.0 |
nM |
Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor |
CHEMBL1125861 |
| Adenosine A2 receptor |
IC50 |
= |
15.0 |
nM |
Concentration required for 50% inhibition of [3H]NECA binding on rat brain adenosine A2 receptor |
CHEMBL1125861 |
| Rattus norvegicus |
ED25 |
= |
0.00075 |
mg kg-1 |
25% reduction in blood pressure in the rat. |
CHEMBL1125861 |
| Rattus norvegicus |
Delta HR |
= |
-25.0 |
% |
Change in heart rate was expressed in percent at at a dose 0.005 mg/kg iv in anesthetized rat |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
168.0 |
mmHg |
Mean arterial pressure were recorded as baseline prior to the drug administration in hypertensive rats at 0.1 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
168.0 |
mmHg |
Mean arterial pressure were recorded as baseline prior to the drug administration in hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-27.0 |
mmHg |
Mean arterial pressure were recorded as change after 6 hr of following oral dosing hypertensive rats at 0.1 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-42.0 |
mmHg |
Mean arterial pressure were recorded as change after 6 hr of following oral dosing hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
377.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 0.1 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
419.0 |
mmHg |
Heart rate was recorded as baseline prior to the drug administration in hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
53.0 |
mmHg |
Heart rate was recorded as change after 6 hr of following oral dosing hypertensive rats at 0.1 mg/kg dose |
CHEMBL1125861 |
| Rattus norvegicus |
Mean arterial blood pressure |
= |
-76.0 |
mmHg |
Heart rate was recorded as change after 6 hr of following oral dosing hypertensive rats at 0.3 mg/kg dose |
CHEMBL1125861 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.00075 |
|
Ratio of IC50 values for A1 receptor binding to that of A2 receptor |
CHEMBL1125861 |
| Adenosine A1 receptor |
EC50 |
= |
63.1 |
nM |
Prolongation of the stimulus-QRS interval by 50% of the maximum response at the Adenosine A1 receptor in langendorff guinea pig heart preparation |
CHEMBL1125661 |
| Adenosine A2 receptor |
EC50 |
= |
2.754 |
nM |
Coronary arteries vasodilation at the Adenosine A2 receptor in langendorff guinea pig heart preparation |
CHEMBL1125661 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
25.0 |
|
Ratio of EC50 stim-QRS (conduction block) and EC50 for vasodilation of coronary arteries |
CHEMBL1125661 |
| Adenosine A1 receptor |
Ki |
= |
63.0 |
nM |
Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. |
CHEMBL1128285 |
| Adenosine A2a receptor |
Ki |
= |
10.3 |
nM |
Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand |
CHEMBL1128285 |
| Adenosine A3 receptor |
Ki |
= |
113.0 |
nM |
Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor |
CHEMBL1128285 |
| Adenosine A3 receptor |
Activity |
= |
100.0 |
|
Agonistic activity expressed as the amount of [35S]GTP gamma-S bound at adenosine A3 receptor |
CHEMBL1134582 |
| Adenosine A3 receptor |
Activity |
= |
100.0 |
|
Agonistic activity expressed as the amount of [35S]GTP gamma-S bound +1 uM NECA at adenosine A3 receptor |
CHEMBL1134582 |
| Adenosine A1 receptor |
Ki |
= |
8.3 |
nM |
Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. |
CHEMBL1125505 |
| Adenosine A2 receptor |
Ki |
= |
10.0 |
nM |
Binding affinity against adenosine A2 receptor from rat striatum using [3H]NECA as radioligand. |
CHEMBL1125505 |
| Rattus norvegicus |
ED30 |
= |
0.23 |
ug kg-1 |
Dose producing 30% decrease in blood pressure of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Rattus norvegicus |
ED10 |
= |
0.35 |
ug kg-1 |
Dose producing 10% decrease in heart rate of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
0.8 |
|
Selectivity determined as Ratio of Ki(nM) of A1 adenosine receptor to the Ki(nM) of A2 adenosine receptor |
CHEMBL1125505 |
| Adenosine A1 receptor |
IC50 |
= |
10.0 |
nM |
Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. |
CHEMBL1124880 |
| Adenosine A2 receptor |
IC50 |
= |
17.0 |
nM |
Evaluated for the binding affinity towards the Adenosine A2 receptor in corpora striata of rats using [3H]NECA as radioligand. |
CHEMBL1124880 |
| Adenosine A1 receptor |
Ki |
= |
63.0 |
nM |
Ability to displace [3H]DPCPX from Adenosine A1 receptor in rat cortical membrane |
CHEMBL1135807 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Binding affinity at Adenosine A2A receptor in rat striatal membrane by [3H]ZM-241385 displacement. |
CHEMBL1135807 |
| Adenosine A3 receptor |
Ki |
= |
11.0 |
nM |
Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]-AB MECA displacement. |
CHEMBL1135807 |
| Adenosine A2a receptor |
Emax |
= |
102.0 |
% |
Maximum level of G-protein activation (Emax) compared to CGS 21680 through Adenosine A2A receptor expressed in CHO cells using cAMP assay |
CHEMBL1135807 |
| Adenosine A2a receptor |
EC50 |
= |
40.0 |
nM |
G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay |
CHEMBL1135807 |
| Adenosine A1 receptor |
Ki |
= |
6.24 |
nM |
Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain |
CHEMBL1122939 |
| Adenosine A2 receptor |
Ki |
= |
10.6 |
nM |
Displacement of [3H]-NECA from adenosine A2 receptor of rat striatal membrane |
CHEMBL1122939 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
1.7 |
|
Relative binding to A2 and A1 receptors (ratio of Ki) |
CHEMBL1122939 |
| Adenosine A1 receptor |
Ki |
= |
63.0 |
nM |
Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the absence of GTP |
CHEMBL1132702 |
| Adenosine A1 receptor |
Ki |
= |
530.0 |
nM |
Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the presence of 1 mM of GTP |
CHEMBL1132702 |
| Adenosine A1 receptor |
Ki |
= |
13.6 |
nM |
Binding affinity for human adenosine A1 receptor |
CHEMBL1132702 |
| Unchecked |
GTP shift |
= |
8.4 |
|
GTP shift was determined |
CHEMBL1132702 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane |
CHEMBL1132702 |
| Adenosine A3 receptor |
Ki |
= |
10.6 |
nM |
Ability to displace radioligand [125I]AB-MECA from membrane of HEK 293 cells stably transfected with human adenosine A3 receptor cDNA |
CHEMBL1132702 |
| Adenosine A3 receptor |
Ki |
= |
113.0 |
nM |
Binding affinity for rat adenosine A3 receptor |
CHEMBL1132702 |
| Adenosine A2b receptor |
EC50 |
= |
3100.0 |
nM |
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA |
CHEMBL1132702 |
| Adenosine A1 receptor |
IC50 |
= |
200.0 |
nM |
Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor |
CHEMBL1124132 |
| Adenosine A1 receptor |
Inhibition |
= |
0.93 |
% |
Maximal inhibition of adenylate cyclase activity relative to R-PIA for Adenosine A1 receptor (Inhibition by R-PIA=53+/-10%) |
CHEMBL1124132 |
| Adenosine A2 receptor |
EC50 |
= |
260.0 |
nM |
Stimulation of adenylate cyclase activity in human platelet membrane at A2 receptor |
CHEMBL1124132 |
| Adenosine A2 receptor |
Stimulation |
= |
1.0 |
% |
Maximal stimulation of adenylate cyclase activity relative to NECA for A2-receptor. (Stimulation by NECA=250+/-30%) |
CHEMBL1124132 |
| Adenosine A1 receptor |
Ki |
= |
8.2 |
nM |
Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes |
CHEMBL1124132 |
| Adenosine A2 receptor |
Ki |
= |
22.0 |
nM |
Displacement of [3H]NECA from A2-receptor of rat striatal membranes |
CHEMBL1124132 |
| Homo sapiens |
IC50 |
= |
600.0 |
nM |
Concentration that inhibits platelet aggregation induced by ADP (7 uM) by 50% |
CHEMBL1124132 |
| Unchecked |
Selectivity |
= |
1.3 |
|
A1 selectivity as ratio of EC50 at A2 receptor to IC50 at A1 receptor |
CHEMBL1124132 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
2.7 |
|
A1 selectivity as ratio of Ki for A2 receptor to Ki for A1 receptor |
CHEMBL1124132 |
| Adenosine A1 receptor |
IC50 |
= |
52000.0 |
nM |
Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor |
CHEMBL1124077 |
| Adenosine A1 receptor |
IC50 |
= |
90000.0 |
nM |
Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor |
CHEMBL1124077 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes |
CHEMBL1132946 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes |
CHEMBL1132946 |
| Adenosine A3 receptor |
Ki |
= |
49.0 |
nM |
Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
1.1 |
|
Selectivity, ratio of affinity towards adenosine A2A to A1 |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
3.5 |
|
Selectivity, ratio of affinity towards adenosine A3 to A1 |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
3.1 |
|
Selectivity, ratio of affinity towards adenosine A3 to A2A |
CHEMBL1132946 |
| Adenosine A1 receptor |
Kd |
= |
8.6 |
nM |
Dissociation constant against Adenosine A1 receptor |
CHEMBL1142733 |
| Adenosine A1 receptor |
KD hydro |
= |
0.25 |
mM |
Dissociation constant against Adenosine A1 receptor |
CHEMBL1142733 |
| Adenosine A1 receptor |
Ki |
= |
5.0 |
nM |
Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells |
CHEMBL1137202 |
| Adenosine A2b receptor |
EC50 |
= |
440.0 |
nM |
Potency against cAMP formation in CHO cells expressing recombinant human A2B receptor |
CHEMBL1137202 |
| Adenosine A2a receptor |
Emax |
= |
100.0 |
% |
Relative efficacy in cAMP formation in CHO cells expressing recombinant human A2A receptor compared to NECA |
CHEMBL1137202 |
| Adenosine A2a receptor |
EC50 |
= |
34.0 |
nM |
Efficacy against phenylephrine precontracted tissue relaxation in rat aorta |
CHEMBL1137202 |
| Adenosine A2a receptor |
Emax |
= |
100.0 |
% |
Efficacy against phenylephrine precontracted tissue relaxation in rat aorta compared to NECA |
CHEMBL1137202 |
| Adenosine A2b receptor |
EC50 |
= |
250.0 |
nM |
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta |
CHEMBL1137202 |
| Adenosine A2b receptor |
Emax |
= |
100.0 |
% |
Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta compared to NECA |
CHEMBL1137202 |
| Cavia porcellus |
EC50 |
= |
84000.0 |
nM |
Concentration-Relaxation Studies was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist CSC ( E-4 M) |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
1.0 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist CSC ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
100.7 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist CSC ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
EC50 |
= |
88000.0 |
nM |
Concentration-Relaxation Studies was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist Alloxazine ( E-4 M) |
CHEMBL1137202 |
| Adenosine A2a receptor |
Ki |
= |
130.0 |
nM |
Inhibition of [3H]ZM-241385 binding to human adenosine A2A receptor expressed in HeLa cells |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
1.0 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist Alloxazine ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
97.5 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist Alloxazine ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
EC50 |
= |
77000.0 |
nM |
Concentration-Relaxation Studies was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist DMPX ( E-4 M) |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
0.9 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist DMPX ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
98.7 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist DMPX ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
EC50 |
= |
65000.0 |
nM |
Concentration-Relaxation Studies was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist 8-PT ( E-4 M) |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
0.8 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist 8-PT ( E-4 M) relative to control |
CHEMBL1137202 |
| Cavia porcellus |
Ratio |
= |
79.2 |
|
Concentration-Relaxation Studies (ratio) was exerted on Guinea Pig Tracheal Rings Precontracted by Carbachol by the compound in presence of Adenosine antagonist 8-PT ( E-4 M) relative to control |
CHEMBL1137202 |
| Adenosine A2b receptor |
Ki |
= |
760.0 |
nM |
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells |
CHEMBL1137202 |
| Adenosine A3 receptor |
Ki |
= |
4.0 |
nM |
Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells |
CHEMBL1137202 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
0.04 |
|
Selectivity ratio for adenosine A1 receptor and adenosine A2A receptor |
CHEMBL1137202 |
| Adenosine A2 receptor |
Ratio |
= |
5.8 |
|
Selectivity ratio for adenosine A2B receptor and adenosine A2A receptor |
CHEMBL1137202 |
| Adenosine receptors; A2a & A3 |
Ratio |
= |
0.03 |
|
Selectivity ratio for adenosine A3 receptor and adenosine A2A receptor |
CHEMBL1137202 |
| Adenosine A2a receptor |
EC50 |
= |
50.0 |
nM |
Potency against cAMP formation in CHO cells expressing recombinant human A2A receptor |
CHEMBL1137202 |
| Adenosine A2a receptor |
Emax |
= |
100.0 |
% |
Relative efficacy in cAMP formation in CHO cells expressing recombinant human A2A receptor compared to NECA |
CHEMBL1137202 |
| Adenosine A1 receptor |
Ki |
= |
18.2 |
nM |
Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine A2a receptor |
Ki |
= |
12.2 |
nM |
Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine A3 receptor |
Ki |
= |
34.8 |
nM |
Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
0.52 |
|
Ratio of binding affinity for Adenosine A1 and Adenosine A3 receptors |
CHEMBL1138800 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes |
CHEMBL1144357 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes |
CHEMBL1144357 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes |
CHEMBL1144357 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
1.14 |
|
Relative affinities against adenosine A2A and A1 receptors (ratio of KiA2A/KiA1) |
CHEMBL1144357 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
5.2 |
|
Relative affinities for adenosine A3 and A1 receptors (ratio of KiA3/KiA1) |
CHEMBL1144357 |
| Adenosine receptors; A2a & A3 |
Ratio |
= |
0.22 |
|
Relative affinities for adenosine A2A and A3 receptors (ratio of KiA2A/KiA3) |
CHEMBL1144357 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1141186 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1141186 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1141186 |
| Adenosine A1 receptor |
Ki |
= |
1.04 |
nM |
Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells |
CHEMBL1147002 |
| Adenosine A2a receptor |
Ki |
= |
124.0 |
nM |
Displacement of [125I]ZM241385 from human adenosine A2A receptor in HEK cells |
CHEMBL1147002 |
| Adenosine A3 receptor |
Ki |
= |
10.2 |
nM |
Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells |
CHEMBL1147002 |
| Adenosine receptors; A1 & A3 |
Ratio Ki |
= |
0.102 |
|
Selectivity for human adenosine A3 receptor over human adenosine A1 receptor |
CHEMBL1147002 |
| Adenosine A2b receptor |
Ki |
= |
884.0 |
nM |
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells |
CHEMBL1147002 |
| Adenosine A3 receptor |
EC50 |
= |
78.0 |
nM |
Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay |
CHEMBL1147643 |
| Adenosine A3 receptor |
EC50 |
= |
10400.0 |
nM |
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay |
CHEMBL1147643 |
| ScN2a |
EC50 |
|
|
|
Reduction of PrPSC accumulation in ScN2a cells |
CHEMBL1139220 |
| Adenosine A2a receptor |
Ki |
= |
680.0 |
nM |
Inhibitory constant against human adenosine A2a receptor |
CHEMBL1139220 |
| Adenosine A1 receptor |
Ki |
= |
18.3 |
nM |
Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1139845 |
| Adenosine A2a receptor |
Ki |
= |
12.5 |
nM |
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1139845 |
| Adenosine A3 receptor |
Ki |
= |
34.6 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1139845 |
| Adenosine A2b receptor |
EC50 |
= |
160.0 |
nM |
Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels |
CHEMBL1139845 |
| Adenosine A1 receptor |
Activity |
|
|
|
Inhibitory constant aganist human adenosine A1 receptor |
CHEMBL1139220 |
| Adenosine A3 receptor |
Activity |
|
|
|
Inhibitory constant against human adenosine A3 receptor |
CHEMBL1139220 |
| Adenosine A1 receptor |
EC50 |
= |
0.3631 |
nM |
Agonist activity at adenosine A1 receptor assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
Inhibition |
= |
98.0 |
% |
Agonist activity at adenosine A1 receptor assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
Kd |
= |
575.44 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
Inhibition |
= |
83.3 |
% |
Displacement of [3H]DPCPX from human adenosine A1 receptor in CHO cells |
CHEMBL1141376 |
| Adenosine A2a receptor |
EC50 |
= |
17.38 |
nM |
Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
Ratio |
= |
3.2 |
|
Ratio of pEC50 to pKd at human adenosine A1 receptor in CHO cells |
CHEMBL1141376 |
| Adenosine A2b receptor |
EC50 |
= |
3630.78 |
nM |
Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
EC50 |
= |
0.3631 |
nM |
Activity at human adenosine A1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A3 receptor |
EC50 |
= |
4.5710000000000015 |
nM |
Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells |
CHEMBL1141376 |
| Adenosine A1 receptor |
Ki |
= |
6.8 |
nM |
Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A2a receptor |
Ki |
= |
2.2 |
nM |
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A3 receptor |
Ki |
= |
16.0 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A2b receptor |
EC50 |
= |
140.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production |
CHEMBL1144471 |
| Adenosine A3 receptor |
Efficacy |
= |
100.0 |
% |
Maximum efficacy at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP production at 10 uM relative to NECA |
CHEMBL1144471 |
| Adenosine A2a receptor |
EC50 |
= |
21.9 |
nM |
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production |
CHEMBL1144471 |
| Adenosine A2b receptor |
EC50 |
= |
110.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production |
CHEMBL1144471 |
| Adenosine A1 receptor |
Ki |
= |
18.2 |
nM |
Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1142924 |
| Adenosine A2a receptor |
Ki |
= |
12.4 |
nM |
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1142924 |
| Adenosine A2b receptor |
EC50 |
= |
155.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production |
CHEMBL1142924 |
| Adenosine A3 receptor |
Ki |
= |
35.7 |
nM |
Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1142924 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1137613 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1137613 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1137613 |
| Adenosine A2a receptor |
Ki |
= |
110.0 |
nM |
Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane |
CHEMBL1138285 |
| Adenosine A3 receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells |
CHEMBL1142932 |
| Adenosine A1 receptor |
Ki |
|
|
|
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293T cells |
CHEMBL1142932 |
| Adenosine A2a receptor |
Ki |
|
|
|
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells |
CHEMBL1142932 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1143166 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1143166 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1143166 |
| Adenosine A2b receptor |
logEC50 |
= |
-2.146 |
|
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase |
CHEMBL1145544 |
| Adenosine A2b receptor |
Activity |
= |
0.0 |
|
Agonist activity human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase relative to NECA |
CHEMBL1145544 |
| Adenosine A3 receptor |
EC50 |
= |
346.74 |
nM |
Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay |
CHEMBL1145629 |
| Adenosine A1 receptor |
Ki |
|
|
|
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293T cells |
CHEMBL1157148 |
| Adenosine A2a receptor |
Ki |
|
|
|
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells |
CHEMBL1157148 |
| Adenosine A3 receptor |
Ki |
= |
17700.0 |
nM |
Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells |
CHEMBL1157148 |
| Adenosine A2a receptor |
Kdiss |
= |
0.081 |
/s |
Dissociation of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cells at 100 uM by liquid scintillation counting relative to control |
CHEMBL1141671 |
| Adenosine A2a receptor |
T1/2 |
= |
0.002367 |
hr |
Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in CHO cells assessed as time course of dissociation at 10 uM by liquid scintillation counting relative to control |
CHEMBL1141671 |
| Adenosine A3 receptor |
Activity |
|
|
|
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP accumulation at 10 uM by liquid scintillation spectrometry |
CHEMBL1153383 |
| Adenosine A2a receptor |
IC50 |
= |
64.0 |
nM |
Displacement of radiolabeled NECA from human adenosine A2A receptor |
CHEMBL1140203 |
| Adenosine A2a receptor |
Ki |
= |
52.0 |
nM |
Displacement of radiolabeled NECA from human adenosine A2A receptor |
CHEMBL1140203 |
| Adenosine A1 receptor |
Ki |
= |
7.8 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane |
CHEMBL1155896 |
| Adenosine A2b receptor |
Ki |
= |
1270.0 |
nM |
Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane |
CHEMBL1155896 |
| Adenosine A3 receptor |
Ki |
= |
11.0 |
nM |
Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cell membrane |
CHEMBL1155896 |
| Adenosine A2a receptor |
IC50 |
= |
23.0 |
nM |
Inhibition of human adenosine A2A receptor |
CHEMBL1155111 |
| Adenosine A2b receptor |
Ki |
= |
1890.0 |
nM |
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells |
CHEMBL1137016 |
| Adenosine A2b receptor |
Ki |
= |
570.0 |
nM |
Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells |
CHEMBL1137016 |
| Adenosine A2b receptor |
Ki |
= |
262.0 |
nM |
Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells |
CHEMBL1137016 |
| Adenosine A3 receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells by scintillation counting |
CHEMBL1152960 |
| Adenosine A2a receptor |
Ki |
|
|
|
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells by scintillation counting |
CHEMBL1152960 |
| Adenosine A1 receptor |
Ki |
|
|
|
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293T cells by scintillation counting |
CHEMBL1152960 |
| Adenosine A2a receptor |
Ki |
= |
25.0 |
nM |
Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in Sf21 cells co-expressing GalphaS2, beta4, gamma2 |
CHEMBL1158518 |
| Adenosine A2a receptor |
IC50 |
= |
16.0 |
nM |
Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay |
CHEMBL1158518 |
| Adenosine A1 receptor |
EC50 |
= |
30.0 |
nM |
Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay |
CHEMBL1158518 |
| Adenosine A3 receptor |
EC50 |
= |
63.0 |
nM |
Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay |
CHEMBL1158518 |
| Adenosine A2b receptor |
EC50 |
= |
38.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay |
CHEMBL1158518 |
| PBMC |
IC50 |
= |
40.0 |
nM |
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA |
CHEMBL1158518 |
| PBMC |
IC50 |
= |
187.0 |
nM |
Antiinflammatory activity in rat PBMC assessed as inhibition of LPS-induced TNFalpha production after 20 hrs by ELISA |
CHEMBL1158518 |
| Adenosine A3 receptor |
Inhibition |
= |
100.0 |
% |
Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release at 10 uM by liquid scintillation spectrophotometry relative to NECA |
CHEMBL1159060 |
| Adenosine A2b receptor |
Activity |
= |
100.0 |
% |
Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release at 10 uM by liquid scintillation spectrophotometry relative to NECA |
CHEMBL1159060 |
| Adenosine A2a receptor |
Activity |
= |
0.75 |
pmol/ml |
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced intracellular cAMP accumulation at 100 nM after 24 hrs (Rvb= 0.40 pmol/ml) |
CHEMBL1156165 |
| Adenosine A3 receptor |
Ki |
= |
6.2 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1157749 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1157749 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1157749 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay |
CHEMBL1255231 |
| microRNA 21 |
Potency |
= |
11.7 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of miRNAs and/or Activators of miR-21. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
EC50 |
< |
88.0 |
nM |
PUBCHEM_BIOASSAY: Luminescence Cell-Based Dose Confirmation HTS to Identify Inhibitors of Platelet Dense Granule Release. (Class of assay: confirmatory) [Related pubchem assays: 1663 (Primary HTS), 1678 (Summary of Project)] |
CHEMBL1201862 |
| Luciferin 4-monooxygenase |
EC50 |
> |
112219.0 |
nM |
PUBCHEM_BIOASSAY: Luminescence Biochemical Dose Response HTS to Identify Inhibitors of Luciferase. (Class of assay: confirmatory) [Related pubchem assays: 1663 (Primary HTS), 1678 (Summary of Project)] |
CHEMBL1201862 |
| MAP kinase ERK2 |
Potency |
= |
8912.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of the ERK Signaling Pathway using a Homogeneous Screening Assay; Stimulation with EGF. (Class of assay: confirmatory) [Related pubchem assays: 995 ] |
CHEMBL1201862 |
| microRNA 21 |
Potency |
= |
11.7 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Modulators of miRNAs and/or Inhibitors of miR-21. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
= |
1258.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A2a receptor |
IC50 |
= |
67.0 |
nM |
Inhibition of human adenosine A2A receptor |
CHEMBL1649335 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
11.6 |
nM |
PUBCHEM_BIOASSAY: Validation screen for small molecules that induce genotoxicity in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493143, AID504466] |
CHEMBL1201862 |
| Nuclear factor erythroid 2-related factor 2 |
Potency |
|
2310.9 |
nM |
PUBCHEM_BIOASSAY: Nrf2 qHTS screen for inhibitors: Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493163, AID504444, AID504648] |
CHEMBL1201862 |
| Relaxin receptor 2 |
Potency |
|
974.2 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP2 Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489012] |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
|
308.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: RXFP1 Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489043, AID492948] |
CHEMBL1201862 |
| Dopamine D1 receptor |
Potency |
|
1158.1 |
nM |
PUBCHEM_BIOASSAY: HTS Assay for Allosteric Agonists of the Human D1 Dopamine Receptor: Primary Screen for Potentiators. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488989, AID488993, AID488995] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
8436.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| Chromobox protein homolog 1 |
Potency |
|
5972.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay for Inhibitors of HP1-beta Chromodomain Interactions with Methylated Histone Tails. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488962] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
18.4 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493014] |
CHEMBL1201862 |
| Vasopressin V1b receptor |
Potency |
|
1943.8 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: V1B Hit Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID2676, AID2703, AID489012] |
CHEMBL1201862 |
| Thyrotropin-releasing hormone receptor |
Potency |
|
517.4 |
nM |
PUBCHEM_BIOASSAY: qHTS for Small Molecule Agonists and Allosteric Enhancers of Human TRH Receptor: Confirmation Screen for Enhancers. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485365] |
CHEMBL1201862 |
| Thioredoxin reductase 1, cytoplasmic |
Potency |
|
446.7 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1): qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488771] |
CHEMBL1201862 |
| Regulator of G-protein signaling 4 |
Potency |
|
1062.1 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504856] |
CHEMBL1201862 |
| Thioredoxin reductase 1, cytoplasmic |
Potency |
|
3768.6 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Substrates of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1): qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488771] |
CHEMBL1201862 |
| Adenosine A2a receptor |
Ki |
= |
2.2 |
nM |
Binding affinity to A2A adenosine receptor |
CHEMBL1949672 |
| Relaxin receptor 1 |
Potency |
|
13761.4 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1: THP1 Hit Validation. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A1 receptor |
EC50 |
= |
10.2 |
nM |
Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay |
CHEMBL2010736 |
| Adenosine A1 receptor |
Inhibition |
= |
100.0 |
% |
Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay relative to 10 uM CPA |
CHEMBL2010736 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane |
CHEMBL2029296 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane |
CHEMBL2029296 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane |
CHEMBL2029296 |
| Adenosine A1 receptor |
Ki |
= |
5.1 |
nM |
Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex |
CHEMBL2040767 |
| Adenosine A1 receptor |
Ki |
= |
13.6 |
nM |
Displacement of [3H]CCPA from human recombinant adenosine A1 receptor |
CHEMBL2040767 |
| Adenosine A2a receptor |
Ki |
= |
15.0 |
nM |
Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatum |
CHEMBL2040767 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor |
CHEMBL2040767 |
| Adenosine A2b receptor |
Ki |
= |
1890.0 |
nM |
Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay |
CHEMBL2040767 |
| Adenosine A3 receptor |
Ki |
= |
6.2 |
nM |
Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells |
CHEMBL2040767 |
| Adenosine A2a receptor |
EC50 |
= |
17.6 |
nM |
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay |
CHEMBL2040767 |
| Adenosine A1 receptor |
Ki |
= |
3.0 |
nM |
Displacement of 3[H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 mins by Liquid scintillation analysis |
CHEMBL2069206 |
| Adenosine A2a receptor |
Ki |
= |
35.0 |
nM |
Displacement of 3[H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cells after 60 mins by Liquid scintillation analysis |
CHEMBL2069206 |
| Adenosine A3 receptor |
Ki |
= |
16.0 |
nM |
Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 mins gamma counter |
CHEMBL2069206 |
| Adenosine A1 receptor |
Ki |
= |
63.0 |
nM |
Displacement of 3[H]R-PIA from rat A1 adenosine receptor expressed in CHO cells after 60 min by Liquid scintillation analysis |
CHEMBL2069206 |
| Adenosine A2a receptor |
Ki |
= |
12.0 |
nM |
Displacement of 3[H]CGS21680 from rat A2A adenosine receptor expressed in HEK293 cells after 60 min by Liquid scintillation analysis |
CHEMBL2069206 |
| Adenosine A1 receptor |
Efficacy |
= |
100.0 |
% |
Agonist activity at human A1 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins relative to NECA |
CHEMBL2069206 |
| Unchecked |
Ratio Ki |
= |
8.0 |
|
Selectivity ratio of Ki for human A2A adenosine receptor expressed in HEK293 cells to Ki for human A1 adenosine receptor expressed in CHO cells |
CHEMBL2069206 |
| Geminin |
Potency |
|
1299.5 |
nM |
PubChem BioAssay. A quantitative high throughput screen for small molecules that induce DNA re-replication in MCF 10a normal breast cells. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Geminin |
Potency |
|
891.3 |
nM |
PubChem BioAssay. A quantitative high throughput screen for small molecules that induce DNA re-replication in SW480 colon adenocarcinoma cells. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Glucagon-like peptide 1 receptor |
Potency |
|
1995.3 |
nM |
PubChem BioAssay. qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
130.0 |
nM |
PubChem BioAssay. qHTS Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling: Hit Validation in Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A2a receptor |
IC50 |
= |
7.05 |
nM |
Displacement of [3H]MSX-2 from rat adenosine A2A receptor |
CHEMBL2150901 |
| Adenosine A2a receptor |
IC50 |
= |
366.0 |
nM |
Displacement of [3H]MSX-2 from rat adenosine A2A receptor in presence of 100 mM NaCl |
CHEMBL2150901 |
| Adenosine A2a receptor |
Ratio IC50 |
= |
49.0 |
|
Ratio of IC50 for rat adenosine A2A receptor in presence of 100 mM NaCl to IC50 for rat adenosine A2A receptor |
CHEMBL2150901 |
| Adenosine A1 receptor |
Inhibition |
= |
100.0 |
% |
Activity at human A1 adenosine receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production at 10 uM after 30 min |
CHEMBL2169760 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer |
CHEMBL2169760 |
| Adenosine A1 receptor |
Ki |
= |
6.8 |
nM |
Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer |
CHEMBL2169760 |
| Adenosine A3 receptor |
EC50 |
= |
63.1 |
nM |
Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells |
CHEMBL3045486 |
| Adenosine A2b receptor |
EC50 |
= |
316.23 |
nM |
Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells |
CHEMBL3045486 |
| Adenosine A2a receptor |
EC50 |
= |
251.19 |
nM |
Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells |
CHEMBL3045486 |
| Adenosine A1 receptor |
EC50 |
= |
31.62 |
nM |
Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells |
CHEMBL3045486 |
| Adenosine A2a receptor |
EC50 |
= |
18.0 |
nM |
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting |
CHEMBL2321867 |
| Adenosine A1 receptor |
Ki |
= |
13.6 |
nM |
Displacement of [3H]CCPA from human recombinant adenosine A1 receptor |
CHEMBL2321867 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells |
CHEMBL2321867 |
| Adenosine A2a receptor |
Ki |
= |
15.0 |
nM |
Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis |
CHEMBL2321867 |
| Adenosine A1 receptor |
Ki |
= |
5.1 |
nM |
Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis |
CHEMBL2321867 |
| Alpha-synuclein |
Potency |
|
28183.8 |
nM |
PubChem BioAssay. qHTS of alpha-syn Inhibitors. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A2a receptor |
IC50 |
= |
10.0 |
nM |
Binding affinity to human adenosine A2A receptor by radioligand displacement assay |
CHEMBL2390917 |
| Adenosine A2a receptor |
Ki |
= |
12.0 |
nM |
Binding affinity to human adenosine A2A receptor by radioligand displacement assay |
CHEMBL2390830 |
| Adenosine A2a receptor |
IC50 |
= |
15.0 |
nM |
Binding affinity to human adenosine A2A receptor by radioligand displacement assay |
CHEMBL2390830 |
| Adenosine A3 receptor |
Ki |
= |
25.0 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis |
CHEMBL2412992 |
| Adenosine A3 receptor |
Ki |
= |
149.0 |
nM |
Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 |
CHEMBL2412992 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis |
CHEMBL2412992 |
| Adenosine A2a receptor |
Ki |
= |
21.2 |
nM |
Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 |
CHEMBL2412992 |
| Adenosine A3 receptor |
Ki |
= |
73.0 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins |
CHEMBL2434872 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins |
CHEMBL2434872 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins |
CHEMBL2434872 |
| Adenosine A1 receptor |
EC50 |
= |
1.259 |
nM |
Agonist activity at human adenosine A1 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay |
CHEMBL3132785 |
| Adenosine A3 receptor |
EC50 |
= |
3.162 |
nM |
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay |
CHEMBL3132785 |
| Adenosine A2b receptor |
EC50 |
= |
3.162 |
nM |
Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay |
CHEMBL3132785 |
| Adenosine A2a receptor |
EC50 |
= |
12.59 |
nM |
Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay |
CHEMBL3132785 |
| Unchecked |
Selectivity ratio |
= |
4.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A2A receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Unchecked |
Selectivity ratio |
= |
1.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A2B receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Adenosine receptors; A1 & A3 |
Selectivity ratio |
= |
0.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A1 receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Cerebroside-sulfatase |
Potency |
|
7568.6 |
nM |
PubChem BioAssay. qHTS screen for enhancers of Arylsulfatase A (ASA1): LOPAC Validation Assay. (Class of assay: confirmatory) |
CHEMBL1201862 |
| DNA-(apurinic or apyrimidinic site) lyase |
Potency |
|
10000.0 |
nM |
PubChem BioAssay. qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A1 receptor |
Inhibition |
= |
105.0 |
% |
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry |
CHEMBL3217410 |
| Adenosine A1 receptor |
Activity |
= |
177.0 |
% |
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gs-mediated activation of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry |
CHEMBL3217410 |
| Adenosine A1 receptor |
Activity |
|
|
|
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs in presence of 1 uM adenosine A1 receptor antagonist XAC by spectrophotometry |
CHEMBL3217410 |
| Adenosine A1 receptor |
Ki |
= |
1122.02 |
nM |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control |
CHEMBL3217410 |
| Adenosine A1 receptor |
IC50 |
= |
0.7943 |
nM |
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry |
CHEMBL3217410 |
| Adenosine A1 receptor |
EC50 |
= |
1479.11 |
nM |
Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gs-mediated activation of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry |
CHEMBL3217410 |
| Adenosine A1 receptor |
Activity |
= |
73.0 |
% |
Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control |
CHEMBL3217410 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Binding affinity to human recombinant adenosine receptor A2a |
CHEMBL3259781 |
| Adenosine A2b receptor |
EC50 |
= |
330.0 |
nM |
Agonist activity at human recombinant adenosine receptor A2b by cAMP assay |
CHEMBL3259781 |
| Adenosine A1 receptor |
Ki |
= |
14.0 |
nM |
Binding affinity to human recombinant adenosine A1 receptor |
CHEMBL3259781 |
| Adenosine A3 receptor |
Ki |
= |
6.2 |
nM |
Binding affinity to human recombinant adenosine A3 receptor |
CHEMBL3259781 |
| Adenosine A2a receptor |
Ki |
= |
8.41 |
nM |
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method |
CHEMBL3414558 |
| Adenosine A1 receptor |
Ki |
= |
8.62 |
nM |
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method |
CHEMBL3414558 |
| Adenosine A2a receptor |
EC50 |
= |
12.58 |
nM |
Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method |
CHEMBL3414558 |
| Adenosine A2b receptor |
EC50 |
> |
10000.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method |
CHEMBL3414558 |
| Adenosine A3 receptor |
Ki |
= |
30.0 |
nM |
Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method |
CHEMBL3414558 |
| Endoplasmin |
Kd |
= |
200.0 |
nM |
Binding affinity to porcine pancreas rough microsomal GRP94 after 1 hr |
CHEMBL3425404 |
| Adenosine A2a receptor |
EC50 |
= |
45.0 |
nM |
Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay |
CHEMBL3739405 |
| Adenosine A3 receptor |
KB |
|
|
|
Antagonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as suppression of NECA-mediated inhibition of forskolin-stimulated cAMP accumulation preincubated for 15 mins followed by incubation with NECA for 15 mins and with forskolin for 3 mins by enzyme immunoassay |
CHEMBL3739405 |
| Adenosine A1 receptor |
EC50 |
= |
1000.0 |
nM |
Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay |
CHEMBL3769381 |
| Adenosine A2a receptor |
EC50 |
= |
338.84 |
nM |
Agonist activity at human Adenosine A2A receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay |
CHEMBL3769381 |
| Adenosine A2b receptor |
EC50 |
= |
14791.08 |
nM |
Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay |
CHEMBL3769381 |
| Adenosine A1 receptor |
pKA |
= |
4.4 |
|
Binding affinity to human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 |
CHEMBL3769381 |
| Adenosine A2a receptor |
pKA |
= |
5.9 |
|
Binding affinity to human Adenosine A2A receptor expressed in yeast cells coexpressed with GPA1/Galphas |
CHEMBL3769381 |
| Adenosine A2b receptor |
pKA |
= |
4.2 |
|
Binding affinity to human Adenosine A2B receptor expressed in yeast cells coexpressed with GPA1/Galphas |
CHEMBL3769381 |
| Adenosine A1 receptor |
IC50 |
= |
0.2089 |
nM |
Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis |
CHEMBL3769381 |
| Adenosine A3 receptor |
IC50 |
= |
0.4898 |
nM |
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis |
CHEMBL3769381 |
| Adenosine A1 receptor |
Activity |
= |
-73.4 |
% |
Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis relative to total forskolin |
CHEMBL3769381 |
| Adenosine A3 receptor |
Activity |
= |
-44.1 |
% |
Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis relative to total forskolin |
CHEMBL3769381 |
| Adenosine A2a receptor |
IC50 |
= |
37.0 |
nM |
Displacement of [3H]CGS 21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells |
CHEMBL3774372 |
| Serotonin 1a (5-HT1a) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]WAY100635 from human 5-HT1AR expressed in CHO cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 1d (5-HT1d) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]5-CT from human 5-HT1D receptor expressed in HEK-T cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 1b (5-HT1b) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]5-CT from human 5-HT1BR expressed in HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 1e (5-HT1e) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]5-HT from human 5-HT1E receptor expressed in HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 4 (5-HT4) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]GR113808 from human 5-HT4 receptor at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 6 (5-HT6) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 7 (5-HT7) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]LSD from human 5-HT7A receptor expressed in HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 3a (5-HT3a) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]GR65630 from human 5-HT3 receptor expressed in HEK-T cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 2a (5-HT2a) receptor |
Ki |
> |
10000.0 |
nM |
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method |
CHEMBL3862033 |
| Serotonin 2a (5-HT2a) receptor |
Inhibition |
< |
10.0 |
% |
Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 2b (5-HT2b) receptor |
Inhibition |
< |
10.0 |
% |
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Serotonin 2c (5-HT2c) receptor |
Inhibition |
< |
10.0 |
% |
Displacement of [3H]mesulergine from human 5-HT2CR expressed in Flp-In HEK cell membranes at 10 uM incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Adenosine A1 receptor |
Ki |
= |
6.8 |
nM |
Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method |
CHEMBL3862033 |
| Adenosine A2a receptor |
Ki |
= |
10.3 |
nM |
Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from rat adenosine receptor A2A after 60 mins by liquid scintillation counting method |
CHEMBL3862033 |
| Transmembrane domain-containing protein TMIGD3 |
Ki |
= |
16.0 |
nM |
Displacement of [125l]N 6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from recombinant human A3AR expressed in CHO cell membranes after 60 mins by gamma counting method |
CHEMBL3862033 |
| Adenosine A3 receptor |
Imax |
= |
100.0 |
% |
Agonist activity at recombinant mouse A3AR expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation at 10 uM after 15 mins relative to adenosine-5'-N-ethyluronamide |
CHEMBL3862033 |
| Serotonin 5a (5-HT5a) receptor |
Inhibition |
< |
50.0 |
% |
Displacement of [3H]LSD from human 5-HT5A receptor expressed in Flp-In-CHO cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method relative to control |
CHEMBL3862033 |
| Adenosine A2a receptor |
IC50 |
= |
37.0 |
nM |
Displacement of [3H]CGS 21680 from human recombinant adenosine receptor A2A expressed in HEK293 cells measured after 120 mins by scintillation counting method |
CHEMBL3875185 |
| Adenosine A2a receptor |
koff |
|
0.03 |
min^-1 |
The binding kinetics for ZM241385 as determined by using radioligand association and dissociation assay. |
CHEMBL3885741 |
| Adenosine A2a receptor |
kon |
|
0.0005 |
nM^-1 min^-1 |
The binding kinetics for ZM241385 as determined by using radioligand association and dissociation assay. |
CHEMBL3885741 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]NECA from human adenosine receptor A2A expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method |
CHEMBL4011624 |
| Adenosine A1 receptor |
Ki |
= |
4.6 |
nM |
Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method |
CHEMBL4011624 |
| Adenosine A3 receptor |
Ki |
= |
12.8 |
nM |
Displacement of [3H]HEMADO from human adenosine receptor A3 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method |
CHEMBL4011624 |
| Adenosine A2b receptor |
EC50 |
= |
1510.0 |
nM |
Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method |
CHEMBL4011624 |
| Adenosine A2b receptor |
Ki |
= |
1890.0 |
nM |
Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method |
CHEMBL4011624 |
| Unchecked |
Activity |
|
|
|
Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in adiponectin production at 20.4 uM after 7 days in presence of IDX |
CHEMBL4017496 |
| Unchecked |
Activity |
= |
20.0 |
% |
Induction of adipogenesis in mouse 7F2 cells transfected with human AR assessed as increase in the production of adiponectin at 1 to 10 uM after 7 to 12 days by staining based oil red O phase contrast microscopic method relative to control |
CHEMBL4017496 |
| Adenosine A2a receptor |
Ki |
= |
481.0 |
nM |
Displacement of MRS5346 from C-terminal 10xHis and 1D4-tagged C-terminal-truncated human A2A adenosine receptor (1 to 316 residues) expressed in Pichia pastoris expression system after 1 hr by fluorescence polarization assay |
CHEMBL4033759 |
| Adenosine A1 receptor |
EC50 |
= |
0.7586 |
nM |
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A1 receptor |
Emax |
= |
101.0 |
% |
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay relative to control |
CHEMBL4043287 |
| Adenosine A1 receptor |
log(activity) |
= |
8.98 |
|
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring agonist transduction coefficient preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A1 receptor |
EC50 |
= |
0.4365 |
nM |
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4 dye-based fluorescence assay |
CHEMBL4043287 |
| Adenosine A1 receptor |
Emax |
= |
54.0 |
% |
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4 dye-based fluorescence assay relative to control |
CHEMBL4043287 |
| Adenosine A1 receptor |
log(activity) |
= |
9.31 |
|
Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by measuring agonist transduction coefficient by Fluo-4 dye-based fluorescence assay |
CHEMBL4043287 |
| Adenosine A2a receptor |
EC50 |
= |
3.3110000000000004 |
nM |
Agonist activity at human A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A2a receptor |
Emax |
= |
105.0 |
% |
Agonist activity at human A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay relative to control |
CHEMBL4043287 |
| Adenosine A2a receptor |
log(activity) |
= |
8.53 |
|
Agonist activity at human A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring agonist transduction coefficient preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A2b receptor |
EC50 |
= |
15.85 |
nM |
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A2b receptor |
Emax |
= |
40.0 |
% |
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay relative to control |
CHEMBL4043287 |
| Adenosine A2b receptor |
log(activity) |
= |
7.65 |
|
Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring agonist transduction coefficient preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A3 receptor |
EC50 |
= |
14.13 |
nM |
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Adenosine A3 receptor |
Emax |
= |
97.0 |
% |
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay relative to control |
CHEMBL4043287 |
| Adenosine A3 receptor |
log(activity) |
= |
7.94 |
|
Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by measuring agonist transduction coefficient preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay |
CHEMBL4043287 |
| Endoplasmin |
Kd |
= |
200.0 |
nM |
Displacement of [3H]NECA from GRP94 in porcine pancreas rough microsomes by liquid scintillation spectrometry |
CHEMBL4152387 |
| Adenosine A3 receptor |
Ki |
= |
75.5 |
nM |
Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins |
CHEMBL4261564 |
| SARS-CoV-2 |
Inhibition |
= |
5.19 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging |
CHEMBL4303101 |
| Adenosine A3 receptor |
IC50 |
= |
1.148 |
nM |
Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
15.49 |
nM |
Agonist activity at wild type human A3 receptor L90'3.32A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Unchecked |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor T94'3.36A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor F168'5.29A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.4898 |
nM |
Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.2089 |
nM |
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
3.802 |
nM |
Agonist activity at wild type human A3 receptor M174'5.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
109.65 |
nM |
Agonist activity at wild type human A3 receptor M177'5.38A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.6166 |
nM |
Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor L246'6.51A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.2951 |
nM |
Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor N250'6.55A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
1.202 |
nM |
Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.5888 |
nM |
Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.7762 |
nM |
Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor I268'7.39A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor S271'7.42A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
pIC50 |
|
|
|
Agonist activity at wild type human A3 receptor H272'7.43A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A3 receptor |
IC50 |
= |
0.257 |
nM |
Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay |
CHEMBL4321810 |
| Adenosine A2a receptor |
Ki |
= |
20.0 |
nM |
Agonist activity at human adenosine receptor A2A |
CHEMBL4351010 |
| Adenosine A1 receptor |
Ki |
= |
3.0 |
nM |
Displacement of [3H]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A1 receptor |
Ki |
= |
0.45 |
nM |
Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A2a receptor |
Ki |
= |
35.0 |
nM |
Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A3 receptor |
Ki |
= |
35.0 |
nM |
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from human A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A3 receptor |
Ki |
= |
14.1 |
nM |
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from mouse A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A3 receptor |
Ki |
= |
113.0 |
nM |
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from rat A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A1 receptor |
EC50 |
= |
5.03 |
nM |
Agonist activity at human A1A adenosine receptor expressed in CHOKI cells assessed as induction of beta-arrestin2 recruitment after 60 mins |
CHEMBL4368904 |
| Adenosine A2b receptor |
EC50 |
= |
140.0 |
nM |
Agonist activity at human A2B adenosine receptor by cell based assay |
CHEMBL4368904 |
| Adenosine A1 receptor |
EC50 |
= |
0.12 |
nM |
Agonist activity at human A1A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay |
CHEMBL4368904 |
| Adenosine A1 receptor |
Ki |
= |
6.8 |
nM |
Binding affinity to human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A1 receptor |
Ki |
= |
63.0 |
nM |
Displacement of [3H]N6-R-phenylisopropyladenosine from rat A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay |
CHEMBL4368904 |
| Adenosine A2a receptor |
Ki |
= |
2.2 |
nM |
Binding affinity to human A2A adenosine receptor expressed in HEK293 cell membranes |
CHEMBL4368904 |
| Adenosine A2a receptor |
Ki |
= |
12.0 |
nM |
Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from rat A2A adenosine receptor expressed in HEK293 cell membranes at 10 uM after 60 mins by scintillation proximity assay relative to adenosine 5-N-ethyluronamide |
CHEMBL4368904 |
| Adenosine A3 receptor |
Emax |
= |
100.0 |
% |
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis relative to adenosine-5'-Nethyluronamide |
CHEMBL4402597 |
| Adenosine A3 receptor |
EC50 |
= |
188.0 |
nM |
Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis |
CHEMBL4402597 |
| Replicase polyprotein 1ab |
Inhibition |
= |
23.96 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| Replicase polyprotein 1ab |
Inhibition |
= |
1.51 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
0.15 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
0.0 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
0.15 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| SARS-CoV-2 |
Inhibition |
= |
0.0 |
% |
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging |
CHEMBL4495565 |
| Endoplasmin |
Kd |
= |
530.0 |
nM |
Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay |
CHEMBL4680372 |
| Endoplasmin |
Ki |
= |
110.0 |
nM |
Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay |
CHEMBL4680372 |
| Heat shock protein HSP 90-alpha |
Kd |
= |
46000.0 |
nM |
Displacement of FITC-geldanamycin from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay |
CHEMBL4680372 |
| Heat shock protein HSP 90-alpha |
Ki |
= |
2700.0 |
nM |
Displacement of FITC-geldanamycin from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay |
CHEMBL4680372 |
| Unchecked |
Selectivity Index |
= |
86.8 |
|
Selectivity index, ratio of Kd for displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay to Kd for displacement of FITC-geldanamycin from HSP90alpha (unknown origin) after 24 hrs by fluorescence polarization assay |
CHEMBL4680372 |
| Adenosine A2b receptor |
EC50 |
= |
94.8 |
nM |
Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay |
CHEMBL4680372 |
| Adenosine A1 receptor |
Ki |
= |
4.6 |
nM |
Displacement of [3H]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay |
CHEMBL4706508 |
| Adenosine A2a receptor |
Ki |
= |
16.0 |
nM |
Displacement of [3H]-NECA from human A2A receptor stably expressed in CHO cell membranes by radioligand competitive binding assay |
CHEMBL4706508 |
| Adenosine A3 receptor |
Ki |
= |
12.8 |
nM |
Displacement of [3H]-HEMADO from human A3 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay |
CHEMBL4706508 |
| Adenosine A1 receptor |
Activity |
|
|
|
Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as induction of positive change of cellular impedance at 1 uM incubated for 2 hrs by xCELLigence real-time cell analysis |
CHEMBL4715802 |
| Adenosine A1 receptor |
EC50 |
= |
0.5012 |
nM |
Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of ERK1/2 phosphorylation incubated for 5 mins |
CHEMBL4715802 |
| Unchecked |
Activity |
|
|
|
Stimulation of ERK1/2 phosphorylation in Flp-In-CHO cells incubated for 5 mins |
CHEMBL4715802 |
| Adenosine A1 receptor |
%max |
= |
103.0 |
% |
Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of ERK1/2 phosphorylation incubated for 5 mins relative to NECA |
CHEMBL4715802 |
| Adenosine A1 receptor |
Activity |
|
|
|
Agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as induction of positive change of cellular impedance at 1 uM incubated for 1.5 hrs followed by addition of 1 uM A1AR selective antagonist SLV320 for 16 mins by xCELLigence real-time cell analysis |
CHEMBL4715802 |
| Adenosine A1 receptor |
Activity |
= |
108.0 |
% |
Binding affinity to human adenosine A1 receptor expressed in Flp-In-CHO cell membranes assessed as [3H]DPCPX binding level at 10 uM incubated for 1 hr followed by washing by liquid scintillation counting based equilibrium radioligand binding assay (Rvb = 93 +/- 10%) |
CHEMBL4715802 |
| Adenosine A1 receptor |
Activity |
= |
57.0 |
% |
Binding affinity to human adenosine A1 receptor expressed in Flp-In-CHO cell membranes assessed as basal [35S]GTP-gamma-S incorporation level at 10 uM incubated for 40 mins followed by washing by liquid scintillation counting (Rvb = 41 +/- 3%) |
CHEMBL4715802 |
| Adenosine A1 receptor |
Activity |
= |
99.0 |
% |
Binding affinity to human adenosine A1 receptor expressed in NECA-pre-treated Flp-In-CHO cell membranes assessed as [35S]GTP-gamma-S incorporation level at 10 uM incubated for 40 mins followed by washing by liquid scintillation counting (Rvb = 41 +/- 3%) |
CHEMBL4715802 |
| Adenosine A1 receptor |
Delta Tm |
= |
4.0 |
degrees C |
Binding affinity to human adenosine A1 receptor expressed in Sf9 cells assessed change in protein melting temperature at 10 uM incubated for 30 mins by Thermo-fluor assay |
CHEMBL4715802 |
| Adenosine A1 receptor |
Tm |
= |
38.7 |
degrees C |
Binding affinity to human adenosine A1 receptor expressed in Sf9 cells assessed protein melting temperature at 10 uM incubated for 30 mins by Thermo-fluor assay (Rvb = 35.2 +/- 1.6 degC) |
CHEMBL4715802 |
| Adenosine A1 receptor |
EC50 |
= |
1.622 |
nM |
Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay |
CHEMBL4715802 |
| Adenosine A2a receptor |
EC50 |
= |
2.512 |
nM |
Irreversible agonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay |
CHEMBL4715802 |
| Adenosine A2b receptor |
EC50 |
= |
42.66 |
nM |
Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay |
CHEMBL4715802 |
| Adenosine A3 receptor |
EC50 |
= |
15.85 |
nM |
Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay |
CHEMBL4715802 |
| Unchecked |
Activity |
|
|
|
Effect on forskolin-induced cAMP accumulation in Flp-In-CHO cells incubated for 30 mins by LANCE cAMP detection assay |
CHEMBL4715802 |
| Adenosine A3 receptor |
Ki |
= |
44.1 |
nM |
Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay |
CHEMBL5038675 |
| Adenosine A3 receptor |
Ki |
= |
19.6 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay |
CHEMBL5038675 |
| Adenosine A1 receptor |
Ki |
= |
5011.87 |
nM |
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay |
CHEMBL5042471 |
| Adenosine A1 receptor |
EC50 |
= |
1.096 |
nM |
Agonist activity at human adenosine A1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
Emax |
= |
50.11 |
% |
Agonist activity at human adenosine A1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by measuring maximal efficacy incubated for 30 mins by LANCE ultra assay relative to control |
CHEMBL5096218 |
| Adenosine A1 receptor |
Ki |
= |
245.47 |
nM |
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A2a receptor |
EC50 |
= |
11.22 |
nM |
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay |
CHEMBL5096218 |
| Adenosine A2a receptor |
Emax |
= |
22.03 |
% |
Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by measuring maximal efficacy incubated for 30 mins by LANCE ultra assay relative to control |
CHEMBL5096218 |
| Adenosine A2b receptor |
EC50 |
= |
63.1 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay |
CHEMBL5096218 |
| Adenosine A2b receptor |
Emax |
= |
68.12 |
% |
Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by measuring maximal efficacy incubated for 30 mins by LANCE ultra assay relative to control |
CHEMBL5096218 |
| Adenosine A3 receptor |
EC50 |
= |
14.79 |
nM |
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay |
CHEMBL5096218 |
| Adenosine A3 receptor |
Emax |
= |
34.34 |
% |
Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation by measuring maximal efficacy incubated for 30 mins by LANCE ultra assay relative to control |
CHEMBL5096218 |
| Adenosine A1 receptor |
Ki |
= |
416.87 |
nM |
Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
K |
= |
2.04 |
10^5/M/min |
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as association rate constant (Kon) by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
K |
= |
0.049 |
/min |
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as dissociation constant (Koff) by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
Kd |
= |
234.42 |
nM |
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
TIME |
= |
0.3495 |
hr |
Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as residence time by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
K |
= |
2.29 |
10^5/M/min |
Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as association rate constant (Kon) by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
K |
= |
0.066 |
/min |
Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as dissociation constant (Koff) by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
Kd |
= |
295.12 |
nM |
Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A1 receptor |
TIME |
= |
0.264 |
hr |
Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as residence time by NanoBRET competition binding assay |
CHEMBL5096218 |
| Adenosine A3 receptor |
IC50 |
= |
0.9333 |
nM |
Antagonist activity at wild type A3R (unknown origin) expressed in Flp-In-CHO cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins |
CHEMBL5108055 |
| Adenosine A3 receptor |
Ki |
= |
190.55 |
nM |
Binding affinity to wild type A3R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
IC50 |
= |
1.122 |
nM |
Antagonist activity at wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins |
CHEMBL5108055 |
| Adenosine A1 receptor |
Ki |
= |
83.18 |
nM |
Binding affinity to wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
Kd |
= |
213.8 |
nM |
Binding affinity to wild type A1R (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Unchecked |
pKd |
|
|
|
Binding affinity to A1R T91 3.36A mutant (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
Kd |
= |
4168.69 |
nM |
Binding affinity to A1R E172 5.30A mutant (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
pKd |
|
|
|
Binding affinity to A1R L250 6.51A mutant (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
Kd |
= |
9.12 |
nM |
Binding affinity to A1R H251 6.52A mutant (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
Kd |
= |
489.78 |
nM |
Binding affinity to A1R S267 7.32A mutant (unknown origin) in by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Unchecked |
Kd |
= |
3548.13 |
nM |
Binding affinity to A1R Y271 7.36A mutant (unknown origin) by saturation NanoBRET binding assay |
CHEMBL5108055 |
| Adenosine A1 receptor |
EC50 |
= |
1.38 |
nM |
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation incubated for 30 mins by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A1 receptor |
Emax |
= |
104.0 |
% |
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation incubated for 30 mins by LANCE cAMP assay relative to control |
CHEMBL5120905 |
| Adenosine A1 receptor |
EC50 |
= |
4.898 |
nM |
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of calcium mobilization by calcium mobilization assay |
CHEMBL5120905 |
| Adenosine A1 receptor |
Emax |
= |
24.0 |
% |
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of calcium mobilization by calcium mobilization assay relative to control |
CHEMBL5120905 |
| Adenosine A2a receptor |
EC50 |
= |
4.7860000000000005 |
nM |
Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A2b receptor |
EC50 |
= |
4.7860000000000005 |
nM |
Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A3 receptor |
EC50 |
= |
47.86 |
nM |
Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A1 receptor |
log(Tau/KA) |
= |
8.86 |
|
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation by measuring agonist transduction coefficient (tau/KA) incubated for 30 mins by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A1 receptor |
log(Tau/KA) |
= |
8.38 |
|
Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of calcium mobilization by measuring agonist transduction coefficient (tau/KA) by calcium mobilization assay |
CHEMBL5120905 |
| Adenosine A2b receptor |
EC50 |
= |
12.3 |
nM |
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay |
CHEMBL5120905 |
| Adenosine A2b receptor |
EC50 |
= |
331.13 |
nM |
Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay |
CHEMBL5120905 |
| Unchecked |
Activity |
|
|
|
Effect on cAMP accumulation in HEK293T cells by GloSensor cAMP accumulation assay |
CHEMBL5126601 |
| Adenosine A1 receptor |
EC50 |
= |
1.82 |
nM |
Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay |
CHEMBL5131549 |
| Adenosine A3 receptor |
EC50 |
= |
0.1175 |
nM |
Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay |
CHEMBL5131549 |
| Adenosine A1 receptor |
Ki |
= |
204.17 |
nM |
Displacement of CA200645 from NLuc human A1 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay |
CHEMBL5131549 |
| Adenosine A3 receptor |
Ki |
= |
89.13 |
nM |
Displacement of CA200645 from NLuc human A3 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay |
CHEMBL5131549 |
| WI-38 |
IC50 |
> |
10000.0 |
nM |
Cytotoxicity against human WI-38 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay |
CHEMBL5131549 |
| PC-3 |
IC50 |
> |
10000.0 |
nM |
Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay |
CHEMBL5131549 |
| HCT-116 |
IC50 |
> |
10000.0 |
nM |
Cytotoxicity against human HCT-116 cells assessed as cell viability incubated for 72 to 96 hrs by MTT assay |
CHEMBL5131549 |
| Adenosine A3 receptor |
EC50 |
= |
177.0 |
nM |
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay |
CHEMBL5154659 |
| Adenosine A3 receptor |
Emax |
= |
99.5 |
% |
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment maximum efficacy by luciferase based NanoBiT assay |
CHEMBL5154659 |
| Adenosine A3 receptor |
EC50 |
= |
154.0 |
nM |
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay |
CHEMBL5154659 |
| Adenosine A3 receptor |
Emax |
= |
99.4 |
% |
Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment maximum efficacy by luciferase based NanoBiT assay |
CHEMBL5154659 |
| Unchecked |
Ratio IC50 |
= |
17.0 |
|
Selectivity ratio of IC50 for human Hsp90alpha to IC50 for dog GRP94 by fluorescence polarization assay |
CHEMBL5214924 |
| Heat shock protein 90 beta |
Kd |
= |
2800.0 |
nM |
Inhibition of N-terminal full length dog GRP94 (73 to 754 residues) expressed in Escherichia coli BL21(DE3) measured after 24 hrs by fluorescence polarization assay |
CHEMBL5214924 |
| Heat shock protein HSP 90-alpha |
Kd |
= |
14000.0 |
nM |
Inhibition of human N-terminal His-tagged Hsp90alpha (1 to 236 residues) expressed in Escherichia coli BL21(DE3) measured after 24 hrs by fluorescence polarization assay |
CHEMBL5214924 |
