| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Binding affinity for adenosine A1 receptor as displacement of [3H]R-PIA from rat brain membranes at 10e-4 M |
CHEMBL1131608 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Binding affinity for adenosine A2A receptor as displacement of [3H]-CGS- 21680 from rat striatal membranes at 10e-4 M |
CHEMBL1131608 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes |
CHEMBL1131608 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
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 |
= |
56.0 |
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 |
= |
1.1 |
nM |
Binding affinity for rat A3-adenosine receptor expressed in chinese hamster ovarian cells (assayed by the displacement of specific [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5''-N-methyluronamide) |
CHEMBL1127835 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
49.0 |
|
Ratio of binding affinities for A1 receptor compared to that of A3 receptor |
CHEMBL1127835 |
| Unchecked |
Ratio |
= |
51.0 |
|
Ratio of binding affinities for A2 receptor compared to that of A3 receptor |
CHEMBL1127835 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Binding affinity for rat Adenosine A3 receptor in CHO cells using [125I]iodo-AB-MECA |
CHEMBL1145992 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA. |
CHEMBL1131059 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680. |
CHEMBL1131059 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-. |
CHEMBL1131059 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
49.0 |
|
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 |
= |
51.0 |
|
Selectivity for binding affinity towards A2A adenosine receptor in rat striatal membrane and rat A3 receptor expressed in CHO cells. |
CHEMBL1131059 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Displacement of [3H]CHA from Adenosine A1 receptor in rat brain homogenates |
CHEMBL1129034 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor in rat striatal homogenates |
CHEMBL1129034 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]AB-MECA from cloned rat Adenosine A3 receptor in stably transfected CHO cells |
CHEMBL1129034 |
| Adenosine receptors; A1 & A3 |
Selectivity |
= |
49.0 |
|
Selectivity, ratio between A1 receptor binding affinity / A3 receptor binding affinity |
CHEMBL1129034 |
| Adenosine receptor A2a and A3 |
Selectivity |
= |
51.0 |
|
Selectivity, ratio between A2A receptor binding affinity / A3 receptor binding affinity |
CHEMBL1129034 |
| Adenosine A2a receptor |
Ki |
= |
370.0 |
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 |
= |
143.0 |
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 |
= |
32.0 |
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 A1 receptor |
Ki |
= |
54.0 |
nM |
Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes |
CHEMBL1127377 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes |
CHEMBL1127377 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA |
CHEMBL1127377 |
| Equilibrative nucleoside transporter 1 |
Ki |
= |
28200.0 |
nM |
Inhibition of [3H]S-(4-Nitrobenzyl)-6-thioinosine binding to adenosine uptake sites in rat brain membranes |
CHEMBL1127377 |
| Adenosine A3 receptor |
Selectivity ratio |
= |
22000.0 |
|
Selectivity for cloned rat A3 receptor |
CHEMBL1127377 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
49.0 |
|
Ratio of Ki for A1 and A3 receptors |
CHEMBL1127377 |
| Adenosine receptor A2a and A3 |
Ratio |
= |
51.0 |
|
Ratio of Ki for A2a and A3 receptors |
CHEMBL1127377 |
| Adenosine A1 receptor |
Ki |
= |
20.0 |
nM |
Binding affinity using [125I]ABA against human Adenosine A1 receptor |
CHEMBL1145953 |
| Adenosine A3 receptor |
Ki |
= |
4.4 |
nM |
Binding affinity using [125I]ABA against human Adenosine A3 receptor |
CHEMBL1145953 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
4.5 |
|
Ratio of binding affinity for human adenosine A1 and A3 receptors |
CHEMBL1145953 |
| Adenosine A3 receptor |
EC50 |
= |
1.0 |
nM |
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor |
CHEMBL1145953 |
| Adenosine A1 receptor |
Ki |
= |
33.1 |
nM |
Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. |
CHEMBL1131221 |
| Adenosine A2a receptor |
Ki |
= |
116.0 |
nM |
Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. |
CHEMBL1131221 |
| Adenosine A3 receptor |
Ki |
= |
30.0 |
nM |
Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
3.51 |
|
Inhibitory selectivity at Adenosine 2A receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
0.9 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
0.25 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 2A receptor. |
CHEMBL1131221 |
| Adenosine A3 receptor |
EC50 |
= |
3.6 |
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 |
= |
100.0 |
% |
Percent efficacy against human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Affinity for human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
1.6 |
nM |
Binding affinity towards human Adenosine A3 receptor wild type |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
0.9 |
nM |
Binding affinity towards Adenosine A3 receptor (W243A) |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
|
|
|
Binding affinity towards Adenosine A3 receptor (H95A receptor); Not determined |
CHEMBL1135592 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Binding affinity against adenosine A1 receptor from rat brain. |
CHEMBL1128362 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Binding affinity against adenosine A2A receptor from rat brain. |
CHEMBL1128362 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Binding affinity against adenosine A3 receptor from rat brain. |
CHEMBL1128362 |
| Adenosine A3 receptor |
Inhibition |
= |
44.4 |
% |
Ability to inhibit the adenylyl cyclase in CHO cells stably transfected with rat Adenosine A3 receptor at the concentration of 100 uM |
CHEMBL1128362 |
| Adenosine A3 receptor |
Inhibition |
= |
22.0 |
% |
Ability to inhibit the adenylyl cyclase in CHO cells stably transfected with rat Adenosine A3 receptor at the concentration of 0.1(uM) |
CHEMBL1128362 |
| Adenosine A3 receptor |
Effect |
|
|
|
Agonist elicited inhibition of adenylyl cyclase via rat Adenosine A3 receptor in transfected CHO cells and effect on IB-MECA was determined from dose response curves at the concentration of 100(uM); No antagonism |
CHEMBL1128362 |
| Adenosine A3 receptor |
Effect |
|
|
|
Agonist elicited inhibition of adenylyl cyclase via rat Adenosine A3 receptor in transfected CHO cells and effect on IB-MECA was determined from dose response curves at the concentration of 0.1(uM); No antagonism |
CHEMBL1128362 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
49.0 |
|
Ratio of the binding affinities against rat brain A1 and A3 receptors, KiA1/KiA3. |
CHEMBL1128362 |
| Adenosine receptor A2a and A3 |
Ratio |
= |
51.0 |
|
Ratio of the binding affinities against rat brain A2a and A3 receptors, KiA2a/KiA3. |
CHEMBL1128362 |
| Adenosine A3 receptor |
Ratio |
= |
9.1 |
|
Ratio of the concentration effecting adenylyl cyclase and binding affinity against rat brain A3 receptors. |
CHEMBL1128362 |
| Adenosine A3 receptor |
Ratio |
= |
91.0 |
|
Ratio of the concentration (0.1 uM) effecting adenylyl cyclase and binding affinity against rat brain A3 receptors |
CHEMBL1128362 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
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 |
= |
56.0 |
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 |
= |
1.1 |
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 A1 receptor |
Ki |
= |
54.0 |
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 |
= |
3.73 |
nM |
Binding affinity for human adenosine A1 receptor |
CHEMBL1132702 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane |
CHEMBL1132702 |
| Adenosine A2a receptor |
Ki |
= |
2520.0 |
nM |
Binding affinity for human adenosine A2A receptor |
CHEMBL1132702 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Binding affinity for rat adenosine A3 receptor |
CHEMBL1132702 |
| Adenosine A3 receptor |
Ki |
= |
1.2 |
nM |
Displacement of [125I]AB-MECA from membranes of HEK 293 cells expressing human Adenosine A3 receptor |
CHEMBL1132702 |
| Adenosine A2b receptor |
EC50 |
= |
11000.0 |
nM |
Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA |
CHEMBL1132702 |
| Adenosine A1 receptor |
Ki |
= |
51.2 |
nM |
Binding affinity towards recombinant human Adenosine A1 receptor was determined using [3H]R-PIA (2.0 nM) as radioligand |
CHEMBL1137867 |
| Adenosine A2a receptor |
Ki |
= |
2910.0 |
nM |
Binding affinity towards recombinant human Adenosine A2a receptor was determined using [3H]CGS-21680 (10 nM) as radioligand |
CHEMBL1137867 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Binding affinity towards human Adenosine A3 receptor stably transfected in CHO cells was determined using [125I]I-AB-MECA (1.0 nM) as radioligand |
CHEMBL1137867 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells |
CHEMBL1138752 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells |
CHEMBL1138752 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells |
CHEMBL1138752 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells |
CHEMBL1138800 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
49.0 |
|
Ratio of binding affinity for Adenosine A1 and Adenosine A3 receptors |
CHEMBL1138800 |
| Adenosine A1 receptor |
Ki |
= |
12.0 |
nM |
Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes |
CHEMBL1144357 |
| Adenosine A2a receptor |
Ki |
= |
40.0 |
nM |
Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes |
CHEMBL1144357 |
| Adenosine A3 receptor |
Ki |
= |
8.8 |
nM |
Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes |
CHEMBL1144357 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
3.33 |
|
Relative affinities against adenosine A2A and A1 receptors (ratio of KiA2A/KiA1) |
CHEMBL1144357 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
0.73 |
|
Relative affinities for adenosine A3 and A1 receptors (ratio of KiA3/KiA1) |
CHEMBL1144357 |
| Adenosine receptors; A2a & A3 |
Ratio |
= |
4.54 |
|
Relative affinities for adenosine A2A and A3 receptors (ratio of KiA2A/KiA3) |
CHEMBL1144357 |
| Adenosine A1 receptor |
Ki |
= |
51.0 |
nM |
Inhibition of [3H]R-PIA binding to human Adenosine A1 receptor expressed in CHO cells |
CHEMBL1142719 |
| Adenosine A2a receptor |
Ki |
= |
2900.0 |
nM |
Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells |
CHEMBL1142719 |
| Adenosine A2b receptor |
Activation |
= |
0.0 |
% |
Relative activation of human Adenosine A2B receptor at 10 uM treatment compared to 10 uM Cl-IB-MECA |
CHEMBL1142719 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells |
CHEMBL1142719 |
| Adenosine A3 receptor |
Activation |
= |
100.0 |
% |
Relative activation of human Adenosine A3 receptor expressed in CHO cells at 10 uM treatment compared to 10 uM Cl-IB-MECA |
CHEMBL1142719 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells |
CHEMBL1142719 |
| Adenosine A3 receptor |
IC50 |
= |
1.2 |
nM |
Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA |
CHEMBL1140374 |
| Adenosine A3 receptor |
Ki |
= |
0.84 |
nM |
Binding affinity towards human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA |
CHEMBL1140374 |
| Adenosine A1 receptor |
Ki |
= |
3.98 |
nM |
Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells |
CHEMBL1147002 |
| Adenosine A2a receptor |
Ki |
= |
510.0 |
nM |
Displacement of [125I]ZM241385 from human adenosine A2A receptor in HEK cells |
CHEMBL1147002 |
| Adenosine A3 receptor |
Ki |
= |
0.215 |
nM |
Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells |
CHEMBL1147002 |
| Adenosine receptors; A1 & A3 |
Ratio Ki |
= |
18.5 |
|
Selectivity for human adenosine A3 receptor over human adenosine A1 receptor |
CHEMBL1147002 |
| Adenosine A3 receptor |
ED50 |
= |
28.0 |
nM |
Activity at adenosine A3 receptor expressed in HEK293 cells by inhibition of isoprotenol-stimulated cAMP gated channel |
CHEMBL1147002 |
| Adenosine A2b receptor |
Ki |
= |
2040.0 |
nM |
Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells |
CHEMBL1147002 |
| Adenosine A3 receptor |
Ki |
= |
4.4 |
nM |
Binding affinity to human adenosine A3 receptor |
CHEMBL1146991 |
| Adenosine receptors; A1 & A3 |
Selectivity ratio |
= |
4.5 |
|
Selectivity for human adenosine A3 receptor over human adenosine A1 receptor |
CHEMBL1146991 |
| ScN2a |
EC50 |
> |
25000.0 |
nM |
Reduction of PrPSC accumulation in ScN2a cells |
CHEMBL1139220 |
| Adenosine A3 receptor |
Ki |
= |
2.0 |
nM |
Inhibitory constant against human adenosine A3 receptor |
CHEMBL1139220 |
| Adenosine A1 receptor |
Activity |
|
|
|
Inhibitory constant aganist human adenosine A1 receptor |
CHEMBL1139220 |
| Adenosine A2a receptor |
Activity |
|
|
|
Inhibitory constant against human adenosine A2a receptor |
CHEMBL1139220 |
| Adenosine A1 receptor |
Ki |
= |
5.9 |
nM |
Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A1 receptor expressed in HEK293 cells |
CHEMBL1145629 |
| Adenosine A2a receptor |
Ki |
= |
1000.0 |
nM |
Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from mouse recombinant adenosine A2A receptor expressed in HEK293 cells |
CHEMBL1145629 |
| Adenosine A3 receptor |
Ki |
= |
0.087 |
nM |
Displacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cells |
CHEMBL1145629 |
| Unchecked |
Ratio Ki |
= |
68.0 |
|
Selectivity for mouse adenosine A3 receptor over mouse adenosine A1 receptor |
CHEMBL1145629 |
| Adenosine A1 receptor |
Ki |
= |
49.3 |
nM |
Displacement of radioligand from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1145629 |
| Adenosine A2a receptor |
Ki |
= |
93.1 |
nM |
Displacement of radioligand from human adenosine A2A receptor expressed in HEK293 cells |
CHEMBL1145629 |
| Adenosine A3 receptor |
Ki |
= |
1.74 |
nM |
Displacement of radioligand from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1145629 |
| Adenosine receptors; A1 & A3 |
Ratio Ki |
= |
28.0 |
|
Selectivity for human adenosine A3 receptor over human adenosine A1 receptor |
CHEMBL1145629 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Displacement of radioligand from rat adenosine A1 receptor |
CHEMBL1145629 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Displacement of radioligand from rat adenosine A2A receptor |
CHEMBL1145629 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of radioligand from rat A3 adenosine receptor |
CHEMBL1145629 |
| Unchecked |
Ratio Ki |
= |
49.0 |
|
Selectivity for rat adenosine A3 receptor over rat adenosine A1 receptor |
CHEMBL1145629 |
| Adenosine A2b receptor |
EC50 |
>= |
10000.0 |
nM |
Activation of mouse adenosine A2B receptor |
CHEMBL1145629 |
| Adenosine A1 receptor |
Ki |
= |
51.0 |
nM |
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1140153 |
| Adenosine A2a receptor |
Ki |
= |
2900.0 |
nM |
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in HEK293 cells |
CHEMBL1140153 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]I-AB-MECA from rat adenosine A3 receptor expressed in CHO cells |
CHEMBL1140153 |
| Adenosine A3 receptor |
Ki |
= |
1.0 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1140153 |
| Adenosine A3 receptor |
Ki |
= |
0.7 |
nM |
Displacement of radiolabeled IB-MECA from human adenosine A3 receptor |
CHEMBL1140203 |
| Adenosine A3 receptor |
IC50 |
= |
1.2 |
nM |
Displacement of radiolabeled IB-MECA from human adenosine A3 receptor |
CHEMBL1140203 |
| Adenosine A3 receptor |
IC50 |
= |
2.5 |
nM |
Inhibition of human adenosine A3 receptor |
CHEMBL1155111 |
| Adenosine A1 receptor |
Ki |
= |
51.0 |
nM |
Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1153082 |
| Adenosine A2a receptor |
Ki |
= |
2900.0 |
nM |
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1153082 |
| Adenosine A3 receptor |
Ki |
= |
1.0 |
nM |
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1153082 |
| Adenosine A3 receptor |
Ki |
= |
1.4 |
nM |
Binding affinity to human adenosine A3 receptor |
CHEMBL1153082 |
| Adenosine A3 receptor |
Activity |
|
|
|
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of cAMP accumulation |
CHEMBL1153082 |
| Adenosine A3 receptor |
Inhibition |
= |
99.0 |
% |
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 |
| H9c2 |
Inhibition |
|
|
% |
Cardioprotective effect against hypoxic simulated ischemia in rat H9c2 cells assessed as reduction in cell death at 100 nM after 12 hrs by propidium iodide staining-based inverted microscopy in presence of adenosine A3 receptor antagonist MRS-1191 |
CHEMBL1158581 |
| H9c2 |
Inhibition |
= |
54.1 |
% |
Cardioprotective effect against hypoxic simulated ischemia in rat H9c2 cells assessed as reduction in cell death at 100 nM after 12 hrs by propidium iodide staining-based inverted microscopy |
CHEMBL1158581 |
| H9c2 |
Inhibition |
|
|
% |
Cardioprotective effect against hypoxic simulated ischemia in rat H9c2 cells assessed as reduction in cell death at 100 nM after 12 hrs by propidium iodide staining-based inverted microscopy |
CHEMBL1158581 |
| H9c2 |
Inhibition |
|
|
% |
Cardioprotective effect against hypoxic simulated ischemia in rat H9c2 cells assessed as reduction in cell death at 10 nM after 12 hrs by propidium iodide staining-based inverted microscopy |
CHEMBL1158581 |
| Relaxin receptor 1 |
Potency |
= |
15848.9 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans |
CHEMBL1697731 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents |
CHEMBL1697731 |
| Hepatotoxicity |
Hepatotoxicity |
|
|
|
Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents |
CHEMBL1697731 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
2908.1 |
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 |
|
23109.3 |
nM |
PUBCHEM_BIOASSAY: Nrf2 qHTS screen for inhibitors: Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493163, AID504444, AID504648] |
CHEMBL1201862 |
| Nuclear factor erythroid 2-related factor 2 |
Potency |
|
29092.9 |
nM |
PUBCHEM_BIOASSAY: Nrf2 qHTS screen for inhibitors. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493153, AID493163, AID504648] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
9200.0 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485345, AID485355] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
11577.4 |
nM |
PUBCHEM_BIOASSAY: qHTS 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):AID493106, AID493143] |
CHEMBL1201862 |
| Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 |
Potency |
|
8912.5 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504404] |
CHEMBL1201862 |
| 6-phospho-1-fructokinase |
Potency |
|
16944.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Validation Assay to Find Inhibitors of T. brucei phosphofructokinase. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488768, AID492961] |
CHEMBL1201862 |
| Chromobox protein homolog 1 |
Potency |
|
100000.0 |
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 |
|
183.6 |
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 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
5011.9 |
nM |
PUBCHEM_BIOASSAY: qHTS screen for small molecules that inhibit ELG1-dependent DNA repair in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493107, AID493125] |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
919.6 |
nM |
PUBCHEM_BIOASSAY: Validation screen for small molecules that inhibit ELG1-dependent DNA repair in human embryonic kidney (HEK293T) cells expressing luciferase-tagged ELG1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493125, AID504467] |
CHEMBL1201862 |
| High-affinity choline transporter |
IC50 |
|
2374.75 |
nM |
PUBCHEM_BIOASSAY: Dose responses of compounds that inhibit the Choline Transporter (CHT) - 5 point CRC. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488975, AID488997, AID493221, AID493222] |
CHEMBL1201862 |
| Plasmodium falciparum |
Potency |
|
10417.9 |
nM |
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 96 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488745, AID488752, AID488774, AID504848, AID504850] |
CHEMBL1201862 |
| Plasmodium falciparum |
Potency |
|
20786.5 |
nM |
PUBCHEM_BIOASSAY: Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID488752, AID488774, AID504848, AID504850] |
CHEMBL1201862 |
| Mothers against decapentaplegic homolog 3 |
Potency |
|
17782.8 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of TGF-b. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588856, AID588860] |
CHEMBL1201862 |
| High-affinity choline transporter |
IC50 |
|
1825.63 |
nM |
PUBCHEM_BIOASSAY: Dose responses of compounds that inhibit the Choline Transporter (CHT) - 10 point CRC. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Geminin |
Potency |
|
28183.8 |
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 |
| Unchecked |
Potency |
|
1636.0 |
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 |
| Glucagon-like peptide 1 receptor |
Potency |
|
14125.4 |
nM |
PubChem BioAssay. qHTS of GLP-1 Receptor Agonists. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A3 receptor |
Ki |
= |
4.1 |
nM |
Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter |
CHEMBL2177029 |
| Adenosine A2a receptor |
Ki |
= |
56.0 |
nM |
Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter |
CHEMBL2177029 |
| Adenosine A1 receptor |
Ki |
= |
54.0 |
nM |
Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter |
CHEMBL2177029 |
| Adenosine receptor A2a and A3 |
Ratio Ki |
= |
51.0 |
|
Selectivity ratio of Ki for rat adenosine A2A receptor to Ki for rat adenosine A3 receptor expressed in CHO cells |
CHEMBL2177029 |
| Unchecked |
Ratio Ki |
= |
49.0 |
|
Selectivity ratio of Ki for rat adenosine A1 receptor to Ki for rat adenosine A3 receptor expressed in CHO cells |
CHEMBL2177029 |
| Adenosine A3 receptor |
Ki |
= |
1.1 |
nM |
Displacement of [125I]I-AB-MECA from human rat adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter |
CHEMBL2177029 |
| Tyrosyl-DNA phosphodiesterase 1 |
Potency |
|
29092.9 |
nM |
PubChem BioAssay. qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Tyrosyl-DNA phosphodiesterase 1 |
Potency |
|
15961.6 |
nM |
PubChem BioAssay. qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in absence of CPT. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Tyrosyl-DNA phosphodiesterase 1 |
Potency |
|
17909.3 |
nM |
PubChem BioAssay. qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in presence of CPT. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A3 receptor |
Ki |
= |
0.72 |
nM |
Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins |
CHEMBL2390918 |
| Adenosine A3 receptor |
IC50 |
= |
0.78 |
nM |
Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins |
CHEMBL2390918 |
| Adenosine A3 receptor |
Inhibition |
= |
22.0 |
% |
Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells at 10 uM after 60 mins relative to control |
CHEMBL2390918 |
| Adenosine A3 receptor |
Ki |
= |
0.08 |
nM |
Binding affinity to human adenosine A3 receptor by radioligand displacement assay |
CHEMBL2390830 |
| Adenosine A3 receptor |
IC50 |
= |
0.13 |
nM |
Binding affinity to human adenosine A3 receptor by radioligand displacement assay |
CHEMBL2390830 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
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 |
= |
10.9 |
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 |
| Unchecked |
Selectivity ratio |
= |
158.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A2A receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Unchecked |
Selectivity ratio |
= |
63.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A2B receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Adenosine receptors; A1 & A3 |
Selectivity ratio |
= |
63.0 |
|
Selectivity ratio; ratio of pEC50 for human adenosine A1 receptor to pEC50 for human adenosine A3 receptor |
CHEMBL3132785 |
| Adenosine A3 receptor |
EC50 |
= |
0.5012 |
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 |
= |
31.62 |
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 A1 receptor |
EC50 |
= |
31.62 |
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 A2a receptor |
EC50 |
= |
79.43 |
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 |
| Parathyroid hormone receptor |
Potency |
|
7943.3 |
nM |
PubChem BioAssay. qHTS of PTHR Inhibitors: Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| DNA-(apurinic or apyrimidinic site) lyase |
Potency |
|
316.2 |
nM |
PubChem BioAssay. qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A3 receptor |
Ki |
= |
1.0 |
nM |
Binding affinity to A3AR (unknown origin) |
CHEMBL3351911 |
| Mus musculus |
TIME |
= |
1.0 |
hr |
Antinociceptive activity in chronic constriction injury neutropathic pain CD-1 mouse model assessed as time for peak protection at 3 umol/kg, po |
CHEMBL3407461 |
| Mus musculus |
Emax |
= |
94.1 |
% |
Antinociceptive activity in chronic constriction injury neutropathic pain CD-1 mouse model assessed as maximum protection on ipsilateral hind paw at 3 umol/kg, po after 30 mins to 5 hrs post dose relative to control |
CHEMBL3407461 |
| Mus musculus |
Activity |
= |
38.7 |
% |
Antinociceptive activity in chronic constriction injury neutropathic pain CD-1 mouse model at 3 umol/kg, po after 3 hrs post dose relative to control |
CHEMBL3407461 |
| Serotonin 2b (5-HT2b) receptor |
Ki |
= |
1080.0 |
nM |
Binding affinity to 5HT2B receptor (unknown origin) by PDSP screening |
CHEMBL3407461 |
| Serotonin 2c (5-HT2c) receptor |
Ki |
= |
5420.0 |
nM |
Binding affinity to 5HT2C receptor (unknown origin) by PDSP screening |
CHEMBL3407461 |
| Adenosine A1 receptor |
Ki |
= |
51.0 |
nM |
Binding affinity to adenosine A1 receptor (unknown origin) |
CHEMBL3769306 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Binding affinity to adenosine A3 receptor (unknown origin) |
CHEMBL3769306 |
| Adenosine A3 receptor |
IC50 |
= |
0.6 |
nM |
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells |
CHEMBL3774372 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Binding affinity to Adenosine receptor A3 (unknown origin) |
CHEMBL3774335 |
| Adenosine A3 receptor |
Ki |
= |
1.0 |
nM |
Binding affinity to human adenosine A3 receptor |
CHEMBL3826905 |
| 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 |
Ki |
= |
1080.0 |
nM |
Displacement of [3H]lysergic from human 5-HT2BR expressed in HEK cell membranes incubated in dark for 90 mins by microbeta scintillation counting method |
CHEMBL3862033 |
| Serotonin 2b (5-HT2b) receptor |
Inhibition |
> |
50.0 |
% |
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 |
Ki |
= |
5420.0 |
nM |
Displacement of [3H]mesulergine from human 5-HT2CR expressed in Flp-In HEK cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method |
CHEMBL3862033 |
| Serotonin 2c (5-HT2c) receptor |
Inhibition |
> |
50.0 |
% |
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 |
= |
700.0 |
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 |
= |
6200.0 |
nM |
Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from recombinant human adenosine receptor A2A expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method |
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 A3 receptor |
IC50 |
= |
0.6 |
nM |
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method |
CHEMBL3875185 |
| Adenosine A3 receptor |
Activity |
= |
100.0 |
% |
Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as decrease in forskolin induced cAMP formation preincubated for 10 mins followed by forskolin challenge measured after 15 mins by AlphaScreen assay relative to adenosine-5'-N- ethyluronamide |
CHEMBL4007510 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis |
CHEMBL4007510 |
| Adenosine A2a receptor |
Ki |
= |
2910.0 |
nM |
Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation analyzer |
CHEMBL4007510 |
| Adenosine A1 receptor |
Ki |
= |
1620.0 |
nM |
Displacement of [3H]R-PLA from human adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation analyzer |
CHEMBL4007510 |
| Mus musculus |
Activity |
|
|
|
Antidiabetic activity in STZ-induced diabetic C57BL/6J mouse assessed as insulin sensitivity by measuring reduction of serum glucose levels at 20 mg/kg,po for 5 days measured at 1 and 4 hrs post last dose |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor alpha |
Inhibition |
= |
14.0 |
% |
Antagonist activity at human GST-tagged PPARalpha LBD assessed as reduction in GW501516-induced fluorescein-C33 coactivator recruitment at 1 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor alpha |
Inhibition |
|
|
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARalpha LBD at 4 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Unchecked |
Activity |
= |
117.0 |
pg/ml |
Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as adiponectin level at 4 uM measured on day 7 after 48 hrs by ELISA |
CHEMBL4017496 |
| Unchecked |
Activity |
= |
216.0 |
pg/ml |
Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as adiponectin level at 20 uM measured on day 7 after 48 hrs by ELISA |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor delta |
Activity |
|
|
|
Transactivation of human GST-tagged PPARdelta LBD assessed as fluorescein-C33 coactivator recruitment at 10 uM by TR-FRET assay |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor gamma |
Activity |
= |
29.9 |
% |
Transactivation of human PPARgamma expressed in African green monkey CV1 cells at 10 uM by luciferase reporter gene assay relative to control |
CHEMBL4017496 |
| Cyclin-dependent kinase 5/CDK5 activator 1 |
Inhibition |
|
|
% |
Inhibition of human CDK5/p35 up to 20 uM using histone H1 as substrate after 40 mins in presence of [gamma32P]ATP by scintillation counting |
CHEMBL4017496 |
| Cyclin-dependent kinase 5/CDK5 activator 1 |
Inhibition |
|
|
% |
Inhibition of human CDK5/p25 up to 20 uM using histone H1 as substrate after 40 mins in presence of [gamma32P]ATP by scintillation counting |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor delta |
Inhibition |
= |
48.3 |
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD at 20 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor gamma |
Inhibition |
= |
22.2 |
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARgamma LBD at 20 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor alpha |
Inhibition |
= |
16.0 |
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARalpha LBD at 20 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Mus musculus |
Activity |
|
|
|
Antidiabetic activity in STZ-induced diabetic C57BL/6J mouse assessed as insulin sensitivity by measuring reduction of serum lactate level at 20 mg/kg,po for 5 days |
CHEMBL4017496 |
| Mus musculus |
Activity |
|
|
|
Antidiabetic activity in STZ-induced diabetic C57BL/6J mouse assessed as insulin sensitivity by measuring reduction of serum triglyceride level at 20 mg/kg,po for 5 days |
CHEMBL4017496 |
| LXR-beta |
Activity |
|
|
|
Binding affinity to human LXRbeta at 4 uM by TR-FRET assay |
CHEMBL4017496 |
| LXR-alpha |
Activity |
|
|
|
Binding affinity to human LXRalpha at 4 uM by TR-FRET assay |
CHEMBL4017496 |
| Glucocorticoid receptor |
Inhibition |
|
|
% |
Displacement of Fluormone-GS1 from human GST-tagged glucocorticoid receptor LBD at 4 uM by TR-FRET assay |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor delta |
Inhibition |
= |
26.0 |
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD at 4 uM by TR-FRET assay relative to control |
CHEMBL4017496 |
| Adenosine A2a receptor |
Ki |
= |
2910.0 |
nM |
Displacement of [3H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by gamma counting method |
CHEMBL4017496 |
| 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 |
|
|
|
Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in the production of adiponectin measured on day 7 after 48 hrs by ELISA |
CHEMBL4017496 |
| Unchecked |
Activity |
|
|
|
Induction of adipogenesis in human bone marrow-derived mesenchymal stem cells assessed as increase in number and size of lipid droplets at 20 uM after 7 days in presence of IDX by oil red O staining based inverted microscopic method |
CHEMBL4017496 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins by gamma counting method |
CHEMBL4017496 |
| Adenosine A1 receptor |
Ki |
= |
51.2 |
nM |
Displacement of [3H]CCPA from human A1 receptor expressed in CHO cell membranes after 60 mins by gamma counting method |
CHEMBL4017496 |
| Peroxisome proliferator-activated receptor delta |
Inhibition |
|
|
% |
Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARdelta LBD by TR-FRET assay |
CHEMBL4017496 |
| Adenosine A1 receptor |
Ki |
= |
51.0 |
nM |
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method |
CHEMBL4270622 |
| Adenosine A2a receptor |
Ki |
= |
2900.0 |
nM |
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method |
CHEMBL4270622 |
| Adenosine A2b receptor |
Ki |
= |
11000.0 |
nM |
Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay |
CHEMBL4270622 |
| Adenosine A3 receptor |
Ki |
= |
1.8 |
nM |
Displacement of [3H]HEMADO from human adenosine A3 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method |
CHEMBL4270622 |
| SARS-CoV-2 |
Inhibition |
= |
8.96 |
% |
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 |
= |
0.02291 |
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 |
= |
2.138 |
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 |
= |
0.005888 |
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 |
= |
0.003311 |
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 |
= |
0.009772 |
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 |
= |
22.91 |
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 |
= |
0.02291 |
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 |
= |
0.02138 |
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 |
= |
0.04898 |
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 |
= |
0.01445 |
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 |
= |
0.05129 |
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 |
= |
0.003547999999999999 |
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 A3 receptor |
EC50 |
= |
0.2512 |
nM |
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay |
CHEMBL4371007 |
| Adenosine A3 receptor |
Emax |
= |
106.0 |
% |
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay relative to control |
CHEMBL4371007 |
| Adenosine A3 receptor |
EC50 |
= |
0.3981 |
nM |
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay |
CHEMBL4371007 |
| Adenosine A3 receptor |
Emax |
= |
72.0 |
% |
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay relative to control |
CHEMBL4371007 |
| Adenosine A3 receptor |
Ratio EC50 |
= |
1.0 |
|
Ratio of pEC50 EC50 for agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation to pEC50 for agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation |
CHEMBL4371007 |
| Adenosine A3 receptor |
EC50 |
= |
0.631 |
nM |
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay |
CHEMBL4371007 |
| Adenosine A3 receptor |
Emax |
= |
85.0 |
% |
Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay relative to control |
CHEMBL4371007 |
| Adenosine A3 receptor |
Ratio |
= |
1.0 |
|
Ratio of pEC50 for agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation to pEC50 for agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay |
CHEMBL4371007 |
| Replicase polyprotein 1ab |
Inhibition |
= |
10.63 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| Replicase polyprotein 1ab |
Inhibition |
= |
12.85 |
% |
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate |
CHEMBL4495564 |
| SARS-CoV-2 |
Inhibition |
= |
-0.01 |
% |
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 |
= |
-0.09 |
% |
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 |
| Peroxisome proliferator-activated receptor alpha |
Activity |
|
|
|
Binding affinity to GST-tagged human PPARalpha LBD up to 30 uM incubated for 2 to 6 hrs by TR-FRET assay |
CHEMBL4610002 |
| SARS-CoV-2 |
Inhibition |
= |
-0.09 |
% |
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 |
= |
-0.01 |
% |
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 |
IC50 |
> |
20000.0 |
nM |
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 |
CHEMBL4651402 |
| SARS-CoV-2 |
IC50 |
< |
19952.62 |
nM |
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 |
CHEMBL4651402 |
| Adenosine A3 receptor |
Ki |
= |
1.2 |
nM |
Binding affinity to A3 receptor (unknown origin) |
CHEMBL4665679 |
| Adenosine A3 receptor |
Ki |
= |
1.74 |
nM |
Binding affinity to human A3AR assessed as inhibitor constant |
CHEMBL4725439 |
| Adenosine A3 receptor |
Ki |
= |
0.96 |
nM |
Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay |
CHEMBL5038675 |
| Adenosine A3 receptor |
Ki |
= |
0.37 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay |
CHEMBL5038675 |
| Adenosine A3 receptor |
Ki |
= |
1800.0 |
nM |
Binding affinity to human adenosine A3 receptor measured by radioligand binding assay |
CHEMBL5038675 |
| HEK-293T |
Cell Viability |
= |
0.11 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.3 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
-0.65 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
-0.98 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.22 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
1.38 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
1.1 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
1.36 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.98 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.82 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.12 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
-0.56 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
1.11 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
1.0 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.89 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.85 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.45 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.1 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.64 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.98 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.79 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.76 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.7 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.24 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.64 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| HEK-293T |
Cell Viability |
= |
0.83 |
|
Incucyte cell viability with HEK293T |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
1.02 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| U2OS |
Cell Viability |
= |
0.81 |
|
Incucyte cell viability with U2OS |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.54 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Fibroblasts |
Cell Viability |
= |
0.42 |
|
Incucyte cell viability with human fibroblast |
CHEMBL5058564 |
| Tyrosine-protein kinase ABL |
Delta TM |
= |
-0.01 |
C |
Thermal Shift Assay. Domain: start/stop: S229-K512 |
CHEMBL4632348 |
| Serine/threonine-protein kinase Aurora-A |
Delta TM |
= |
0.15 |
C |
Thermal Shift Assay. Domain: start/stop: E122-S403 |
CHEMBL4632348 |
| Bromodomain-containing protein 4 |
Delta TM |
= |
-1.97 |
C |
Thermal Shift Assay. Domain: start/stop: N44-E168 |
CHEMBL4632348 |
| Peregrin |
Delta TM |
= |
-1.74 |
C |
Thermal Shift Assay. Domain: start/stop: M626-G740 |
CHEMBL4632348 |
| Cyclin-dependent kinase 2 |
Delta TM |
= |
0.31 |
C |
Thermal Shift Assay. Domain: start/stop: M1-L298 |
CHEMBL4632348 |
| Casein kinase I delta |
Delta TM |
= |
0.6 |
C |
Thermal Shift Assay. Domain: start/stop: M1-K294 |
CHEMBL4632348 |
| Fibroblast growth factor receptor 3 |
Delta TM |
= |
0.11 |
C |
Thermal Shift Assay. Domain: start/stop: P449-E759 |
CHEMBL4632348 |
| Glycogen synthase kinase-3 beta |
Delta TM |
= |
-0.04 |
C |
Thermal Shift Assay. Domain: start/stop: M26-R383 |
CHEMBL4632348 |
| MAP kinase ERK2 |
Delta TM |
= |
0.24 |
C |
Thermal Shift Assay. Domain: start/stop: M1-S360 |
CHEMBL4632348 |
| Transcription intermediary factor 1-alpha |
Delta TM |
= |
-1.57 |
C |
Thermal Shift Assay. Domain: start/stop: G861-E979 |
CHEMBL4632348 |
| C-X3-C chemokine receptor 1 |
%Max (Mean) |
= |
-2.74 |
% |
GPCR beta-arrestin recruitment assay with target: CX3CR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C-X3-C chemokine receptor 1 |
%Inhib (Mean) |
= |
-78.9 |
% |
GPCR beta-arrestin recruitment assay with target: CX3CR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucagon-like peptide 1 receptor |
%Max (Mean) |
= |
-2.722 |
% |
GPCR beta-arrestin recruitment assay with target: GLP1R Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucagon-like peptide 1 receptor |
%Inhib (Mean) |
= |
-56.1 |
% |
GPCR beta-arrestin recruitment assay with target: GLP1R Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Type-1 angiotensin II receptor |
%Max (Mean) |
= |
-3.71 |
% |
GPCR beta-arrestin recruitment assay with target: AGTR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Type-1 angiotensin II receptor |
%Inhib (Mean) |
= |
-14.69 |
% |
GPCR beta-arrestin recruitment assay with target: AGTR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Adhesion G-protein coupled receptor F1 |
%Max (Mean) |
= |
2.66 |
% |
GPCR beta-arrestin recruitment assay with target: ADGRF1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Adhesion G-protein coupled receptor F1 |
%Inhib (Mean) |
= |
-27.35 |
% |
GPCR beta-arrestin recruitment assay with target: ADGRF1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Sphingosine 1-phosphate receptor Edg-1 |
%Max (Mean) |
= |
12.18 |
% |
GPCR beta-arrestin recruitment assay with target: S1PR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Sphingosine 1-phosphate receptor Edg-1 |
%Inhib (Mean) |
= |
-24.5 |
% |
GPCR beta-arrestin recruitment assay with target: S1PR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C5a anaphylatoxin chemotactic receptor |
%Max (Mean) |
= |
-2.372 |
% |
GPCR beta-arrestin recruitment assay with target: C5AR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| C5a anaphylatoxin chemotactic receptor |
%Inhib (Mean) |
= |
-0.51 |
% |
GPCR beta-arrestin recruitment assay with target: C5AR1 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 120 |
%Max (Mean) |
= |
13.37 |
% |
GPCR beta-arrestin recruitment assay with target: FFAR4 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 120 |
%Inhib (Mean) |
= |
-42.36 |
% |
GPCR beta-arrestin recruitment assay with target: FFAR4 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 35 |
%Max (Mean) |
= |
-1.305 |
% |
GPCR beta-arrestin recruitment assay with target: GPR35 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| G-protein coupled receptor 35 |
%Inhib (Mean) |
= |
-4.68 |
% |
GPCR beta-arrestin recruitment assay with target: GPR35 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Alpha-2a adrenergic receptor |
%Max (Mean) |
= |
-0.91 |
% |
GPCR beta-arrestin recruitment assay with target: ADRA2A Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Alpha-2a adrenergic receptor |
%Inhib (Mean) |
= |
-28.54 |
% |
GPCR beta-arrestin recruitment assay with target: ADRA2A Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucose-dependent insulinotropic receptor |
%Max (Mean) |
= |
-1.354 |
% |
GPCR beta-arrestin recruitment assay with target: GPR119 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Glucose-dependent insulinotropic receptor |
%Inhib (Mean) |
= |
-24.21 |
% |
GPCR beta-arrestin recruitment assay with target: GPR119 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Beta-2 adrenergic receptor |
%Max (Mean) |
= |
-2.374 |
% |
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Beta-2 adrenergic receptor |
%Inhib (Mean) |
= |
-31.13 |
% |
GPCR beta-arrestin recruitment assay with target: ADRB2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Apelin receptor |
%Max (Mean) |
= |
-0.634 |
% |
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Apelin receptor |
%Inhib (Mean) |
= |
-9.58 |
% |
GPCR beta-arrestin recruitment assay with target: APLNR Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Lipoxin A4 receptor |
%Max (Mean) |
= |
-2.5340000000000003 |
% |
GPCR beta-arrestin recruitment assay with target: FPR2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
| Lipoxin A4 receptor |
%Inhib (Mean) |
= |
-15.25 |
% |
GPCR beta-arrestin recruitment assay with target: FPR2 Assay Type: PRESTO-Tango Concentration: 0.00001 |
CHEMBL5209801 |
