| Adenosine A1 receptor |
Ki |
= |
1.17 |
nM |
Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. |
CHEMBL1124694 |
| Adenosine A2 receptor |
Ki |
= |
124.0 |
nM |
Inhibition of binding of [3H]NECA to adenosine A2 receptor of rat striatal membranes. |
CHEMBL1124694 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
106.0 |
|
Selectivity ratio for A1 receptor to that of A2 receptor in vitro in rat tissues |
CHEMBL1124694 |
| Adenosine A1 receptor |
Ki |
= |
1.2 |
nM |
Binding affinity to adenosine A1 receptor in rat whole brain membranes by [3H]N6-cyclohexyladenosine displacement. |
CHEMBL1123600 |
| Adenosine A2 receptor |
Ki |
= |
124.0 |
nM |
Binding affinity to A2 adenosine receptor in rat striatal membranes by [3H]NECA (1-(6-amino-9H-purin-9-yl)-1-deoxy-N-ethyl-beta-D-ribofuranuronamide) displacement. |
CHEMBL1123600 |
| Mus musculus |
ED50 |
= |
0.8 |
mg.kg-1 |
Effect on Motor activity in mouse following i.p. administration. |
CHEMBL1123600 |
| Mus musculus |
ED50 |
= |
2.0 |
mg.kg-1 |
Effect on Ataxia in mouse following i.p. administration. |
CHEMBL1123600 |
| Adenosine A1 receptor |
Ki |
= |
1.2 |
nM |
Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. |
CHEMBL1124142 |
| Adenosine A2 receptor |
Ki |
= |
124.0 |
nM |
Binding affinity at adenosine A2 receptor from rat striatal membranes by [3H]NECA displacement. |
CHEMBL1124142 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
106.0 |
|
Ratio of binding affinity against A2 and A1 receptors |
CHEMBL1124142 |
| Adenosine A1 receptor |
Ki |
= |
1.1 |
nM |
Binding affinity for adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand |
CHEMBL1123411 |
| Adenosine A2 receptor |
Ki |
= |
120.0 |
nM |
Binding affinity for adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand |
CHEMBL1123411 |
| Adenosine receptors; A1 & A2 |
Selectivity index |
= |
110.0 |
|
Ratio of binding affinities for A2 and A1 receptors |
CHEMBL1123411 |
| Mus musculus |
LAD |
= |
1.0 |
mg kg-1 |
Dose required to inhibit mouse locomotor activity by 60% |
CHEMBL1123411 |
| Mus musculus |
LAD |
= |
3.0 |
mg kg-1 |
CNS activity measured using screen test failure |
CHEMBL1123411 |
| Rattus norvegicus |
ED20 |
= |
0.006 |
mg kg-1 |
Compound was evaluated for Cardiovascular activity (as 20% decrease in rate) in rats |
CHEMBL1123411 |
| Rattus norvegicus |
ED20 |
= |
0.005 |
mg kg-1 |
Compound was evaluated for Cardiovascular activity (as 20% decrease in blood pressure) in rats |
CHEMBL1123411 |
| Adenosine A1 receptor |
Affinity constant |
= |
0.003 |
uM |
Affinity constant for inhibition of A1 receptor control of adenylate cyclase in adipocytes, heart and brain cells |
CHEMBL1122012 |
| Adenosine A2 receptor |
Affinity constant |
= |
30.0 |
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 A2a receptor |
Ki |
= |
3.3 |
nM |
Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain |
CHEMBL1122012 |
| Adenosine receptor |
Ki |
= |
1.6 |
nM |
Antagonist binding of N6-cyclohexyl-[3H]-adenosine to rat brain |
CHEMBL1122012 |
| Adenosine A1 receptor |
Ki |
= |
0.25 |
nM |
Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain |
CHEMBL1122012 |
| Adenosine receptor |
Ki |
= |
1.4 |
nM |
Antagonist binding of N6-cyclohexyl-[3H]-adenosine to rat testes |
CHEMBL1122012 |
| Adenosine receptor |
Ki |
= |
23.0 |
nM |
Antagonist binding of L-N6-phenyl-isopropyl)-[3H]adenosine to rat brain |
CHEMBL1122012 |
| Adenosine receptor |
Ki |
= |
5.0 |
nM |
Antagonist binding of L-N6-phenyl-isopropyl)-[3H]adenosine to rat fat |
CHEMBL1122012 |
| Adenosine receptor |
Ki |
= |
0.6 |
nM |
Antagonist binding of 2-chloro-[3H]-adenosine to rat brain |
CHEMBL1122012 |
| Adenosine A1 receptor |
Ki |
= |
1.2 |
nM |
Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine |
CHEMBL1124304 |
| Adenosine A2 receptor |
Ki |
= |
120.0 |
nM |
Binding affinity towards adenosine A2 receptor on rat striatal membrane using [3H]NECA as radioligand |
CHEMBL1124304 |
| Adenosine A1 receptor |
EC25 |
= |
13.0 |
nM |
Reduction of heart rate (A1 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Adenosine A2 receptor |
EC25 |
= |
10.0 |
nM |
Enhancement of coronary flow (A2 response) in isolated rat heart preparation |
CHEMBL1124304 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
100.0 |
|
Ratio of Ki at adenosine A2 and A1 receptors |
CHEMBL1124304 |
| Sodium channel alpha subunits; brain (Types I, II, III) |
Inhibition |
= |
2.2 |
% |
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM |
CHEMBL1122963 |
| ADMET |
k' |
= |
2.57 |
|
HPLC capacity factor (k') |
CHEMBL1123137 |
| Alpha-1a adrenergic receptor |
MPR |
= |
4.3 |
|
Molar potency ratio was evaluated |
CHEMBL1123137 |
| No relevant target |
pKa |
= |
3.4 |
|
Ionisation constant (pKa) |
CHEMBL1123137 |
| Adenosine A1 receptor |
Ki |
= |
2.6 |
nM |
Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain |
CHEMBL1132368 |
| Adenosine A2a receptor |
Ki |
= |
117.0 |
nM |
Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue |
CHEMBL1132368 |
| Unchecked |
IC50 |
= |
0.4 |
nM |
In vitro inhibition of isoprenaline-stimulated cAMP accumulation in DDT1-MF2 cells (measured by adenosine A1 functional assay) |
CHEMBL1132368 |
| Cavia porcellus |
EC50 |
= |
440.0 |
nM |
Negative inotropy effect in isolated guinea pig atria. |
CHEMBL1132368 |
| Mus musculus |
ED50 |
= |
0.05 |
mg.kg-1 |
In vivo inhibition of spontaneous locomotor activity of mouse by the compound 30 min after intraperitoneal administration. |
CHEMBL1132368 |
| Mus musculus |
ED50 |
= |
0.5 |
mg.kg-1 |
In vivo inhibition of DMCM-induced seizures in mouse by the compound 30 min after intraperitoneal administration |
CHEMBL1132368 |
| Gerbillinae |
Reduction |
= |
24.0 |
|
Reduction in hippocampal cell death by compound administered 30 min after a period of severe forebrain ischemia in the Mongolian gerbil at 0.3 mg/kg |
CHEMBL1132368 |
| Rattus norvegicus |
Reduction |
= |
78.0 |
% |
Percent reduction in blood pressure in an anesthetized rat 5 min after intravenous administration of 0.1 mg/kg of compound |
CHEMBL1132368 |
| Rattus norvegicus |
MBP |
= |
102.0 |
|
Mean blood pressure(MBP) at an infused iv dose of agonist administered intravenously 0 mg/kg/h |
CHEMBL1132368 |
| Rattus norvegicus |
MBP |
= |
98.0 |
|
Mean blood pressure(MBP) at an infused iv dose of agonist administered intravenously 0.005 mg/kg/h |
CHEMBL1132368 |
| Rattus norvegicus |
MBP |
= |
91.0 |
|
Mean blood pressure(MBP) at an infused iv dose of agonist administered intravenously 0.01 mg/kg/h |
CHEMBL1132368 |
| Rattus norvegicus |
MBP |
= |
80.0 |
|
Mean blood pressure(MBP) at an infused iv dose of agonist administered intravenously 0.05 mg/kg/h |
CHEMBL1132368 |
| Adenosine A1 receptor |
Ki |
= |
1.0 |
nM |
Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
200.0 |
nM |
Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
1.3 |
nM |
Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
730.0 |
nM |
Binding affinity against adenosine A2 receptor from rat striatal membranes with 50 nM CPA using [3H]-NECA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
1700.0 |
nM |
Binding affinity against adenosine A2 receptor from human platelet membranes using [3H]NECA |
CHEMBL1126089 |
| Adenosine receptors; A1 & A2 |
A2 selectivity |
= |
0.001 |
|
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 |
= |
0.002 |
|
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 |
= |
1.2 |
nM |
Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand |
CHEMBL1125572 |
| Adenosine A2 receptor |
Ratio |
= |
124.0 |
nM |
Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand |
CHEMBL1125572 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
100.0 |
|
Ratio of A2 to A1. |
CHEMBL1125572 |
| Adenosine A1 receptor |
Ki |
= |
0.6 |
nM |
Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. |
CHEMBL1131221 |
| Adenosine A2a receptor |
Ki |
= |
750.0 |
nM |
Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. |
CHEMBL1131221 |
| Adenosine A3 receptor |
Ki |
= |
53.0 |
nM |
Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
1263.0 |
|
Inhibitory selectivity at Adenosine 2A receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
88.0 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 1 receptor. |
CHEMBL1131221 |
| Unchecked |
Selectivity |
= |
0.07 |
|
Inhibitory selectivity at Adenosine A3 receptor compared to Adenosine 2A receptor. |
CHEMBL1131221 |
| Adenosine A3 receptor |
EC50 |
= |
27.0 |
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 |
= |
102.0 |
% |
Percent efficacy against human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A3 receptor |
Ki |
= |
8.7 |
nM |
Affinity for human Adenosine A3 receptor expressed in CHO cell |
CHEMBL1135592 |
| Adenosine A1 receptor |
Ki |
= |
11.0 |
nM |
Affinity for the Adenosine A1 receptor in the absence of GTP (A1-GTP) by using [3H]DPCPX as radioligand |
CHEMBL1128455 |
| Adenosine A1 receptor |
Ki |
= |
62.0 |
nM |
Affinity for the Adenosine A1 receptor in the presence of GTP (A1+GTP) by using [3H]-DPCPX as radioligand |
CHEMBL1128455 |
| Rattus norvegicus |
GTP shift |
= |
5.5 |
|
GTP shift was determined in rat |
CHEMBL1128455 |
| Adenosine A2a receptor |
Ki |
= |
140.0 |
nM |
Binding affinity against Adenosine A2A receptor by using [3H]CGS-21680 as radioligand |
CHEMBL1128455 |
| Adenosine A1 receptor |
Ki |
= |
0.6 |
nM |
Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine A2a receptor |
Displacement |
= |
750.0 |
% |
Ability to displace [3H]-CGS- 21680 from Adenosine A2A receptor of rat brain striatum at 10e-5 M |
CHEMBL1135881 |
| Adenosine A3 receptor |
Ki |
= |
53.0 |
nM |
Affinity to Adenosine A3 receptor of rat testis membrane using [3H](R)-PIA with 150 nM DPCPX |
CHEMBL1135881 |
| Adenosine receptors; A1 & A2a |
Selectivity |
= |
1250.0 |
|
Selectivity for Adenosine A2A over Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine receptors; A1 & A3 |
Selectivity |
= |
88.0 |
|
Selectivity for Adenosine A3 over Adenosine A1 receptor |
CHEMBL1135881 |
| Adenosine receptor A2a and A3 |
Selectivity |
= |
0.07 |
|
Selectivity towards Adenosine A3 receptor to Adenosine A2A receptor |
CHEMBL1135881 |
| Adenosine A1 receptor |
Ki |
= |
4.2 |
nM |
Intrinsic activity towards Adenosine A1 receptor as displacement of [3H]DPCPX from bovine cortical membranes without GTP |
CHEMBL1134334 |
| Adenosine A1 receptor |
Ki |
= |
19.9 |
nM |
Intrinsic activity towards Adenosine A1 receptor as displacement of [3H]DPCPX from bovine cortical membranes with 1 mM GTP |
CHEMBL1134334 |
| Adenosine A1 receptor |
Ki |
= |
1.2 |
nM |
Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor |
CHEMBL1125222 |
| Adenosine A2 receptor |
Ki |
= |
220.0 |
nM |
Inhibition of [3H]- NECA binding to adenosine receptor A2 |
CHEMBL1125222 |
| Unchecked |
IC50 |
= |
980.0 |
nM |
Effective concentration against A2AR mediated P12 adenylatencyclase activity |
CHEMBL1125222 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
180.0 |
|
Ratio of binding potencies at adenosine A2AR and AIAR receptors |
CHEMBL1125222 |
| Adenosine receptor |
IC50 |
= |
95.7 |
nM |
Displacement of [3H]CHA from rat brain adenosine receptor |
CHEMBL1122392 |
| Adenosine A1 receptor |
IC50 |
= |
5.0 |
nM |
Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor |
CHEMBL1125861 |
| Adenosine A2 receptor |
IC50 |
= |
530.0 |
nM |
Concentration required for 50% inhibition of [3H]NECA binding on rat brain adenosine A2 receptor |
CHEMBL1125861 |
| Rattus norvegicus |
ED25 |
= |
0.005 |
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 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.009000000000000001 |
|
Ratio of IC50 values for A1 receptor binding to that of A2 receptor |
CHEMBL1125861 |
| Adenosine receptor |
IC50 |
= |
3.7 |
nM |
Displacement of [3H]CHA from rat brain adenosine receptor |
CHEMBL1122392 |
| Adenosine A1 receptor |
Ki |
= |
3.0 |
nM |
Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. |
CHEMBL1124880 |
| Adenosine A2 receptor |
Ki |
= |
30000.0 |
nM |
Binding affinity for Adenosine A2 receptor in corpora striata of rats using [3H]NECA |
CHEMBL1124880 |
| Adenosine A1 receptor |
IC50 |
= |
2.4 |
nM |
Evaluated for the binding affinity towards the Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. |
CHEMBL1124880 |
| Adenosine A1 receptor |
Ki |
= |
1.17 |
nM |
Binding affinity for Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]-CHA |
CHEMBL1124880 |
| Adenosine A1 receptor |
Ki |
= |
1.15 |
nM |
Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain |
CHEMBL1122939 |
| Adenosine A2 receptor |
Ki |
= |
124.0 |
nM |
Displacement of [3H]-NECA from adenosine A2 receptor of rat striatal membrane |
CHEMBL1122939 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
108.0 |
|
Relative binding to A2 and A1 receptors (ratio of Ki) |
CHEMBL1122939 |
| Adenosine A1 receptor |
IC50 |
= |
40.0 |
nM |
Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor |
CHEMBL1124132 |
| Adenosine A1 receptor |
Inhibition |
= |
1.0 |
% |
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 |
= |
950.0 |
nM |
Stimulation of adenylate cyclase activity in human platelet membrane at A2 receptor |
CHEMBL1124132 |
| Adenosine A2 receptor |
Stimulation |
= |
0.53 |
% |
Maximal stimulation of adenylate cyclase activity relative to NECA for A2-receptor. (Stimulation by NECA=250+/-30%) |
CHEMBL1124132 |
| Adenosine A1 receptor |
Ki |
= |
1.3 |
nM |
Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes |
CHEMBL1124132 |
| Adenosine A2 receptor |
Ki |
= |
730.0 |
nM |
Displacement of [3H]NECA from A2-receptor of rat striatal membranes |
CHEMBL1124132 |
| Unchecked |
Selectivity |
= |
24.0 |
|
A1 selectivity as ratio of EC50 at A2 receptor to IC50 at A1 receptor |
CHEMBL1124132 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
560.0 |
|
A1 selectivity as ratio of Ki for A2 receptor to Ki for A1 receptor |
CHEMBL1124132 |
| ADMET |
k' |
= |
2.57 |
|
Index of hydrophobicity (k') |
CHEMBL1123294 |
| Adenosine A2 receptor |
Activity |
= |
3.09 |
M g-1 |
Binding affinity against A2 adenosine receptor |
CHEMBL1123294 |
| Adenosine A2 receptor |
K |
= |
8405.0 |
M-1 |
Association constant against A2 adenosine receptor |
CHEMBL1123294 |
| Adenosine A2 receptor |
MPR |
= |
4.3 |
|
Molar potency ratio (MPR) against A2 adenosine receptor of coronary artery |
CHEMBL1123294 |
| Adenosine A1 receptor |
Ki |
= |
0.6 |
nM |
Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes |
CHEMBL1132946 |
| Adenosine A2a receptor |
Ki |
= |
750.0 |
nM |
Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes |
CHEMBL1132946 |
| Adenosine A3 receptor |
Ki |
= |
53.0 |
nM |
Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
1250.0 |
|
Selectivity, ratio of affinity towards adenosine A2A to A1 |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
88.0 |
|
Selectivity, ratio of affinity towards adenosine A3 to A1 |
CHEMBL1132946 |
| Unchecked |
Selectivity |
= |
0.07 |
|
Selectivity, ratio of affinity towards adenosine A3 to A2A |
CHEMBL1132946 |
| ADMET |
k' |
= |
2.61 |
|
Index of hydrophobicity (k') |
CHEMBL1123294 |
| Adenosine A2 receptor |
Activity |
= |
3.13 |
M g-1 |
Binding affinity against A2 adenosine receptor |
CHEMBL1123294 |
| Adenosine A2 receptor |
K |
= |
8515.0 |
M-1 |
Association constant against A2 adenosine receptor |
CHEMBL1123294 |
| Adenosine A2b receptor |
EC50 |
= |
1680.0 |
nM |
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production |
CHEMBL1144471 |
| Adenosine A1 receptor |
Ki |
= |
2.0 |
nM |
Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A2a receptor |
Ki |
= |
884.0 |
nM |
Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A3 receptor |
Ki |
= |
8.7 |
nM |
Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells |
CHEMBL1144471 |
| Adenosine A3 receptor |
Efficacy |
= |
102.0 |
% |
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 A2b receptor |
logEC50 |
= |
-3.225 |
|
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase |
CHEMBL1145544 |
| Adenosine A2b receptor |
Activity |
= |
-1.079 |
|
Agonist activity human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase relative to NECA |
CHEMBL1145544 |
| Adenosine A1 receptor |
EC50 |
= |
1200.0 |
nM |
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells |
CHEMBL1157299 |
| Unchecked |
Inhibition |
|
|
% |
Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay |
CHEMBL1255231 |
| Ras-related protein Rab-9A |
Potency |
= |
16360.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Rab9 Promoter Activators. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Niemann-Pick C1 protein |
Potency |
= |
16360.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for NPC1 Promoter Activators. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Relaxin receptor 1 |
Potency |
= |
11220.2 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Agonists of the Relaxin Receptor RXFP1. (Class of assay: confirmatory) |
CHEMBL1201862 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
5802.4 |
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 |
|
20596.2 |
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 |
|
43620.6 |
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 |
|
5491.5 |
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 |
| Unchecked |
Potency |
|
2310.9 |
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 |
|
12990.0 |
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 |
|
316.2 |
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 |
|
5.3 |
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 |
|
92.0 |
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 |
|
21862.1 |
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 |
| ATPase family AAA domain-containing protein 5 |
Potency |
|
4466.8 |
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 |
|
5171.4 |
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 |
| Ataxin-2 |
Potency |
|
8912.5 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of ATXN expression: Validation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID588349, AID588380] |
CHEMBL1201862 |
| High-affinity choline transporter |
IC50 |
|
2455.36 |
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 |
|
8275.3 |
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 |
| GTP-binding nuclear protein Ran/Importin subunit beta-1/Snurportin-1 |
Potency |
|
6513.1 |
nM |
PUBCHEM_BIOASSAY: qHTS Assay for Inhibitors of RanGTP induced Rango (Ran-regulated importin-beta cargo) - Importin beta complex dissociation. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID540262] |
CHEMBL1201862 |
| Regulator of G-protein signaling 4 |
Potency |
|
1498.9 |
nM |
PUBCHEM_BIOASSAY: Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID504856] |
CHEMBL1201862 |
| Unchecked |
Potency |
|
6510.4 |
nM |
PUBCHEM_BIOASSAY: qHTS for inhibitors of binding or entry into cells for Marburg Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249, AID540278] |
CHEMBL1201862 |
| HEK293 |
Potency |
|
129.9 |
nM |
PUBCHEM_BIOASSAY: qHTS for Inhibitors of binding or entry into cells for Lassa Virus. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID463114, AID540249] |
CHEMBL1201862 |
| High-affinity choline transporter |
IC50 |
|
1267.28 |
nM |
PUBCHEM_BIOASSAY: Dose responses of compounds that inhibit the Choline Transporter (CHT) - 10 point CRC. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Glucagon-like peptide 1 receptor |
Potency |
|
3548.1 |
nM |
PubChem BioAssay. qHTS of GLP-1 Receptor Inverse Agonists (Inhibition Mode). (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
183.6 |
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 |
| Tyrosyl-DNA phosphodiesterase 1 |
Potency |
|
23109.3 |
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 |
| Isocitrate dehydrogenase [NADP] cytoplasmic |
Potency |
|
29092.9 |
nM |
PubChem BioAssay. qHTS for induction of synthetic lethality in tumor cells producing 2HG: qHTS for the HT-1080-NT fibrosarcoma cell line. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A1 receptor |
Ki |
= |
490.0 |
nM |
Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells after 90 mins |
CHEMBL2390918 |
| Adenosine A1 receptor |
IC50 |
= |
830.0 |
nM |
Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells after 90 mins |
CHEMBL2390918 |
| Adenosine A1 receptor |
Inhibition |
= |
25.0 |
% |
Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells at 10 uM after 90 mins relative to control |
CHEMBL2390918 |
| Ubiquitin carboxyl-terminal hydrolase 1 |
Potency |
|
15848.9 |
nM |
PubChem BioAssay. Inhibitors of USP1/UAF1: Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Parathyroid hormone receptor |
Potency |
|
125892.5 |
nM |
PubChem BioAssay. qHTS of PTHR Inhibitors: Primary Screen. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Cerebroside-sulfatase |
Potency |
|
1069.1 |
nM |
PubChem BioAssay. qHTS screen for enhancers of Arylsulfatase A (ASA1): LOPAC Validation Assay. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Unchecked |
Potency |
|
35481.3 |
nM |
PubChem BioAssay. qHTS for Inhibitors of binding or entry into cells for Marburg Virus. (Class of assay: confirmatory) |
CHEMBL1201862 |
| Adenosine A1 receptor |
Ki |
= |
2.0 |
nM |
Binding affinity to adenosine A1 receptor (unknown origin) |
CHEMBL3769306 |
| Adenosine A3 receptor |
Ki |
= |
16.0 |
nM |
Binding affinity to adenosine A3 receptor (unknown origin) |
CHEMBL3769306 |
| Adenosine A1 receptor |
log(Tau/KA) |
= |
8.96 |
|
Agonist activity at adenosine A1 receptor (unknown origin) expressed in FlpIn-CHO cells assessed as increase in cAMP accumulation |
CHEMBL4371007 |
| Adenosine A1 receptor |
log(Tau/KA) |
= |
9.5 |
|
Agonist activity at adenosine A1 receptor (unknown origin) expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation |
CHEMBL4371007 |
