| Adenosine A1 receptor |
Ki |
= |
18.0 |
nM |
Binding affinity against Human recombinant Adenosine A1 receptor stably transfected in CHO cells using [3H]CCPA as radioligand |
CHEMBL1135517 |
| Adenosine A2a receptor |
Ki |
= |
5.7 |
nM |
Binding affinity against Human recombinant Adenosine A2A receptor stably transfected in CHO cells using [3H]NECA as radioligand |
CHEMBL1135517 |
| Adenosine A3 receptor |
Ki |
= |
4.7 |
nM |
Binding affinity against Human recombinant Adenosine A3 receptor stably transfected in CHO cells using [3H]NECA as radioligand |
CHEMBL1135517 |
| Adenosine A2b receptor |
EC50 |
= |
100000.0 |
nM |
Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand |
CHEMBL1135517 |
| Adenosine receptors; A1 & A3 |
Ratio |
= |
4.0 |
|
Selectivity ratio of Ki at A1 adenosine receptor to Ki at A3 adenosine receptor |
CHEMBL1135517 |
| Adenosine receptors; A2a & A3 |
Ratio |
= |
1.0 |
|
Selectivity ratio of Ki at A2A adenosine receptor to Ki at A3 adenosine receptor |
CHEMBL1135517 |
| Adenosine A1 receptor |
Ki |
= |
98.0 |
nM |
Displacement of [3H]CHA from Adenosine A1 receptor of rat brain |
CHEMBL1129447 |
| Adenosine A2a receptor |
Ki |
= |
2.2 |
nM |
Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. |
CHEMBL1129447 |
| Adenosine receptors; A1 & A2a |
Ratio |
= |
49.0 |
|
Relative affinities for Adenosine A1 and A2A receptors |
CHEMBL1129447 |
| Adenosine A1 receptor |
EC50 |
> |
1.0 |
nM |
Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria |
CHEMBL1129447 |
| Adenosine A2a receptor |
EC50 |
= |
79.2 |
nM |
Vasorelaxation as Adenosine A2A receptor activity in rat aorta |
CHEMBL1129447 |
| Adenosine A2a receptor |
Ratio |
= |
0.58 |
|
Ratio of inhibition of ADP-induced rabbit platelet aggregation and Adenosine A2a receptor binding |
CHEMBL1129447 |
| Adenosine A1 receptor |
Ki |
= |
12.5 |
nM |
Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
633.0 |
nM |
Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
15.9 |
nM |
Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
3.6 |
nM |
Binding affinity against adenosine A2 receptor from rat striatal membranes with 50 nM CPA using [3H]-NECA |
CHEMBL1126089 |
| Adenosine A2 receptor |
Ki |
= |
8.1 |
nM |
Binding affinity against adenosine A2 receptor from human platelet membranes using [3H]NECA |
CHEMBL1126089 |
| Adenosine A1 receptor |
IC50 |
= |
2300.0 |
nM |
Inhibition of adenylate cyclase via adenosine A1 receptors in rat fat cell membranes |
CHEMBL1126089 |
| Adenosine A2 receptor |
EC50 |
= |
128.0 |
nM |
Maximal NECA stimulation of adenylate cyclase via adenosine A2 receptor in human platelet membranes |
CHEMBL1126089 |
| Adenosine A2 receptor |
Emax |
= |
65.0 |
% |
Agonistic activity at adenosine A2 receptor |
CHEMBL1126089 |
| Adenosine receptors; A1 & A2 |
A2 selectivity |
= |
3.0 |
|
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 |
= |
4.0 |
|
Selectivity as A1 adenosine receptors(high affinity) using [3H]CCPA compared to A2 adenosine receptors using [3H]-NECA in rat striatal membranes |
CHEMBL1126089 |
| Unchecked |
A2 selectivity |
= |
19.0 |
|
Selectivity as ratio of IC50 for A1 adenosine receptor compared to EC50 for A2 adenosine receptor |
CHEMBL1126089 |
| Adenosine A1 receptor |
Ki |
= |
147.0 |
nM |
Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand |
CHEMBL1125572 |
| Adenosine A2 receptor |
Ratio |
= |
4.1 |
nM |
Binding affinity against adenosine A2 receptor using [3H]- NECA as radioligand |
CHEMBL1125572 |
| Adenosine receptors; A1 & A2 |
Ratio |
= |
0.028 |
|
Ratio of A2 to A1. |
CHEMBL1125572 |
| Adenosine A1 receptor |
Ki |
= |
126.0 |
nM |
Inhibition of [3H]CHA binding to adenosine A1 receptor from rat brain membranes |
CHEMBL1126082 |
| Adenosine A2 receptor |
Ki |
= |
2.8 |
nM |
Inhibition of [3H]NECA binding to adenosine A2 receptor from rat striatal membranes |
CHEMBL1126082 |
| Rattus norvegicus |
ED30 |
= |
0.11 |
ug kg-1 |
Dose producing 30% decrease in blood pressure of anesthetized spontaneous hypertensive male rat(SHR) |
CHEMBL1126082 |
| Rattus norvegicus |
ED10 |
= |
67.0 |
ug kg-1 |
Dose producing 10% decrease in heart rate of anaesthetized spontaneous hypertensive male rat(SHR) |
CHEMBL1126082 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
45.0 |
|
Selectivity for adenosine receptor subtype, ratio of Ki(nM) at A1 receptor to Ki(nM) at A2 receptor |
CHEMBL1126082 |
| Adenosine A1 receptor |
Ki |
= |
126.0 |
nM |
Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand |
CHEMBL1126140 |
| Adenosine A2 receptor |
Ki |
= |
2.8 |
nM |
Binding affinity against adenosine A2 receptor in rat striatal membranes using [3H]NECA as radioligand |
CHEMBL1126140 |
| Rattus norvegicus |
ED30 |
= |
0.11 |
ug kg-1 |
Dose producing 30% decrease of blood pressure in anesthetized rats (SHR) |
CHEMBL1126140 |
| Rattus norvegicus |
ED10 |
= |
66.9 |
ug kg-1 |
Dose producing 10% decrease of heart rate in anesthetized rats (SHR) |
CHEMBL1126140 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
45.0 |
|
Selectivity against adenosine A1 to A2 receptors |
CHEMBL1126140 |
| Adenosine A1 receptor |
Ki |
= |
103.0 |
nM |
Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. |
CHEMBL1125505 |
| Adenosine A2 receptor |
Ki |
= |
2.4 |
nM |
Binding affinity against adenosine A2 receptor from rat striatum using [3H]NECA as radioligand. |
CHEMBL1125505 |
| Rattus norvegicus |
ED30 |
= |
0.11 |
ug kg-1 |
Dose producing 30% decrease in blood pressure of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Rattus norvegicus |
ED10 |
= |
70.4 |
ug kg-1 |
Dose producing 10% decrease in heart rate of anesthetized spontaneously hypertensive rats (SHR's) |
CHEMBL1125505 |
| Adenosine receptors; A1 & A2 |
Selectivity |
= |
43.0 |
|
Selectivity determined as Ratio of Ki(nM) of A1 adenosine receptor to the Ki(nM) of A2 adenosine receptor |
CHEMBL1125505 |
| Adenosine A1 receptor |
Displacement |
= |
63.7 |
% |
Ability to displace [3H]DPCPX from Adenosine A1 receptor in rat cortical membrane at 10e-5 M |
CHEMBL1135807 |
| Adenosine A2a receptor |
Ki |
= |
6.0 |
nM |
Binding affinity at Adenosine A2A receptor in rat striatal membrane by [3H]ZM-241385 displacement. |
CHEMBL1135807 |
| Adenosine A3 receptor |
Ki |
= |
16.9 |
nM |
Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]-AB MECA displacement. |
CHEMBL1135807 |
| Adenosine A2a receptor |
Emax |
= |
105.0 |
% |
Maximum level of G-protein activation (Emax) compared to CGS 21680 through Adenosine A2A receptor expressed in CHO cells using cAMP assay |
CHEMBL1135807 |
| Adenosine A2a receptor |
EC50 |
= |
10.0 |
nM |
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay |
CHEMBL1135807 |
| Adenosine A3 receptor |
Emax |
= |
79.0 |
% |
Percent inhibition of forskolin induced (10 uM) cAMP production compared to C1-IB-MECA through Adenosine A3 receptor expressed in CHO cells at 3 uM |
CHEMBL1135807 |
| Adenosine A2a receptor |
Ki |
= |
2.2 |
nM |
Receptor binding affinity for the adenosine A2A receptor was determined using [3H]ZM-241385 as a radioligand in rat |
CHEMBL1134910 |
| Adenosine A2b receptor |
logEC50 |
= |
-5.0 |
|
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase |
CHEMBL1145544 |
| Adenosine A2b receptor |
Activity |
= |
-1.62 |
|
Agonist activity human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase relative to NECA |
CHEMBL1145544 |
| Unchecked |
Ki |
> |
100000.0 |
nM |
Displacement of [3H]adenine from adenine 1 receptor in rat brain cortical membrane by liquid scintillation counting |
CHEMBL1156038 |
| Unchecked |
Inhibition |
= |
5.0 |
% |
Inhibition of [3H]adenine binding to adenine 1 receptor in rat brain cortical membrane at 100 uM by liquid scintillation counting |
CHEMBL1156038 |
| Adenosine A2a receptor |
Ki |
= |
5.7 |
nM |
Binding affinity to A2A adenosine receptor |
CHEMBL1949672 |
