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Assay Detail

CHEMBL919032

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Binding
Displacement of [3H]ZM241385 from adenosine A2A receptor in rat brain membrane
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
Peng H, Kumaravel G, Yao G, Sha L, Wang J, Van Vlijmen H, Bohnert T, Huang C, Vu CB, Ensinger CL, Chang H, Engber TM, Whalley ET, Petter RC.
J Med Chem (2004) 47 : 6218 -6229
PubMed 15566292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 79 7.58 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373700 — — 1 9.70
CHEMBL373560 — — 1 9.52
CHEMBL222784 — — 1 9.52
CHEMBL222868 — — 1 9.52
CHEMBL374881 — — 1 9.22
CHEMBL223419 — — 1 9.05
CHEMBL374149 — — 1 8.70
CHEMBL222097 — — 1 8.70
CHEMBL222589 — — 1 8.70
CHEMBL221615 — — 1 8.52
CHEMBL221573 — — 1 8.52
CHEMBL173672 — — 1 8.44
CHEMBL223745 — — 1 8.40
CHEMBL221561 — — 1 8.40
CHEMBL222478 — — 1 8.40
CHEMBL2373304 — — 1 8.30
CHEMBL222590 — — 1 8.22
CHEMBL222530 — — 1 8.15
CHEMBL373941 — — 1 8.05
CHEMBL222145 — — 1 8.05
CHEMBL439141 — — 1 7.92
CHEMBL376346 — — 1 7.89
CHEMBL189192 — — 1 7.85
CHEMBL222431 — — 1 7.85
CHEMBL387328 — — 1 7.80
CHEMBL222767 — — 1 7.72
CHEMBL449710 — — 1 7.70
CHEMBL222921 — — 1 7.68
CHEMBL375128 — — 1 7.60
CHEMBL2096850 — — 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373700 — Ki = 0.2 nM 9.70
CHEMBL373560 — Ki = 0.3 nM 9.52
CHEMBL222868 — Ki = 0.3 nM 9.52
CHEMBL222784 — Ki = 0.3 nM 9.52
CHEMBL374881 — Ki = 0.6 nM 9.22
CHEMBL223419 — Ki = 0.9 nM 9.05
CHEMBL374149 — Ki = 2.0 nM 8.70
CHEMBL222097 — Ki = 2.0 nM 8.70
CHEMBL222589 — Ki = 2.0 nM 8.70
CHEMBL221615 — Ki = 3.0 nM 8.52
CHEMBL221573 — Ki = 3.0 nM 8.52
CHEMBL173672 — Ki = 3.6 nM 8.44
CHEMBL222478 — Ki = 4.0 nM 8.40
CHEMBL221561 — Ki = 4.0 nM 8.40
CHEMBL223745 — Ki = 4.0 nM 8.40
CHEMBL2373304 — Ki = 5.0 nM 8.30
CHEMBL222590 — Ki = 6.0 nM 8.22
CHEMBL222530 — Ki = 7.0 nM 8.15
CHEMBL373941 — Ki = 9.0 nM 8.05
CHEMBL222145 — Ki = 9.0 nM 8.05
CHEMBL439141 — Ki = 12.0 nM 7.92
CHEMBL376346 — Ki = 13.0 nM 7.89
CHEMBL189192 — Ki = 14.0 nM 7.85
CHEMBL222431 — Ki = 14.0 nM 7.85
CHEMBL387328 — Ki = 16.0 nM 7.80
CHEMBL222767 — Ki = 19.0 nM 7.72
CHEMBL449710 — Ki = 20.0 nM 7.70
CHEMBL222921 — Ki = 21.0 nM 7.68
CHEMBL375128 — Ki = 25.0 nM 7.60
CHEMBL2096850 — Ki = 30.0 nM 7.52
CHEMBL446621 — Ki = 30.0 nM 7.52
CHEMBL223976 — Ki = 34.0 nM 7.47
CHEMBL223252 — Ki = 35.0 nM 7.46
CHEMBL222701 — Ki = 36.0 nM 7.44
CHEMBL224971 — Ki = 36.0 nM 7.44
CHEMBL222676 — Ki = 37.0 nM 7.43
CHEMBL17127 SCH-58261 Ki = 37.0 nM 7.43
CHEMBL375846 — Ki = 38.0 nM 7.42
CHEMBL387318 — Ki = 41.0 nM 7.39
CHEMBL376712 — Ki = 45.0 nM 7.35
CHEMBL221359 — Ki = 45.0 nM 7.35
CHEMBL375436 — Ki = 45.0 nM 7.35
CHEMBL221352 — Ki = 46.0 nM 7.34
CHEMBL221613 — Ki = 47.0 nM 7.33
CHEMBL222481 — Ki = 47.0 nM 7.33
CHEMBL225462 — Ki = 49.0 nM 7.31
CHEMBL390976 — Ki = 51.0 nM 7.29
CHEMBL221772 — Ki = 53.0 nM 7.28
CHEMBL222131 — Ki = 53.0 nM 7.28
CHEMBL426906 — Ki = 56.0 nM 7.25