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Assay Detail

CHEMBL921473

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Binding
Binding affinity at human adenosine A2A receptor
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Jordan AM, Knight AR, Lerpiniere J, Misra A, Pratt RM, Roffey J, Stratton GC, Upton R, Weiss SM, Williamson DS.
Bioorg Med Chem Lett (2008) 18 : 2924 -2929
PubMed 18411049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 7.73 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261203 1 9.00
CHEMBL409915 1 9.00
CHEMBL429144 1 9.00
CHEMBL259049 1 9.00
CHEMBL411034 1 9.00
CHEMBL260146 1 9.00
CHEMBL257757 1 9.00
CHEMBL264432 1 9.00
CHEMBL259832 1 8.70
CHEMBL409682 1 8.70
CHEMBL401973 1 8.70
CHEMBL402409 1 8.70
CHEMBL402172 1 8.52
CHEMBL259418 1 8.52
CHEMBL371615 1 8.52
CHEMBL403252 1 8.40
CHEMBL256361 1 8.40
CHEMBL256360 1 8.40
CHEMBL258181 1 8.40
CHEMBL407049 1 8.40
CHEMBL260209 1 8.30
CHEMBL260989 1 8.22
CHEMBL424827 1 8.22
CHEMBL261534 1 8.22
CHEMBL256344 1 8.22
CHEMBL371436 1 8.15
CHEMBL410033 1 8.10
CHEMBL261349 1 8.10
CHEMBL403470 1 8.10
CHEMBL257756 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261203 Ki = 1.0 nM 9.00
CHEMBL264432 Ki = 1.0 nM 9.00
CHEMBL257757 Ki = 1.0 nM 9.00
CHEMBL260146 Ki = 1.0 nM 9.00
CHEMBL411034 Ki = 1.0 nM 9.00
CHEMBL429144 Ki = 1.0 nM 9.00
CHEMBL409915 Ki = 1.0 nM 9.00
CHEMBL259049 Ki = 1.0 nM 9.00
CHEMBL402409 Ki = 2.0 nM 8.70
CHEMBL259832 Ki = 2.0 nM 8.70
CHEMBL401973 Ki = 2.0 nM 8.70
CHEMBL409682 Ki = 2.0 nM 8.70
CHEMBL402172 Ki = 3.0 nM 8.52
CHEMBL259418 Ki = 3.0 nM 8.52
CHEMBL371615 Ki = 3.0 nM 8.52
CHEMBL403252 Ki = 4.0 nM 8.40
CHEMBL256361 Ki = 4.0 nM 8.40
CHEMBL256360 Ki = 4.0 nM 8.40
CHEMBL258181 Ki = 4.0 nM 8.40
CHEMBL407049 Ki = 4.0 nM 8.40
CHEMBL260209 Ki = 5.0 nM 8.30
CHEMBL260989 Ki = 6.0 nM 8.22
CHEMBL424827 Ki = 6.0 nM 8.22
CHEMBL261534 Ki = 6.0 nM 8.22
CHEMBL256344 Ki = 6.0 nM 8.22
CHEMBL371436 Ki = 7.0 nM 8.15
CHEMBL261349 Ki = 8.0 nM 8.10
CHEMBL403470 Ki = 8.0 nM 8.10
CHEMBL410033 Ki = 8.0 nM 8.10
CHEMBL257756 Ki = 9.0 nM 8.05
CHEMBL258006 Ki = 9.0 nM 8.05
CHEMBL257982 Ki = 12.0 nM 7.92
CHEMBL264431 Ki = 13.0 nM 7.89
CHEMBL411473 Ki = 13.0 nM 7.89
CHEMBL406298 Ki = 14.0 nM 7.85
CHEMBL267200 Ki = 16.0 nM 7.80
CHEMBL410678 Ki = 16.0 nM 7.80
CHEMBL259164 Ki = 17.0 nM 7.77
CHEMBL402389 Ki = 17.0 nM 7.77
CHEMBL260788 Ki = 23.0 nM 7.64
CHEMBL409152 Ki = 23.0 nM 7.64
CHEMBL410679 Ki = 26.0 nM 7.58
CHEMBL256359 Ki = 26.0 nM 7.58
CHEMBL259416 Ki = 28.0 nM 7.55
CHEMBL437804 Ki = 36.0 nM 7.44
CHEMBL196436 Ki = 40.0 nM 7.40
CHEMBL260721 Ki = 45.0 nM 7.35
CHEMBL405789 Ki = 45.0 nM 7.35
CHEMBL260557 Ki = 48.0 nM 7.32
CHEMBL258960 Ki = 56.0 nM 7.25