Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL933567

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity at human adenosine A2A receptor
39
Total Activities
39
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 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Giles PR, Jordan AM, Knight AR, Lawrence A, Lerpiniere J, Misra A, Pratt RM, Todd RS, Upton R, Weiss SM, Williamson DS.
Bioorg Med Chem Lett (2008) 18 : 2920 -2923
PubMed 18407496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 39 7.46 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406315 1 8.89
CHEMBL407307 1 8.85
CHEMBL407650 1 8.80
CHEMBL259323 1 8.68
CHEMBL402464 1 8.64
CHEMBL260718 1 8.55
CHEMBL406049 1 8.51
CHEMBL260719 1 8.48
CHEMBL406048 1 8.44
CHEMBL407064 1 8.24
CHEMBL259442 1 8.18
CHEMBL408624 1 7.92
CHEMBL259337 1 7.89
CHEMBL406314 1 7.85
CHEMBL406298 1 7.85
CHEMBL407638 1 7.75
CHEMBL259952 1 7.72
CHEMBL260773 1 7.70
CHEMBL259953 1 7.58
CHEMBL265695 1 7.52
CHEMBL259111 1 7.46
CHEMBL259445 1 7.40
CHEMBL265696 1 7.26
CHEMBL260667 1 7.24
CHEMBL405567 1 7.22
CHEMBL402817 1 7.16
CHEMBL406483 1 7.09
CHEMBL403704 1 6.85
CHEMBL407327 1 6.81
CHEMBL405479 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406315 Ki = 1.3 nM 8.89
CHEMBL407307 Ki = 1.4 nM 8.85
CHEMBL407650 Ki = 1.6 nM 8.80
CHEMBL259323 Ki = 2.1 nM 8.68
CHEMBL402464 Ki = 2.3 nM 8.64
CHEMBL260718 Ki = 2.8 nM 8.55
CHEMBL406049 Ki = 3.1 nM 8.51
CHEMBL260719 Ki = 3.3 nM 8.48
CHEMBL406048 Ki = 3.6 nM 8.44
CHEMBL407064 Ki = 5.7 nM 8.24
CHEMBL259442 Ki = 6.6 nM 8.18
CHEMBL408624 Ki = 12.0 nM 7.92
CHEMBL259337 Ki = 13.0 nM 7.89
CHEMBL406314 Ki = 14.0 nM 7.85
CHEMBL406298 Ki = 14.0 nM 7.85
CHEMBL407638 Ki = 18.0 nM 7.75
CHEMBL259952 Ki = 19.0 nM 7.72
CHEMBL260773 Ki = 20.0 nM 7.70
CHEMBL259953 Ki = 26.0 nM 7.58
CHEMBL265695 Ki = 30.0 nM 7.52
CHEMBL259111 Ki = 35.0 nM 7.46
CHEMBL259445 Ki = 40.0 nM 7.40
CHEMBL265696 Ki = 55.0 nM 7.26
CHEMBL260667 Ki = 58.0 nM 7.24
CHEMBL405567 Ki = 60.0 nM 7.22
CHEMBL402817 Ki = 69.0 nM 7.16
CHEMBL406483 Ki = 81.0 nM 7.09
CHEMBL403704 Ki = 142.0 nM 6.85
CHEMBL407327 Ki = 154.0 nM 6.81
CHEMBL405479 Ki = 172.0 nM 6.76
CHEMBL258900 Ki = 203.0 nM 6.69
CHEMBL408146 Ki = 299.0 nM 6.52
CHEMBL253753 Ki = 391.0 nM 6.41
CHEMBL265937 Ki = 444.0 nM 6.35
CHEMBL259338 Ki = 681.0 nM 6.17
CHEMBL258901 Ki = 748.0 nM 6.13
CHEMBL407652 Ki = 779.0 nM 6.11
CHEMBL261754 Ki = 1326.0 nM 5.88
CHEMBL406745 Ki = 3079.0 nM 5.51