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Assay Detail

CHEMBL3223903

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

Functional
Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells preincubated for 15 mins before NECA addition measured after 5.5 to 6 hrs by beta-galactosidase reporter gene assay
ChEMBL ↗
85
Total Activities
85
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists
Shook BC, Charavarty D, Barbay JK, Wang A, Leonard K, Alford V, Powell M, Beauchamp DA, Rassnick S, Scannevin R, Carroll K, Wallace N, Crooke J, Ault M, Lampron L, Westover L, Rhodes K, Jackson PF
Medchemcomm (2011) 2 : 950 -965
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 85 7.12 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3222062 — — 1 8.28
CHEMBL3222058 — — 1 8.19
CHEMBL3222061 — — 1 8.18
CHEMBL3222066 — — 1 8.14
CHEMBL3222068 — — 1 8.06
CHEMBL3217800 — — 1 8.04
CHEMBL3222065 — — 1 8.04
CHEMBL3222085 — — 1 8.00
CHEMBL3222067 — — 1 7.99
CHEMBL3222084 — — 1 7.96
CHEMBL3222089 — — 1 7.92
CHEMBL3217866 — — 1 7.88
CHEMBL3222086 — — 1 7.80
CHEMBL3222072 — — 1 7.77
CHEMBL3222059 — — 1 7.71
CHEMBL3222087 — — 1 7.65
CHEMBL3222080 — — 1 7.65
CHEMBL3222070 — — 1 7.60
CHEMBL3222052 — — 1 7.58
CHEMBL3222054 — — 1 7.56
CHEMBL3222051 — — 1 7.55
CHEMBL3222076 — — 1 7.54
CHEMBL3222053 — — 1 7.54
CHEMBL3222055 — — 1 7.54
CHEMBL3222088 — — 1 7.52
CHEMBL3222075 — — 1 7.51
CHEMBL3222056 — — 1 7.48
CHEMBL3222081 — — 1 7.48
CHEMBL3222049 — — 1 7.44
CHEMBL3222109 — — 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3222062 — Ki = 5.3 nM 8.28
CHEMBL3222058 — Ki = 6.5 nM 8.19
CHEMBL3222061 — Ki = 6.6 nM 8.18
CHEMBL3222066 — Ki = 7.2 nM 8.14
CHEMBL3222068 — Ki = 8.7 nM 8.06
CHEMBL3217800 — Ki = 9.1 nM 8.04
CHEMBL3222065 — Ki = 9.2 nM 8.04
CHEMBL3222085 — Ki = 10.0 nM 8.00
CHEMBL3222067 — Ki = 10.3 nM 7.99
CHEMBL3222084 — Ki = 11.0 nM 7.96
CHEMBL3222089 — Ki = 12.1 nM 7.92
CHEMBL3217866 — Ki = 13.2 nM 7.88
CHEMBL3222086 — Ki = 15.9 nM 7.80
CHEMBL3222072 — Ki = 17.0 nM 7.77
CHEMBL3222059 — Ki = 19.7 nM 7.71
CHEMBL3222087 — Ki = 22.5 nM 7.65
CHEMBL3222080 — Ki = 22.2 nM 7.65
CHEMBL3222070 — Ki = 25.2 nM 7.60
CHEMBL3222052 — Ki = 26.1 nM 7.58
CHEMBL3222054 — Ki = 27.6 nM 7.56
CHEMBL3222051 — Ki = 28.1 nM 7.55
CHEMBL3222076 — Ki = 28.6 nM 7.54
CHEMBL3222053 — Ki = 28.8 nM 7.54
CHEMBL3222055 — Ki = 29.0 nM 7.54
CHEMBL3222088 — Ki = 30.0 nM 7.52
CHEMBL3222075 — Ki = 30.8 nM 7.51
CHEMBL3222081 — Ki = 33.4 nM 7.48
CHEMBL3222056 — Ki = 32.8 nM 7.48
CHEMBL3222049 — Ki = 36.0 nM 7.44
CHEMBL3222109 — Ki = 36.1 nM 7.44
CHEMBL3222083 — Ki = 36.7 nM 7.43
CHEMBL3217864 — Ki = 39.0 nM 7.41
CHEMBL3222077 — Ki = 42.2 nM 7.38
CHEMBL3222079 — Ki = 43.2 nM 7.37
CHEMBL3222082 — Ki = 45.4 nM 7.34
CHEMBL3222060 — Ki = 49.6 nM 7.30
CHEMBL3217865 — Ki = 50.9 nM 7.29
CHEMBL3217863 — Ki = 54.4 nM 7.26
CHEMBL3222048 — Ki = 55.5 nM 7.26
CHEMBL3222110 — Ki = 64.6 nM 7.19
CHEMBL3217872 — Ki = 79.2 nM 7.10
CHEMBL3222069 — Ki = 78.9 nM 7.10
CHEMBL3222108 — Ki = 83.5 nM 7.08
CHEMBL3222095 — Ki = 89.1 nM 7.05
CHEMBL3217882 — Ki = 97.7 nM 7.01
CHEMBL3222074 — Ki = 110.0 nM 6.96
CHEMBL3222104 — Ki = 110.0 nM 6.96
CHEMBL3222098 — Ki = 110.0 nM 6.96
CHEMBL3222105 — Ki = 120.0 nM 6.92
CHEMBL3222099 — Ki = 125.0 nM 6.90