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Assay Detail

CHEMBL618339

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

Functional
Antagonist activity against human A2B adenosine receptor expressed in HEK293 cells uisng [3H]ZM-241385 or [125I]-IABOPX
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
Kim YC, Ji X, Melman N, Linden J, Jacobson KA.
J Med Chem (2000) 43 : 1165 -1172
PubMed 10737749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 8.02 8.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17002 1 8.86
CHEMBL16677 1 8.83
CHEMBL16787 1 8.82
CHEMBL16866 1 8.75
CHEMBL432664 1 8.73
CHEMBL273807 1 8.71
CHEMBL275605 1 8.69
CHEMBL278039 1 8.67
CHEMBL277386 1 8.67
CHEMBL16929 1 8.65
CHEMBL17003 1 8.63
CHEMBL275427 1 8.61
CHEMBL17341 1 8.56
CHEMBL17167 1 8.48
CHEMBL17202 1 8.44
CHEMBL444281 1 8.43
CHEMBL16741 1 8.41
CHEMBL16534 1 8.31
CHEMBL275606 1 8.27
CHEMBL275360 1 8.11
CHEMBL273094 XANTHINE AMINE CONGENER 1 8.11
CHEMBL275149 1 8.01
CHEMBL27081 1 8.01
CHEMBL17141 1 7.82
CHEMBL16931 1 7.79
CHEMBL27043 1 7.79
CHEMBL17294 1 7.78
CHEMBL17173 1 7.58
CHEMBL17299 1 7.47
CHEMBL27041 1 7.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17002 Ki = 1.39 nM 8.86
CHEMBL16677 Ki = 1.48 nM 8.83
CHEMBL16787 Ki = 1.52 nM 8.82
CHEMBL16866 Ki = 1.78 nM 8.75
CHEMBL432664 Ki = 1.88 nM 8.73
CHEMBL273807 Ki = 1.97 nM 8.71
CHEMBL275605 Ki = 2.04 nM 8.69
CHEMBL278039 Ki = 2.13 nM 8.67
CHEMBL277386 Ki = 2.14 nM 8.67
CHEMBL16929 Ki = 2.22 nM 8.65
CHEMBL17003 Ki = 2.35 nM 8.63
CHEMBL275427 Ki = 2.47 nM 8.61
CHEMBL17341 Ki = 2.74 nM 8.56
CHEMBL17167 Ki = 3.34 nM 8.48
CHEMBL17202 Ki = 3.65 nM 8.44
CHEMBL444281 Ki = 3.71 nM 8.43
CHEMBL16741 Ki = 3.93 nM 8.41
CHEMBL16534 Ki = 4.92 nM 8.31
CHEMBL275606 Ki = 5.42 nM 8.27
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 7.75 nM 8.11
CHEMBL275360 Ki = 7.75 nM 8.11
CHEMBL275149 Ki = 9.88 nM 8.01
CHEMBL27081 Ki = 9.75 nM 8.01
CHEMBL17141 Ki = 15.2 nM 7.82
CHEMBL16931 Ki = 16.1 nM 7.79
CHEMBL27043 Ki = 16.3 nM 7.79
CHEMBL17294 Ki = 16.7 nM 7.78
CHEMBL17173 Ki = 26.6 nM 7.58
CHEMBL17299 Ki = 33.7 nM 7.47
CHEMBL27041 Ki = 40.0 nM 7.40
CHEMBL16984 Ki = 43.4 nM 7.36
CHEMBL17123 Ki = 48.0 nM 7.32
CHEMBL16997 Ki = 60.0 nM 7.22
CHEMBL16724 Ki = 141.0 nM 6.85
CHEMBL17103 Ki = 199.0 nM 6.70
CHEMBL16908 Ki = 469.0 nM 6.33
CHEMBL417812 Ki = 1760.0 nM 5.75