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Assay Detail

CHEMBL840044

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

Binding
Inhibition of [125I]- AB-MECA binding to human adenosine A3 receptor expressed in CHO cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
Perreira M, Jiang JK, Klutz AM, Gao ZG, Shainberg A, Lu C, Thomas CJ, Jacobson KA.
J Med Chem (2005) 48 : 4910 -4918
PubMed 16033270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.37 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113046 1 7.43
CHEMBL187458 1 7.38
CHEMBL363419 1 7.33
CHEMBL188592 1 7.29
CHEMBL366216 1 7.16
CHEMBL188967 1 7.16
CHEMBL2113045 1 7.13
CHEMBL446698 1 6.91
CHEMBL191270 1 6.87
CHEMBL365026 1 6.47
CHEMBL188345 1 6.38
CHEMBL188343 REVERSINE 1 6.18
CHEMBL190147 1 6.04
CHEMBL188958 1 6.02
CHEMBL191551 1 5.95
CHEMBL188496 1 5.86
CHEMBL426076 1 5.84
CHEMBL188541 1 5.82
CHEMBL362740 1 5.80
CHEMBL191522 1 5.74
CHEMBL364948 1 5.73
CHEMBL427161 1 5.62
CHEMBL187336 1 5.56
CHEMBL187794 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113046 Ki = 37.0 nM 7.43
CHEMBL187458 Ki = 42.0 nM 7.38
CHEMBL363419 Ki = 47.0 nM 7.33
CHEMBL188592 Ki = 51.0 nM 7.29
CHEMBL366216 Ki = 70.0 nM 7.16
CHEMBL188967 Ki = 70.0 nM 7.16
CHEMBL2113045 Ki = 74.0 nM 7.13
CHEMBL446698 Ki = 122.0 nM 6.91
CHEMBL191270 Ki = 134.0 nM 6.87
CHEMBL365026 Ki = 340.0 nM 6.47
CHEMBL188345 Ki = 420.0 nM 6.38
CHEMBL188343 REVERSINE Ki = 660.0 nM 6.18
CHEMBL190147 Ki = 920.0 nM 6.04
CHEMBL188958 Ki = 960.0 nM 6.02
CHEMBL191551 Ki = 1120.0 nM 5.95
CHEMBL188496 Ki = 1390.0 nM 5.86
CHEMBL426076 Ki = 1460.0 nM 5.84
CHEMBL188541 Ki = 1530.0 nM 5.82
CHEMBL362740 Ki = 1570.0 nM 5.80
CHEMBL191522 Ki = 1810.0 nM 5.74
CHEMBL364948 Ki = 1870.0 nM 5.73
CHEMBL427161 Ki = 2420.0 nM 5.62
CHEMBL187336 Ki = 2770.0 nM 5.56
CHEMBL187794 Ki = 5400.0 nM 5.27