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Assay Detail

CHEMBL829118

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

Binding
Percent inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells at 10 uM
9
Total Activities
9
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 A1 (CHEMBL226)
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 9 5.38 5.83

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113045 1 5.83
CHEMBL187458 1 5.76
CHEMBL188967 1 5.73
CHEMBL188958 1 5.71
CHEMBL191270 1 5.52
CHEMBL366216 1 5.41
CHEMBL363419 1 4.58
CHEMBL446698 1 4.47
CHEMBL188343 REVERSINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113045 Ki = 1470.0 nM 5.83
CHEMBL187458 Ki = 1720.0 nM 5.76
CHEMBL188967 Ki = 1880.0 nM 5.73
CHEMBL188958 Ki = 1940.0 nM 5.71
CHEMBL191270 Ki = 3000.0 nM 5.52
CHEMBL366216 Ki = 3900.0 nM 5.41
CHEMBL363419 Ki = 26000.0 nM 4.58
CHEMBL446698 Ki = 34000.0 nM 4.47
CHEMBL188343 REVERSINE Ki > 10000.0 nM -