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Assay Detail

CHEMBL641436

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

Binding
Displacement of specific [125I]AB-MECA binding at rat Adenosine A3 receptor in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL3360)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.
Jiang J, van Rhee AM, Chang L, Patchornik A, Ji XD, Evans P, Melman N, Jacobson KA.
J Med Chem (1997) 40 : 2596 -2608
PubMed 9258367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.58 5.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL89844 1 5.95
CHEMBL89803 1 5.88
CHEMBL327554 1 5.86
CHEMBL89852 1 5.85
CHEMBL86588 1 5.82
CHEMBL86377 1 5.77
CHEMBL313459 1 5.52
CHEMBL265096 1 5.42
CHEMBL86647 1 5.40
CHEMBL329342 1 5.29
CHEMBL405982 1 5.29
CHEMBL312989 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL89844 Ki = 1120.0 nM 5.95
CHEMBL89803 Ki = 1320.0 nM 5.88
CHEMBL327554 Ki = 1380.0 nM 5.86
CHEMBL89852 Ki = 1420.0 nM 5.85
CHEMBL86588 Ki = 1520.0 nM 5.82
CHEMBL86377 Ki = 1690.0 nM 5.77
CHEMBL313459 Ki = 3000.0 nM 5.52
CHEMBL265096 Ki = 3850.0 nM 5.42
CHEMBL86647 Ki = 4020.0 nM 5.40
CHEMBL329342 Ki = 5070.0 nM 5.29
CHEMBL405982 Ki = 5070.0 nM 5.29
CHEMBL312989 Ki = 13000.0 nM 4.89