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Assay Detail

CHEMBL643936

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

Binding
Binding affinity against cloned human adenosine A3 receptor by radioligand binding assay using [125I]-AB-MECA.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
Jiang JL, van Rhee AM, Melman N, Ji XD, Jacobson KA.
J Med Chem (1996) 39 : 4667 -4675
PubMed 8917655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 5.91 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315168 1 7.23
CHEMBL357837 1 7.14
CHEMBL139931 1 6.96
CHEMBL419306 1 6.70
CHEMBL143938 1 6.54
CHEMBL141291 1 6.48
CHEMBL341839 1 6.39
CHEMBL2112411 1 6.17
CHEMBL344284 1 6.11
CHEMBL142868 1 6.05
CHEMBL143019 1 6.04
CHEMBL142262 1 5.84
CHEMBL337552 1 5.76
CHEMBL108797 1 5.56
CHEMBL108753 1 5.55
CHEMBL405355 NIGULDIPINE 2.0 1 5.55
CHEMBL2112831 1 5.50
CHEMBL142226 1 5.49
CHEMBL140693 1 5.38
CHEMBL100071 1 5.14
CHEMBL105764 1 5.07
CHEMBL99744 1 4.87
CHEMBL103404 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315168 Ki = 58.5 nM 7.23
CHEMBL357837 Ki = 72.4 nM 7.14
CHEMBL139931 Ki = 109.0 nM 6.96
CHEMBL419306 Ki = 198.0 nM 6.70
CHEMBL143938 Ki = 286.0 nM 6.54
CHEMBL141291 Ki = 334.0 nM 6.48
CHEMBL341839 Ki = 407.0 nM 6.39
CHEMBL2112411 Ki = 670.0 nM 6.17
CHEMBL344284 Ki = 785.0 nM 6.11
CHEMBL142868 Ki = 887.0 nM 6.05
CHEMBL143019 Ki = 907.0 nM 6.04
CHEMBL142262 Ki = 1430.0 nM 5.84
CHEMBL337552 Ki = 1750.0 nM 5.76
CHEMBL108797 Ki = 2750.0 nM 5.56
CHEMBL108753 Ki = 2800.0 nM 5.55
CHEMBL405355 NIGULDIPINE Ki = 2800.0 nM 5.55
CHEMBL2112831 Ki = 3130.0 nM 5.50
CHEMBL142226 Ki = 3250.0 nM 5.49
CHEMBL140693 Ki = 4140.0 nM 5.38
CHEMBL100071 Ki = 7240.0 nM 5.14
CHEMBL105764 Ki = 8490.0 nM 5.07
CHEMBL99744 Ki = 13600.0 nM 4.87
CHEMBL103404 Ki = 32300.0 nM 4.49