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Assay Detail

CHEMBL642199

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

Binding
Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
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 29 4.86 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88147 1 6.52
CHEMBL90160 1 5.44
CHEMBL311542 1 5.35
CHEMBL2112340 1 5.27
CHEMBL315984 1 5.23
CHEMBL328932 1 5.09
CHEMBL314071 1 5.09
CHEMBL315720 1 5.07
CHEMBL86692 1 5.07
CHEMBL315458 1 4.96
CHEMBL2063640 1 4.96
CHEMBL89343 1 4.90
CHEMBL86829 1 4.90
CHEMBL276854 1 4.83
CHEMBL89797 1 4.81
CHEMBL315897 1 4.79
CHEMBL89874 1 4.76
CHEMBL89264 1 4.73
CHEMBL85130 1 4.73
CHEMBL90733 1 4.72
CHEMBL89494 1 4.64
CHEMBL86968 1 4.63
CHEMBL89575 1 4.58
CHEMBL328895 1 4.50
CHEMBL88688 1 4.46
CHEMBL89852 1 4.40
CHEMBL84583 1 4.28
CHEMBL89358 1 4.18
CHEMBL89093 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88147 Ki = 305.0 nM 6.52
CHEMBL90160 Ki = 3650.0 nM 5.44
CHEMBL311542 Ki = 4480.0 nM 5.35
CHEMBL2112340 Ki = 5390.0 nM 5.27
CHEMBL315984 Ki = 5930.0 nM 5.23
CHEMBL328932 Ki = 8200.0 nM 5.09
CHEMBL314071 Ki = 8030.0 nM 5.09
CHEMBL315720 Ki = 8590.0 nM 5.07
CHEMBL86692 Ki = 8580.0 nM 5.07
CHEMBL315458 Ki = 11000.0 nM 4.96
CHEMBL2063640 Ki = 11000.0 nM 4.96
CHEMBL89343 Ki = 12600.0 nM 4.90
CHEMBL86829 Ki = 12500.0 nM 4.90
CHEMBL276854 Ki = 14900.0 nM 4.83
CHEMBL89797 Ki = 15400.0 nM 4.81
CHEMBL315897 Ki = 16200.0 nM 4.79
CHEMBL89874 Ki = 17400.0 nM 4.76
CHEMBL89264 Ki = 18800.0 nM 4.73
CHEMBL85130 Ki = 18500.0 nM 4.73
CHEMBL90733 Ki = 19100.0 nM 4.72
CHEMBL89494 Ki = 23100.0 nM 4.64
CHEMBL86968 Ki = 23600.0 nM 4.63
CHEMBL89575 Ki = 26600.0 nM 4.58
CHEMBL328895 Ki = 31500.0 nM 4.50
CHEMBL88688 Ki = 34500.0 nM 4.46
CHEMBL89852 Ki = 40100.0 nM 4.40
CHEMBL84583 Ki = 53000.0 nM 4.28
CHEMBL89358 Ki = 65600.0 nM 4.18
CHEMBL89093 Ki = 100000.0 nM 4.00