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Assay Detail

CHEMBL646598

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

Binding
Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor.
ChEMBL ↗
51
Total Activities
51
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

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 51 6.52 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88147 — — 1 9.19
CHEMBL265096 — — 1 8.57
CHEMBL329342 — — 1 8.07
CHEMBL52735 — — 1 7.89
CHEMBL313459 — — 1 7.75
CHEMBL89472 — — 1 7.75
CHEMBL89852 — — 1 7.50
CHEMBL405982 — — 1 7.44
CHEMBL442752 — — 1 7.43
CHEMBL86588 — — 1 7.28
CHEMBL315168 — — 1 7.23
CHEMBL89264 — — 1 7.22
CHEMBL89844 — — 1 7.17
CHEMBL90282 — — 1 7.16
CHEMBL327554 — — 1 7.12
CHEMBL315458 — — 1 7.12
CHEMBL86647 — — 1 7.03
CHEMBL315984 — — 1 6.97
CHEMBL86377 — — 1 6.96
CHEMBL87053 — — 1 6.95
CHEMBL89803 — — 1 6.84
CHEMBL330696 — — 1 6.77
CHEMBL419306 — — 1 6.70
CHEMBL89362 — — 1 6.66
CHEMBL328895 — — 1 6.54
CHEMBL85410 — — 1 6.53
CHEMBL90160 — — 1 6.50
CHEMBL86829 — — 1 6.35
CHEMBL89797 — — 1 6.29
CHEMBL84583 — — 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88147 — Ki = 0.65 nM 9.19
CHEMBL265096 — Ki = 2.69 nM 8.57
CHEMBL329342 — Ki = 8.58 nM 8.07
CHEMBL52735 — Ki = 13.0 nM 7.89
CHEMBL313459 — Ki = 17.7 nM 7.75
CHEMBL89472 — Ki = 18.0 nM 7.75
CHEMBL89852 — Ki = 31.4 nM 7.50
CHEMBL405982 — Ki = 36.0 nM 7.44
CHEMBL442752 — Ki = 37.4 nM 7.43
CHEMBL86588 — Ki = 52.4 nM 7.28
CHEMBL315168 — Ki = 58.5 nM 7.23
CHEMBL89264 — Ki = 59.6 nM 7.22
CHEMBL89844 — Ki = 68.2 nM 7.17
CHEMBL90282 — Ki = 69.5 nM 7.16
CHEMBL315458 — Ki = 76.6 nM 7.12
CHEMBL327554 — Ki = 75.7 nM 7.12
CHEMBL86647 — Ki = 93.7 nM 7.03
CHEMBL315984 — Ki = 108.0 nM 6.97
CHEMBL86377 — Ki = 110.0 nM 6.96
CHEMBL87053 — Ki = 112.0 nM 6.95
CHEMBL89803 — Ki = 146.0 nM 6.84
CHEMBL330696 — Ki = 169.0 nM 6.77
CHEMBL419306 — Ki = 198.0 nM 6.70
CHEMBL89362 — Ki = 220.0 nM 6.66
CHEMBL328895 — Ki = 290.0 nM 6.54
CHEMBL85410 — Ki = 296.0 nM 6.53
CHEMBL90160 — Ki = 314.0 nM 6.50
CHEMBL86829 — Ki = 443.0 nM 6.35
CHEMBL89797 — Ki = 507.0 nM 6.29
CHEMBL84583 — Ki = 567.0 nM 6.25
CHEMBL2112340 — Ki = 940.0 nM 6.03
CHEMBL89494 — Ki = 1040.0 nM 5.98
CHEMBL315720 — Ki = 1040.0 nM 5.98
CHEMBL86968 — Ki = 1580.0 nM 5.80
CHEMBL314071 — Ki = 1710.0 nM 5.77
CHEMBL86692 — Ki = 1720.0 nM 5.76
CHEMBL89343 — Ki = 2270.0 nM 5.64
CHEMBL89358 — Ki = 2440.0 nM 5.61
CHEMBL88688 — Ki = 2580.0 nM 5.59
CHEMBL85172 — Ki = 3100.0 nM 5.51
CHEMBL312989 — Ki = 5000.0 nM 5.30
CHEMBL315897 — Ki = 5560.0 nM 5.25
CHEMBL276854 — Ki = 8310.0 nM 5.08
CHEMBL311542 — Ki = 8560.0 nM 5.07
CHEMBL85130 — Ki = 10900.0 nM 4.96
CHEMBL2063640 — Ki = 12000.0 nM 4.92
CHEMBL89874 — Ki = 12200.0 nM 4.91
CHEMBL89575 — Ki = 19200.0 nM 4.72
CHEMBL89093 — Ki = 560.0 nM -
CHEMBL89391 — Ki = 170000.0 nM -