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Assay Detail

CHEMBL760448

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

Functional
Antagonist activity against platelet activating factor (PAF) receptor in rabbit platelet membranes using [3H]C18-PAF as radioligand
94
Total Activities
93
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Platelet-activating factor receptor (CHEMBL5136)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.
Sheppard GS, Pireh D, Carrera GM, Bures MG, Heyman HR, Steinman DH, Davidsen SK, Phillips JG, Guinn DE, May PD.
J Med Chem (1994) 37 : 2011 -2032
PubMed 8027984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 94 7.88 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL63100 1 9.22
CHEMBL64057 1 9.10
CHEMBL539673 1 9.00
CHEMBL64691 1 9.00
CHEMBL64214 1 9.00
CHEMBL61416 1 9.00
CHEMBL60081 1 8.96
CHEMBL64428 1 8.92
CHEMBL305372 1 8.89
CHEMBL293662 1 8.85
CHEMBL293906 1 8.85
CHEMBL64464 1 8.82
CHEMBL62497 1 8.80
CHEMBL62830 1 8.80
CHEMBL439937 1 8.80
CHEMBL291372 1 8.74
CHEMBL64636 1 8.72
CHEMBL63383 1 8.72
CHEMBL417563 1 8.70
CHEMBL293457 1 8.66
CHEMBL293259 1 8.62
CHEMBL292860 1 8.59
CHEMBL64860 1 8.52
CHEMBL60359 1 8.52
CHEMBL302696 1 8.47
CHEMBL64035 1 8.47
CHEMBL62815 1 8.47
CHEMBL64621 1 8.44
CHEMBL62942 1 8.36
CHEMBL64445 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL63100 Ki = 0.6 nM 9.22
CHEMBL64057 Ki = 0.8 nM 9.10
CHEMBL64691 Ki = 1.0 nM 9.00
CHEMBL64214 Ki = 1.0 nM 9.00
CHEMBL61416 Ki = 1.0 nM 9.00
CHEMBL539673 Ki = 1.0 nM 9.00
CHEMBL60081 Ki = 1.1 nM 8.96
CHEMBL64428 Ki = 1.2 nM 8.92
CHEMBL305372 Ki = 1.3 nM 8.89
CHEMBL293662 Ki = 1.4 nM 8.85
CHEMBL293906 Ki = 1.4 nM 8.85
CHEMBL64464 Ki = 1.5 nM 8.82
CHEMBL439937 Ki = 1.6 nM 8.80
CHEMBL62830 Ki = 1.6 nM 8.80
CHEMBL62497 Ki = 1.6 nM 8.80
CHEMBL291372 Ki = 1.8 nM 8.74
CHEMBL64636 Ki = 1.9 nM 8.72
CHEMBL63383 Ki = 1.9 nM 8.72
CHEMBL417563 Ki = 2.0 nM 8.70
CHEMBL293457 Ki = 2.2 nM 8.66
CHEMBL293259 Ki = 2.4 nM 8.62
CHEMBL292860 Ki = 2.6 nM 8.59
CHEMBL64860 Ki = 3.0 nM 8.52
CHEMBL60359 Ki = 3.0 nM 8.52
CHEMBL62815 Ki = 3.4 nM 8.47
CHEMBL64035 Ki = 3.4 nM 8.47
CHEMBL302696 Ki = 3.4 nM 8.47
CHEMBL64621 Ki = 3.6 nM 8.44
CHEMBL62942 Ki = 4.4 nM 8.36
CHEMBL64445 Ki = 4.6 nM 8.34
CHEMBL64472 Ki = 5.0 nM 8.30
CHEMBL304879 Ki = 5.4 nM 8.27
CHEMBL293862 Ki = 5.6 nM 8.25
CHEMBL62983 Ki = 5.7 nM 8.24
CHEMBL418125 Ki = 5.7 nM 8.24
CHEMBL302683 Ki = 6.2 nM 8.21
CHEMBL62219 Ki = 6.5 nM 8.19
CHEMBL29067 Ki = 7.1 nM 8.15
CHEMBL60996 Ki = 7.8 nM 8.11
CHEMBL303357 Ki = 7.7 nM 8.11
CHEMBL442170 Ki = 8.2 nM 8.09
CHEMBL62722 Ki = 8.1 nM 8.09
CHEMBL60477 Ki = 8.8 nM 8.06
CHEMBL64034 Ki = 8.8 nM 8.06
CHEMBL293642 Ki = 9.2 nM 8.04
CHEMBL64125 Ki = 9.5 nM 8.02
CHEMBL64882 Ki = 9.5 nM 8.02
CHEMBL305145 Ki = 10.0 nM 8.00
CHEMBL293641 Ki = 10.0 nM 8.00
CHEMBL62308 Ki = 12.5 nM 7.90