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Assay Detail

CHEMBL768980

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

Functional
Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.
22
Total Activities
22
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

Novel antagonists of platelet-activating factor. 1. Synthesis and structure-activity relationships of benzodiazepine and benzazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.
Fray MJ, Cooper K, Parry MJ, Richardson K, Steele J.
J Med Chem (1995) 38 : 3514 -3523
PubMed 7658438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.74 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334275 1 9.30
CHEMBL324709 1 9.30
CHEMBL119412 1 9.30
CHEMBL434028 1 9.22
CHEMBL331566 1 9.15
CHEMBL115529 1 9.05
CHEMBL119366 1 8.72
CHEMBL116198 1 8.40
CHEMBL29067 1 8.37
CHEMBL119847 1 8.31
CHEMBL333674 1 8.30
CHEMBL116515 1 7.82
CHEMBL118017 1 7.36
CHEMBL119470 1 7.17
CHEMBL325439 BEPAFANT 2.0 1 7.14
CHEMBL273392 1 6.72
CHEMBL326077 1 6.70
CHEMBL115695 1 6.46
CHEMBL333242 1 6.22
CHEMBL323940 1 6.08
CHEMBL326517 1 5.58
CHEMBL117250 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334275 IC50 = 0.5 nM 9.30
CHEMBL324709 IC50 = 0.5 nM 9.30
CHEMBL119412 IC50 = 0.5 nM 9.30
CHEMBL434028 IC50 = 0.6 nM 9.22
CHEMBL331566 IC50 = 0.7 nM 9.15
CHEMBL115529 IC50 = 0.9 nM 9.05
CHEMBL119366 IC50 = 1.9 nM 8.72
CHEMBL116198 IC50 = 4.0 nM 8.40
CHEMBL29067 IC50 = 4.3 nM 8.37
CHEMBL119847 IC50 = 4.9 nM 8.31
CHEMBL333674 IC50 = 5.0 nM 8.30
CHEMBL116515 IC50 = 15.0 nM 7.82
CHEMBL118017 IC50 = 44.0 nM 7.36
CHEMBL119470 IC50 = 67.0 nM 7.17
CHEMBL325439 BEPAFANT IC50 = 73.0 nM 7.14
CHEMBL273392 IC50 = 190.0 nM 6.72
CHEMBL326077 IC50 = 200.0 nM 6.70
CHEMBL115695 IC50 = 350.0 nM 6.46
CHEMBL333242 IC50 = 600.0 nM 6.22
CHEMBL323940 IC50 = 840.0 nM 6.08
CHEMBL326517 IC50 = 2600.0 nM 5.58
CHEMBL117250 IC50 = 2800.0 nM 5.55