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Assay Detail

CHEMBL768978

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

Functional
In vitro inhibition of PAF-induced aggregation of rabbit washed platelets.
37
Total Activities
37
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

1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.
Cooper K, Fray MJ, Parry MJ, Richardson K, Steele J.
J Med Chem (1992) 35 : 3115 -3129
PubMed 1507200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.82 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106908 1 9.30
CHEMBL318172 1 8.89
CHEMBL106350 1 8.80
CHEMBL106475 1 8.74
CHEMBL263022 1 8.68
CHEMBL323382 1 8.64
CHEMBL106819 1 8.60
CHEMBL326039 1 8.51
CHEMBL106526 1 8.49
CHEMBL318348 1 8.49
CHEMBL323067 1 8.47
CHEMBL29067 1 8.37
CHEMBL320900 1 8.30
CHEMBL323407 1 8.25
CHEMBL322772 1 8.23
CHEMBL323429 1 8.00
CHEMBL107113 1 7.92
CHEMBL107951 1 7.89
CHEMBL106800 1 7.89
CHEMBL326201 1 7.85
CHEMBL108260 1 7.85
CHEMBL323290 1 7.82
CHEMBL107321 1 7.66
CHEMBL107159 1 7.64
CHEMBL321722 1 7.60
CHEMBL326012 1 7.55
CHEMBL323023 1 7.52
CHEMBL107241 1 7.48
CHEMBL280164 APAFANT 2.0 1 6.84
CHEMBL320226 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106908 IC50 = 0.5 nM 9.30
CHEMBL318172 IC50 = 1.3 nM 8.89
CHEMBL106350 IC50 = 1.6 nM 8.80
CHEMBL106475 IC50 = 1.8 nM 8.74
CHEMBL263022 IC50 = 2.1 nM 8.68
CHEMBL323382 IC50 = 2.3 nM 8.64
CHEMBL106819 IC50 = 2.5 nM 8.60
CHEMBL326039 IC50 = 3.1 nM 8.51
CHEMBL106526 IC50 = 3.2 nM 8.49
CHEMBL318348 IC50 = 3.2 nM 8.49
CHEMBL323067 IC50 = 3.4 nM 8.47
CHEMBL29067 IC50 = 4.3 nM 8.37
CHEMBL320900 IC50 = 5.0 nM 8.30
CHEMBL323407 IC50 = 5.6 nM 8.25
CHEMBL322772 IC50 = 5.9 nM 8.23
CHEMBL323429 IC50 = 10.0 nM 8.00
CHEMBL107113 IC50 = 12.0 nM 7.92
CHEMBL106800 IC50 = 13.0 nM 7.89
CHEMBL107951 IC50 = 13.0 nM 7.89
CHEMBL326201 IC50 = 14.0 nM 7.85
CHEMBL108260 IC50 = 14.0 nM 7.85
CHEMBL323290 IC50 = 15.0 nM 7.82
CHEMBL107321 IC50 = 22.0 nM 7.66
CHEMBL107159 IC50 = 23.0 nM 7.64
CHEMBL321722 IC50 = 25.0 nM 7.60
CHEMBL326012 IC50 = 28.0 nM 7.55
CHEMBL323023 IC50 = 30.0 nM 7.52
CHEMBL107241 IC50 = 33.0 nM 7.48
CHEMBL280164 APAFANT IC50 = 146.0 nM 6.84
CHEMBL320226 IC50 = 190.0 nM 6.72
CHEMBL105500 IC50 = 200.0 nM 6.70
CHEMBL326474 IC50 = 270.0 nM 6.57
CHEMBL106564 IC50 = 580.0 nM 6.24
CHEMBL107198 IC50 = 1400.0 nM 5.85
CHEMBL323151 IC50 = 3000.0 nM 5.52
CHEMBL431069 IC50 > 10000.0 nM -
CHEMBL320855 IC50 > 10000.0 nM -