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Assay Detail

CHEMBL764537

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

Binding
Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Platelet-activating factor receptor (CHEMBL250)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A partial pharmacophore for the platelet activating factor (PAF) receptor
Hodgkin EE, Miller A, Whittaker M
Bioorg Med Chem Lett (1992) 2 : 597 -602
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.85 10.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157078 1 10.82
CHEMBL156461 1 8.64
CHEMBL349811 TULOPAFANT 2.0 1 7.96
CHEMBL29067 1 7.89
CHEMBL277245 1 7.40
CHEMBL280164 APAFANT 2.0 1 7.30
CHEMBL418608 1 6.52
CHEMBL345902 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157078 IC50 = 0.015 nM 10.82
CHEMBL156461 IC50 = 2.3 nM 8.64
CHEMBL349811 TULOPAFANT IC50 = 11.0 nM 7.96
CHEMBL29067 IC50 = 13.0 nM 7.89
CHEMBL277245 IC50 = 40.0 nM 7.40
CHEMBL280164 APAFANT IC50 = 50.0 nM 7.30
CHEMBL418608 IC50 = 300.0 nM 6.52
CHEMBL345902 IC50 = 500.0 nM 6.30