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Assay Detail

CHEMBL760449

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

Binding
Inhibition of [3H]PAF binding to rabbit platelet membrane
15
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines.
Lamouri A, Heymans F, Tavet F, Dive G, Batt JP, Blavet N, Braquet P, Godfroid JJ.
J Med Chem (1993) 36 : 990 -1000
PubMed 8478911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.60 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6203 3 7.30
CHEMBL258053 1 7.16
CHEMBL6270 3 7.05
CHEMBL269132 1 6.75
CHEMBL514432 GINKOLIDE B 1 6.75
CHEMBL268596 3 6.52
CHEMBL6217 1 6.40
CHEMBL269131 1 6.17
CHEMBL269340 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6203 EC50 = 50.0 nM 7.30
CHEMBL258053 EC50 = 70.0 nM 7.16
CHEMBL6270 EC50 = 90.0 nM 7.05
CHEMBL269132 EC50 = 180.0 nM 6.75
CHEMBL514432 GINKOLIDE B EC50 = 180.0 nM 6.75
CHEMBL6270 EC50 = 220.0 nM 6.66
CHEMBL6270 EC50 = 250.0 nM 6.60
CHEMBL268596 EC50 = 300.0 nM 6.52
CHEMBL268596 EC50 = 300.0 nM 6.52
CHEMBL6217 EC50 = 400.0 nM 6.40
CHEMBL268596 EC50 = 420.0 nM 6.38
CHEMBL6203 EC50 = 450.0 nM 6.35
CHEMBL6203 EC50 = 610.0 nM 6.21
CHEMBL269131 EC50 = 680.0 nM 6.17
CHEMBL269340 EC50 = 700.0 nM 6.16