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Assay Detail

CHEMBL765337

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

Binding
In vitro effect on inhibition of the binding of [3H]C18-Platelet activating factor to human PMN membranes preparation
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.
Girotra NN, Biftu T, Ponpipom MM, Acton JJ, Alberts AW, Bach TN, Ball RG, Bugianesi RL, Parsons WH, Chabala JC.
J Med Chem (1992) 35 : 3474 -3482
PubMed 1404229 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.10 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118105 1 8.54
CHEMBL299944 1 8.49
CHEMBL334115 1 8.43
CHEMBL116072 1 8.28
CHEMBL325491 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118105 Ki = 2.9 nM 8.54
CHEMBL299944 Ki = 3.2 nM 8.49
CHEMBL334115 Ki = 3.7 nM 8.43
CHEMBL116072 Ki = 5.26 nM 8.28
CHEMBL325491 Ki = 174.0 nM 6.76