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Assay Detail

CHEMBL882497

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Binding
Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 10 7.90 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118105 1 8.73
CHEMBL117413 1 8.60
CHEMBL334115 1 8.54
CHEMBL407427 1 8.52
CHEMBL116072 1 8.43
CHEMBL299944 1 8.20
CHEMBL1793831 1 8.05
CHEMBL297624 1 6.99
CHEMBL325491 1 6.96
CHEMBL112481 VERAGUENSIN 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118105 Ki = 1.85 nM 8.73
CHEMBL117413 Ki = 2.5 nM 8.60
CHEMBL334115 Ki = 2.86 nM 8.54
CHEMBL407427 Ki = 3.0 nM 8.52
CHEMBL116072 Ki = 3.72 nM 8.43
CHEMBL299944 Ki = 6.3 nM 8.20
CHEMBL1793831 Ki = 9.0 nM 8.05
CHEMBL297624 Ki = 103.0 nM 6.99
CHEMBL325491 Ki = 110.0 nM 6.96
CHEMBL112481 VERAGUENSIN Ki = 1000.0 nM 6.00