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Assay Detail

CHEMBL699501

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

Functional
Inhibitory activity against PAF-induced aggregation of human platelets suspended in buffer [washed platelets (WP)]
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Intermediate

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
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
IC50 6 8.55 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118105 1 9.10
CHEMBL407427 1 9.05
CHEMBL116072 1 9.05
CHEMBL117413 1 9.00
CHEMBL299944 1 8.82
CHEMBL325491 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118105 IC50 = 0.8 nM 9.10
CHEMBL407427 IC50 = 0.9 nM 9.05
CHEMBL116072 IC50 = 0.9 nM 9.05
CHEMBL117413 IC50 = 1.0 nM 9.00
CHEMBL299944 IC50 = 1.5 nM 8.82
CHEMBL325491 IC50 = 515.0 nM 6.29