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Assay Detail

CHEMBL768487

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

Binding
Displacement of [3H]PAF from PAF receptor of human platelet membranes
15
Total Activities
15
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

(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.
Cai X, Scannell RT, Yaeger D, Hussoin MS, Killian DB, Qian C, Eckman J, Hwang SB, Libertine-Garahan L, Yeh CG, Ip SH, Shen TY.
J Med Chem (1998) 41 : 1970 -1979
PubMed 9599246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.55 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113725 1 8.70
CHEMBL299944 1 8.22
CHEMBL2113720 1 8.00
CHEMBL2113727 1 7.70
CHEMBL2113723 1 7.68
CHEMBL2113722 1 7.66
CHEMBL2113721 1 7.64
CHEMBL2113733 1 7.60
CHEMBL59051 1 7.48
CHEMBL2113726 1 7.42
CHEMBL2113730 1 7.41
CHEMBL2113724 1 7.35
CHEMBL280164 APAFANT 2.0 1 7.03
CHEMBL2113731 1 6.78
CHEMBL2113732 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113725 IC50 = 2.0 nM 8.70
CHEMBL299944 IC50 = 6.0 nM 8.22
CHEMBL2113720 IC50 = 10.0 nM 8.00
CHEMBL2113727 IC50 = 20.0 nM 7.70
CHEMBL2113723 IC50 = 21.0 nM 7.68
CHEMBL2113722 IC50 = 22.0 nM 7.66
CHEMBL2113721 IC50 = 23.0 nM 7.64
CHEMBL2113733 IC50 = 25.0 nM 7.60
CHEMBL59051 IC50 = 33.0 nM 7.48
CHEMBL2113726 IC50 = 38.0 nM 7.42
CHEMBL2113730 IC50 = 39.0 nM 7.41
CHEMBL2113724 IC50 = 45.0 nM 7.35
CHEMBL280164 APAFANT IC50 = 94.0 nM 7.03
CHEMBL2113731 IC50 = 167.0 nM 6.78
CHEMBL2113732 IC50 = 285.0 nM 6.54