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Assay Detail

CHEMBL760186

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

Binding
Displacement of [3H]-WEB 2086 from Platelet activating factor receptor (guinea pig) transgenic mouse muscle membrane
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Platelet-activating factor receptor (CHEMBL5136)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Vogensen SB, Strømgaard K, Shindou H, Jaracz S, Suehiro M, Ishii S, Shimizu T, Nakanishi K.
J Med Chem (2003) 46 : 601 -608
PubMed 12570381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.95 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435037 1 7.00
CHEMBL422003 1 6.96
CHEMBL345420 1 6.92
CHEMBL154481 1 6.26
CHEMBL347597 1 6.22
CHEMBL345909 1 6.21
CHEMBL514432 GINKOLIDE B 1 6.06
CHEMBL156402 1 6.00
CHEMBL433516 1 5.79
CHEMBL158006 1 5.78
CHEMBL348623 1 5.62
CHEMBL3349895 1 5.37
CHEMBL347433 1 5.11
CHEMBL346787 1 5.06
CHEMBL1868593 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435037 Ki = 100.0 nM 7.00
CHEMBL422003 Ki = 110.0 nM 6.96
CHEMBL345420 Ki = 120.0 nM 6.92
CHEMBL154481 Ki = 550.0 nM 6.26
CHEMBL347597 Ki = 600.0 nM 6.22
CHEMBL345909 Ki = 610.0 nM 6.21
CHEMBL514432 GINKOLIDE B Ki = 880.0 nM 6.06
CHEMBL156402 Ki = 990.0 nM 6.00
CHEMBL433516 Ki = 1620.0 nM 5.79
CHEMBL158006 Ki = 1670.0 nM 5.78
CHEMBL348623 Ki = 2400.0 nM 5.62
CHEMBL3349895 Ki = 4260.0 nM 5.37
CHEMBL347433 Ki = 7840.0 nM 5.11
CHEMBL346787 Ki = 8640.0 nM 5.06
CHEMBL1868593 Ki = 12600.0 nM 4.90