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Assay Detail

CHEMBL760187

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

Binding
Inhibiting Platelet activating factor receptor by radioreceptor binding assay using rabbit platelets and [3H]-PAF
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists.
Sugano M, Sato A, Saito K, Takaishi S, Matsushita Y, Iijima Y.
J Med Chem (1996) 39 : 5281 -5284
PubMed 8978857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.55 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297624 1 7.62
CHEMBL148491 1 7.58
CHEMBL150892 1 7.51
CHEMBL346391 1 7.30
CHEMBL151688 1 7.10
CHEMBL348494 PHOMACTIN 1 6.92
CHEMBL148549 1 6.89
CHEMBL151310 1 6.75
CHEMBL151075 1 6.75
CHEMBL147337 1 6.47
CHEMBL149102 1 6.39
CHEMBL421954 1 6.26
CHEMBL147079 1 6.00
CHEMBL345748 1 5.89
CHEMBL150968 1 4.77
CHEMBL358635 1 4.52
CHEMBL356428 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297624 IC50 = 24.0 nM 7.62
CHEMBL148491 IC50 = 26.0 nM 7.58
CHEMBL150892 IC50 = 31.0 nM 7.51
CHEMBL346391 IC50 = 50.0 nM 7.30
CHEMBL151688 IC50 = 80.0 nM 7.10
CHEMBL348494 PHOMACTIN IC50 = 120.0 nM 6.92
CHEMBL148549 IC50 = 130.0 nM 6.89
CHEMBL151310 IC50 = 180.0 nM 6.75
CHEMBL151075 IC50 = 180.0 nM 6.75
CHEMBL147337 IC50 = 340.0 nM 6.47
CHEMBL149102 IC50 = 410.0 nM 6.39
CHEMBL421954 IC50 = 550.0 nM 6.26
CHEMBL147079 IC50 = 1000.0 nM 6.00
CHEMBL345748 IC50 = 1300.0 nM 5.89
CHEMBL150968 IC50 = 17000.0 nM 4.77
CHEMBL358635 IC50 = 30000.0 nM 4.52
CHEMBL356428 IC50 > 280000.0 nM -