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Assay Detail

CHEMBL767100

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

Binding
Inhibition of [3H]PAF binding to dog platelets.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Platelet-activating factor receptor (CHEMBL250)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor.
Guthrie RW, Kaplan GL, Mennona FA, Tilley JW, Kierstead RW, Mullin JG, LeMahieu RA, Zawoiski S, O'Donnell M, Crowley H.
J Med Chem (1989) 32 : 1820 -1835
PubMed 2754709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.18 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52925 1 8.40
CHEMBL415953 1 8.30
CHEMBL53527 1 8.05
CHEMBL52966 1 7.60
CHEMBL54046 1 7.52
CHEMBL299856 1 7.52
CHEMBL277245 1 7.40
CHEMBL52971 1 7.40
CHEMBL300299 1 7.40
CHEMBL52615 1 7.22
CHEMBL300463 1 7.00
CHEMBL52970 1 6.94
CHEMBL50244 1 6.70
CHEMBL280164 APAFANT 2.0 1 6.70
CHEMBL54068 1 6.60
CHEMBL431923 1 6.52
CHEMBL54163 1 6.52
CHEMBL52924 1 6.40
CHEMBL52526 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52925 IC50 = 4.0 nM 8.40
CHEMBL415953 IC50 = 5.0 nM 8.30
CHEMBL53527 IC50 = 9.0 nM 8.05
CHEMBL52966 IC50 = 25.0 nM 7.60
CHEMBL54046 IC50 = 30.0 nM 7.52
CHEMBL299856 IC50 = 30.0 nM 7.52
CHEMBL277245 IC50 = 40.0 nM 7.40
CHEMBL52971 IC50 = 40.0 nM 7.40
CHEMBL300299 IC50 = 40.0 nM 7.40
CHEMBL52615 IC50 = 60.0 nM 7.22
CHEMBL300463 IC50 = 100.0 nM 7.00
CHEMBL52970 IC50 = 115.0 nM 6.94
CHEMBL50244 IC50 = 200.0 nM 6.70
CHEMBL280164 APAFANT IC50 = 200.0 nM 6.70
CHEMBL54068 IC50 = 250.0 nM 6.60
CHEMBL431923 IC50 = 300.0 nM 6.52
CHEMBL54163 IC50 = 300.0 nM 6.52
CHEMBL52924 IC50 = 400.0 nM 6.40
CHEMBL52526 IC50 = 700.0 nM 6.16