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Assay Detail

CHEMBL667333

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

Binding
PAF-antagonist activity determined in dog platelets by PAF-binding assay
78
Total Activities
78
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

Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.
Walser A, Flynn T, Mason C, Crowley H, Maresca C, Yaremko B, O'Donnell M.
J Med Chem (1991) 34 : 1209 -1221
PubMed 2002463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 7.65 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277701 1 9.70
CHEMBL20195 1 9.52
CHEMBL19640 1 9.22
CHEMBL19747 1 9.15
CHEMBL20019 1 9.15
CHEMBL283162 1 9.00
CHEMBL282883 1 9.00
CHEMBL281779 1 9.00
CHEMBL279665 1 8.70
CHEMBL429066 1 8.52
CHEMBL20163 1 8.52
CHEMBL280210 1 8.40
CHEMBL283339 1 8.40
CHEMBL20267 1 8.40
CHEMBL20418 1 8.40
CHEMBL20208 1 8.30
CHEMBL19947 1 8.30
CHEMBL20194 1 8.30
CHEMBL277029 1 8.30
CHEMBL20877 1 8.30
CHEMBL280683 1 8.30
CHEMBL277246 1 8.22
CHEMBL21224 1 8.22
CHEMBL435756 1 8.22
CHEMBL282905 1 8.22
CHEMBL278072 1 8.15
CHEMBL20003 1 8.15
CHEMBL277618 1 8.15
CHEMBL20323 1 8.15
CHEMBL20343 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277701 IC50 = 0.2 nM 9.70
CHEMBL20195 IC50 = 0.3 nM 9.52
CHEMBL19640 IC50 = 0.6 nM 9.22
CHEMBL19747 IC50 = 0.7 nM 9.15
CHEMBL20019 IC50 = 0.7 nM 9.15
CHEMBL283162 IC50 = 1.0 nM 9.00
CHEMBL282883 IC50 = 1.0 nM 9.00
CHEMBL281779 IC50 = 1.0 nM 9.00
CHEMBL279665 IC50 = 2.0 nM 8.70
CHEMBL429066 IC50 = 3.0 nM 8.52
CHEMBL20163 IC50 = 3.0 nM 8.52
CHEMBL20267 IC50 = 4.0 nM 8.40
CHEMBL20418 IC50 = 4.0 nM 8.40
CHEMBL283339 IC50 = 4.0 nM 8.40
CHEMBL280210 IC50 = 4.0 nM 8.40
CHEMBL20208 IC50 = 5.0 nM 8.30
CHEMBL280683 IC50 = 5.0 nM 8.30
CHEMBL20877 IC50 = 5.0 nM 8.30
CHEMBL277029 IC50 = 5.0 nM 8.30
CHEMBL20194 IC50 = 5.0 nM 8.30
CHEMBL19947 IC50 = 5.0 nM 8.30
CHEMBL277246 IC50 = 6.0 nM 8.22
CHEMBL21224 IC50 = 6.0 nM 8.22
CHEMBL435756 IC50 = 6.0 nM 8.22
CHEMBL282905 IC50 = 6.0 nM 8.22
CHEMBL278072 IC50 = 7.0 nM 8.15
CHEMBL20323 IC50 = 7.0 nM 8.15
CHEMBL20003 IC50 = 7.0 nM 8.15
CHEMBL277618 IC50 = 7.0 nM 8.15
CHEMBL20343 IC50 = 9.0 nM 8.05
CHEMBL279234 IC50 = 9.0 nM 8.05
CHEMBL19801 IC50 = 10.0 nM 8.00
CHEMBL283525 IC50 = 12.0 nM 7.92
CHEMBL417275 IC50 = 12.0 nM 7.92
CHEMBL280401 IC50 = 12.0 nM 7.92
CHEMBL277650 IC50 = 13.0 nM 7.89
CHEMBL20644 IC50 = 15.0 nM 7.82
CHEMBL277678 IC50 = 15.0 nM 7.82
CHEMBL430333 IC50 = 15.0 nM 7.82
CHEMBL418556 IC50 = 15.0 nM 7.82
CHEMBL279664 IC50 = 20.0 nM 7.70
CHEMBL20033 IC50 = 20.0 nM 7.70
CHEMBL278635 IC50 = 25.0 nM 7.60
CHEMBL20691 IC50 = 25.0 nM 7.60
CHEMBL282495 IC50 = 25.0 nM 7.60
CHEMBL279893 IC50 = 30.0 nM 7.52
CHEMBL20293 IC50 = 30.0 nM 7.52
CHEMBL277245 IC50 = 40.0 nM 7.40
CHEMBL19991 IC50 = 45.0 nM 7.35
CHEMBL279021 IC50 = 50.0 nM 7.30