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Assay Detail

CHEMBL764536

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

Binding
In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets.
30
Total Activities
30
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

Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
Walser A, Flynn T, Mason C, Crowley H, Maresca C, O'Donnell M.
J Med Chem (1991) 34 : 1440 -1446
PubMed 2016721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.94 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34461 1 8.10
CHEMBL442259 1 8.00
CHEMBL430919 1 8.00
CHEMBL286217 1 8.00
CHEMBL32475 1 7.70
CHEMBL287465 1 7.70
CHEMBL289463 1 7.70
CHEMBL32942 1 7.52
CHEMBL432850 1 7.46
CHEMBL284079 1 7.22
CHEMBL286229 1 7.10
CHEMBL369194 1 7.00
CHEMBL286762 1 6.96
CHEMBL32389 1 6.92
CHEMBL286557 1 6.75
CHEMBL32327 1 6.75
CHEMBL280164 APAFANT 2.0 1 6.70
CHEMBL285035 1 6.60
CHEMBL32479 BROTIZOLAM 4.0 1 6.52
CHEMBL33857 1 6.52
CHEMBL20359 1 6.43
CHEMBL284280 1 6.42
CHEMBL286337 1 6.40
CHEMBL32932 1 6.40
CHEMBL34796 1 6.38
CHEMBL285199 1 6.38
CHEMBL285067 1 6.35
CHEMBL32767 1 6.19
CHEMBL32303 1 6.00
CHEMBL33217 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34461 IC50 = 8.0 nM 8.10
CHEMBL442259 IC50 = 10.0 nM 8.00
CHEMBL430919 IC50 = 10.0 nM 8.00
CHEMBL286217 IC50 = 10.0 nM 8.00
CHEMBL32475 IC50 = 20.0 nM 7.70
CHEMBL287465 IC50 = 20.0 nM 7.70
CHEMBL289463 IC50 = 20.0 nM 7.70
CHEMBL32942 IC50 = 30.0 nM 7.52
CHEMBL432850 IC50 = 35.0 nM 7.46
CHEMBL284079 IC50 = 60.0 nM 7.22
CHEMBL286229 IC50 = 80.0 nM 7.10
CHEMBL369194 IC50 = 100.0 nM 7.00
CHEMBL286762 IC50 = 110.0 nM 6.96
CHEMBL32389 IC50 = 120.0 nM 6.92
CHEMBL286557 IC50 = 180.0 nM 6.75
CHEMBL32327 IC50 = 180.0 nM 6.75
CHEMBL280164 APAFANT IC50 = 200.0 nM 6.70
CHEMBL285035 IC50 = 250.0 nM 6.60
CHEMBL32479 BROTIZOLAM IC50 = 300.0 nM 6.52
CHEMBL33857 IC50 = 300.0 nM 6.52
CHEMBL20359 IC50 = 370.0 nM 6.43
CHEMBL284280 IC50 = 380.0 nM 6.42
CHEMBL286337 IC50 = 400.0 nM 6.40
CHEMBL32932 IC50 = 400.0 nM 6.40
CHEMBL34796 IC50 = 420.0 nM 6.38
CHEMBL285199 IC50 = 420.0 nM 6.38
CHEMBL285067 IC50 = 450.0 nM 6.35
CHEMBL32767 IC50 = 650.0 nM 6.19
CHEMBL32303 IC50 = 1000.0 nM 6.00
CHEMBL33217 IC50 = 1000.0 nM 6.00