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Assay Detail

CHEMBL764097

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

Binding
Inhibition of [3H]PAF receptor binding to washed human platelet membranes determined in vitro
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Cyclic ether acetal platelet activating factor (PAF) receptor antagonists II: imidazo[4,5-c]pyridyl derivatives
Wood L, Whittaker M, Timmis DJ, Thompson TM, Saroglou L, Miller A, Davidson AH, Christodoulou MS, Cackett KS, Bowles SA, Bebbington DS
Bioorg Med Chem Lett (1993) 3 : 1499 -1504
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.21 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34548 1 8.52
CHEMBL284276 1 8.30
CHEMBL288329 1 8.15
CHEMBL37358 1 8.15
CHEMBL37357 1 8.00
CHEMBL1793831 1 7.89
CHEMBL35776 1 7.82
CHEMBL34182 1 7.70
CHEMBL34361 1 7.60
CHEMBL36269 1 7.00
CHEMBL34612 1 6.92
CHEMBL286197 1 6.82
CHEMBL36154 1 6.72
CHEMBL286696 1 6.60
CHEMBL418608 1 6.52
CHEMBL34669 1 6.30
CHEMBL37770 1 6.30
CHEMBL37602 1 6.05
CHEMBL37792 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34548 IC50 = 3.0 nM 8.52
CHEMBL284276 IC50 = 5.0 nM 8.30
CHEMBL288329 IC50 = 7.0 nM 8.15
CHEMBL37358 IC50 = 7.0 nM 8.15
CHEMBL37357 IC50 = 10.0 nM 8.00
CHEMBL1793831 IC50 = 13.0 nM 7.89
CHEMBL35776 IC50 = 15.0 nM 7.82
CHEMBL34182 IC50 = 20.0 nM 7.70
CHEMBL34361 IC50 = 25.0 nM 7.60
CHEMBL36269 IC50 = 100.0 nM 7.00
CHEMBL34612 IC50 = 120.0 nM 6.92
CHEMBL286197 IC50 = 150.0 nM 6.82
CHEMBL36154 IC50 = 190.0 nM 6.72
CHEMBL286696 IC50 = 250.0 nM 6.60
CHEMBL418608 IC50 = 300.0 nM 6.52
CHEMBL34669 IC50 = 500.0 nM 6.30
CHEMBL37770 IC50 = 500.0 nM 6.30
CHEMBL37602 IC50 = 900.0 nM 6.05
CHEMBL37792 IC50 = 2000.0 nM 5.70