Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL761643

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

Binding
Ability to inhibit platelet activating factor (PAF) binding to platelets by 50% was determined by using [3H]PAF as radioligand
34
Total Activities
34
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

Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists.
Tilley JW, Burghardt B, Burghardt C, Mowles TF, Leinweber FJ, Klevans L, Young R, Hirkaler G, Fahrenholtz K, Zawoiski S.
J Med Chem (1988) 31 : 466 -472
PubMed 3339617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.19 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143914 1 7.00
CHEMBL291332 1 6.75
CHEMBL141825 1 6.70
CHEMBL57825 1 6.60
CHEMBL56588 1 6.60
CHEMBL57736 1 6.46
CHEMBL56418 1 6.43
CHEMBL142903 1 6.40
CHEMBL417781 1 6.40
CHEMBL294706 1 6.35
CHEMBL300338 1 6.30
CHEMBL295212 1 6.22
CHEMBL57716 1 6.22
CHEMBL142433 1 6.22
CHEMBL58518 1 6.16
CHEMBL57489 1 6.00
CHEMBL293362 1 6.00
CHEMBL57480 1 5.92
CHEMBL301215 1 5.92
CHEMBL57072 1 5.89
CHEMBL60625 1 5.75
CHEMBL418141 1 5.60
CHEMBL56434 1 5.46
CHEMBL56742 1 5.30
CHEMBL142354 1 -
CHEMBL143740 1 -
CHEMBL141818 1 -
CHEMBL60930 1 -
CHEMBL143037 1 -
CHEMBL143040 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143914 IC50 = 100.0 nM 7.00
CHEMBL291332 IC50 = 180.0 nM 6.75
CHEMBL141825 IC50 = 200.0 nM 6.70
CHEMBL57825 IC50 = 250.0 nM 6.60
CHEMBL56588 IC50 = 250.0 nM 6.60
CHEMBL57736 IC50 = 350.0 nM 6.46
CHEMBL56418 IC50 = 370.0 nM 6.43
CHEMBL142903 IC50 = 400.0 nM 6.40
CHEMBL417781 IC50 = 400.0 nM 6.40
CHEMBL294706 IC50 = 450.0 nM 6.35
CHEMBL300338 IC50 = 500.0 nM 6.30
CHEMBL295212 IC50 = 600.0 nM 6.22
CHEMBL57716 IC50 = 600.0 nM 6.22
CHEMBL142433 IC50 = 600.0 nM 6.22
CHEMBL58518 IC50 = 700.0 nM 6.16
CHEMBL57489 IC50 = 1000.0 nM 6.00
CHEMBL293362 IC50 = 1000.0 nM 6.00
CHEMBL57480 IC50 = 1200.0 nM 5.92
CHEMBL301215 IC50 = 1200.0 nM 5.92
CHEMBL57072 IC50 = 1300.0 nM 5.89
CHEMBL60625 IC50 = 1800.0 nM 5.75
CHEMBL418141 IC50 = 2500.0 nM 5.60
CHEMBL56434 IC50 = 3500.0 nM 5.46
CHEMBL56742 IC50 = 5000.0 nM 5.30
CHEMBL142354 IC50 > 1000.0 nM -
CHEMBL143740 IC50 > 1000.0 nM -
CHEMBL141818 IC50 > 1000.0 nM -
CHEMBL60930 IC50 > 1000.0 nM -
CHEMBL143037 IC50 > 1000.0 nM -
CHEMBL143040 IC50 > 1000.0 nM -
CHEMBL60764 IC50 > 1000.0 nM -
CHEMBL56932 IC50 > 1000.0 nM -
CHEMBL141336 IC50 > 1000.0 nM -
CHEMBL142786 IC50 > 1000.0 nM -