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Assay Detail

CHEMBL770633

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Functional
Inhibition of PAF-induced rabbit platelet aggregation
42
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Platelet-activating factor receptor (CHEMBL5136)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines.
Lamouri A, Heymans F, Tavet F, Dive G, Batt JP, Blavet N, Braquet P, Godfroid JJ.
J Med Chem (1993) 36 : 990 -1000
PubMed 8478911 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.29 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6270 3 7.40
CHEMBL6203 3 7.10
CHEMBL258053 1 7.10
CHEMBL269133 1 7.00
CHEMBL269134 1 7.00
CHEMBL268596 3 7.00
CHEMBL6232 1 6.92
CHEMBL6359 1 6.89
CHEMBL380444 1 6.89
CHEMBL6202 1 6.85
CHEMBL332848 1 6.77
CHEMBL269340 1 6.62
CHEMBL269132 1 6.55
CHEMBL258253 1 6.54
CHEMBL268597 1 6.54
CHEMBL1793831 1 6.52
CHEMBL6211 1 6.51
CHEMBL266886 1 6.50
CHEMBL24879 1 6.43
CHEMBL269131 1 6.42
CHEMBL6341 1 6.38
CHEMBL6217 1 6.37
CHEMBL204022 1 6.33
CHEMBL514432 GINKOLIDE B 1 6.13
CHEMBL6319 1 5.90
CHEMBL6244 1 5.75
CHEMBL414007 1 5.57
CHEMBL266184 1 5.55
CHEMBL6350 1 5.41
CHEMBL265773 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6270 IC50 = 40.0 nM 7.40
CHEMBL6270 IC50 = 60.0 nM 7.22
CHEMBL6270 IC50 = 70.0 nM 7.16
CHEMBL6203 IC50 = 80.0 nM 7.10
CHEMBL258053 IC50 = 80.0 nM 7.10
CHEMBL268596 IC50 = 100.0 nM 7.00
CHEMBL269133 IC50 = 100.0 nM 7.00
CHEMBL269134 IC50 = 100.0 nM 7.00
CHEMBL268596 IC50 = 100.0 nM 7.00
CHEMBL268596 IC50 = 120.0 nM 6.92
CHEMBL6232 IC50 = 120.0 nM 6.92
CHEMBL380444 IC50 = 130.0 nM 6.89
CHEMBL6359 IC50 = 130.0 nM 6.89
CHEMBL6202 IC50 = 140.0 nM 6.85
CHEMBL332848 IC50 = 170.0 nM 6.77
CHEMBL6203 IC50 = 170.0 nM 6.77
CHEMBL269340 IC50 = 240.0 nM 6.62
CHEMBL269132 IC50 = 280.0 nM 6.55
CHEMBL258253 IC50 = 290.0 nM 6.54
CHEMBL268597 IC50 = 290.0 nM 6.54
CHEMBL1793831 IC50 = 300.0 nM 6.52
CHEMBL6211 IC50 = 310.0 nM 6.51
CHEMBL266886 IC50 = 320.0 nM 6.50
CHEMBL24879 IC50 = 370.0 nM 6.43
CHEMBL269131 IC50 = 380.0 nM 6.42
CHEMBL6341 IC50 = 420.0 nM 6.38
CHEMBL6217 IC50 = 430.0 nM 6.37
CHEMBL204022 IC50 = 470.0 nM 6.33
CHEMBL514432 GINKOLIDE B IC50 = 740.0 nM 6.13
CHEMBL6203 IC50 = 880.0 nM 6.06
CHEMBL6319 IC50 = 1250.0 nM 5.90
CHEMBL6244 IC50 = 1780.0 nM 5.75
CHEMBL414007 IC50 = 2700.0 nM 5.57
CHEMBL266184 IC50 = 2820.0 nM 5.55
CHEMBL6350 IC50 = 3900.0 nM 5.41
CHEMBL265773 IC50 = 5000.0 nM 5.30
CHEMBL414696 IC50 = 10300.0 nM 4.99
CHEMBL6263 IC50 = 11400.0 nM 4.94
CHEMBL267229 IC50 = 12500.0 nM 4.90
CHEMBL267357 IC50 = 13800.0 nM 4.86
CHEMBL6322 PMS-601 IC50 = 25800.0 nM 4.59
CHEMBL227457 IC50 = 45000.0 nM 4.35