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Assay Detail

CHEMBL698311

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

Functional
In vitro antagonist activity, determined by 50% inhibition of PAF-induced platelet aggregation of human platelet rich plasma when challenged with PAF
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Dual antagonists of platelet activating factor and histamine. 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines.
Piwinski JJ, Wong JK, Green MJ, Kaminski JJ, Colizzo F, Albanese MM, Ganguly AK, Billah MM, Anthes JC, West RE.
Bioorg Med Chem Lett (1998) 8 : 3469 -3474
PubMed 9934454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 5.46 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280164 APAFANT 2.0 1 7.40
CHEMBL2448125 1 6.68
CHEMBL326821 1 6.40
CHEMBL332566 1 6.38
CHEMBL10971 SCH-37370 1 6.21
CHEMBL117289 1 6.18
CHEMBL2111767 1 5.89
CHEMBL326289 1 5.85
CHEMBL326978 1 5.75
CHEMBL116935 1 5.62
CHEMBL324336 1 4.92
CHEMBL117745 1 4.89
CHEMBL325909 1 4.85
CHEMBL333594 1 4.85
CHEMBL116144 1 4.82
CHEMBL331159 1 4.58
CHEMBL118807 1 4.55
CHEMBL1172 DESLORATADINE 4.0 1 4.51
CHEMBL331603 1 4.48
CHEMBL334318 1 4.39
CHEMBL325470 1 -
CHEMBL332936 1 -
CHEMBL410734 1 -
CHEMBL420316 1 -
CHEMBL505 CHLORPHENIRAMINE 4.0 1 -
CHEMBL998 LORATADINE 4.0 1 -
CHEMBL325718 1 -
CHEMBL117406 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280164 APAFANT IC50 = 40.0 nM 7.40
CHEMBL2448125 IC50 = 210.0 nM 6.68
CHEMBL326821 IC50 = 400.0 nM 6.40
CHEMBL332566 IC50 = 420.0 nM 6.38
CHEMBL10971 SCH-37370 IC50 = 610.0 nM 6.21
CHEMBL117289 IC50 = 660.0 nM 6.18
CHEMBL2111767 IC50 = 1300.0 nM 5.89
CHEMBL326289 IC50 = 1400.0 nM 5.85
CHEMBL326978 IC50 = 1800.0 nM 5.75
CHEMBL116935 IC50 = 2400.0 nM 5.62
CHEMBL324336 IC50 = 12000.0 nM 4.92
CHEMBL117745 IC50 = 13000.0 nM 4.89
CHEMBL325909 IC50 = 14000.0 nM 4.85
CHEMBL333594 IC50 = 14000.0 nM 4.85
CHEMBL116144 IC50 = 15000.0 nM 4.82
CHEMBL331159 IC50 = 26000.0 nM 4.58
CHEMBL118807 IC50 = 28000.0 nM 4.55
CHEMBL1172 DESLORATADINE IC50 = 31000.0 nM 4.51
CHEMBL331603 IC50 = 33000.0 nM 4.48
CHEMBL334318 IC50 = 41000.0 nM 4.39
CHEMBL325470 IC50 > 50000.0 nM -
CHEMBL332936 IC50 > 50000.0 nM -
CHEMBL410734 IC50 > 50000.0 nM -
CHEMBL420316 IC50 >= 50000.0 nM -
CHEMBL505 CHLORPHENIRAMINE IC50 > 50000.0 nM -
CHEMBL998 LORATADINE IC50 > 50000.0 nM -
CHEMBL325718 IC50 > 50000.0 nM -
CHEMBL117406 IC50 >= 23000.0 nM -