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Assay Detail

CHEMBL698058

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Functional
Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.
Piwinski JJ, Wong JK, Green MJ, Ganguly AK, Billah MM, West RE, Kreutner W.
J Med Chem (1991) 34 : 457 -461
PubMed 1671420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.63 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280164 APAFANT 2.0 1 7.40
CHEMBL10971 SCH-37370 1 6.21
CHEMBL344942 1 6.17
CHEMBL142268 1 6.09
CHEMBL143272 1 6.09
CHEMBL342747 1 6.00
CHEMBL143242 1 6.00
CHEMBL140483 1 5.85
CHEMBL297624 1 5.82
CHEMBL139760 1 5.75
CHEMBL116935 1 5.62
CHEMBL131155 1 5.47
CHEMBL334127 1 5.47
CHEMBL358332 1 5.06
CHEMBL325909 1 4.89
CHEMBL140919 1 4.55
CHEMBL331603 1 4.48
CHEMBL334318 1 4.39
CHEMBL124466 1 -
CHEMBL141432 1 -
CHEMBL946 AZATADINE 4.0 1 -
CHEMBL998 LORATADINE 4.0 1 -
CHEMBL140924 1 -
CHEMBL342455 1 -
CHEMBL341584 1 -
CHEMBL505 CHLORPHENIRAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280164 APAFANT IC50 = 40.0 nM 7.40
CHEMBL10971 SCH-37370 IC50 = 610.0 nM 6.21
CHEMBL344942 IC50 = 670.0 nM 6.17
CHEMBL142268 IC50 = 810.0 nM 6.09
CHEMBL143272 IC50 = 820.0 nM 6.09
CHEMBL342747 IC50 = 1000.0 nM 6.00
CHEMBL143242 IC50 = 1000.0 nM 6.00
CHEMBL140483 IC50 = 1400.0 nM 5.85
CHEMBL297624 IC50 = 1500.0 nM 5.82
CHEMBL139760 IC50 = 1800.0 nM 5.75
CHEMBL116935 IC50 = 2400.0 nM 5.62
CHEMBL131155 IC50 = 3400.0 nM 5.47
CHEMBL334127 IC50 = 3400.0 nM 5.47
CHEMBL358332 IC50 = 8700.0 nM 5.06
CHEMBL325909 IC50 = 13000.0 nM 4.89
CHEMBL140919 IC50 = 28000.0 nM 4.55
CHEMBL331603 IC50 = 33000.0 nM 4.48
CHEMBL334318 IC50 = 41000.0 nM 4.39
CHEMBL124466 IC50 > 50000.0 nM -
CHEMBL141432 IC50 > 50000.0 nM -
CHEMBL946 AZATADINE IC50 > 50000.0 nM -
CHEMBL998 LORATADINE IC50 > 50000.0 nM -
CHEMBL140924 IC50 > 50000.0 nM -
CHEMBL342455 IC50 > 50000.0 nM -
CHEMBL341584 IC50 > 50000.0 nM -
CHEMBL505 CHLORPHENIRAMINE IC50 > 50000.0 nM -