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Assay Detail

CHEMBL815017

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Functional
In vitro inhibition of thromboxane B2 production in rat whole blood.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thromboxane-A synthase (CHEMBL4028)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Imidazol-1-yl and pyridin-3-yl derivatives of 4-phenyl-1,4-dihydropyridines combining Ca2+ antagonism and thromboxane A2 synthase inhibition.
Cozzi P, Carganico G, Fusar D, Grossoni M, Menichincheri M, Pinciroli V, Tonani R, Vaghi F, Salvati P.
J Med Chem (1993) 36 : 2964 -2972
PubMed 8411014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.42 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101233 1 6.77
CHEMBL100780 1 6.66
CHEMBL319993 1 6.62
CHEMBL100671 1 6.58
CHEMBL323095 1 6.57
CHEMBL101723 1 6.55
CHEMBL98611 1 6.52
CHEMBL103348 1 6.40
CHEMBL323096 1 6.19
CHEMBL320388 1 6.16
CHEMBL103656 1 6.14
CHEMBL267473 DAZOXIBEN 2.0 1 5.92
CHEMBL100607 1 -
CHEMBL101861 1 -
CHEMBL318342 1 -
CHEMBL193 NIFEDIPINE 4.0 1 -
CHEMBL101234 1 -
CHEMBL102156 1 -
CHEMBL555860 1 -
CHEMBL101942 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101233 IC50 = 170.0 nM 6.77
CHEMBL100780 IC50 = 220.0 nM 6.66
CHEMBL319993 IC50 = 240.0 nM 6.62
CHEMBL100671 IC50 = 260.0 nM 6.58
CHEMBL323095 IC50 = 270.0 nM 6.57
CHEMBL101723 IC50 = 280.0 nM 6.55
CHEMBL98611 IC50 = 300.0 nM 6.52
CHEMBL103348 IC50 = 400.0 nM 6.40
CHEMBL323096 IC50 = 640.0 nM 6.19
CHEMBL320388 IC50 = 700.0 nM 6.16
CHEMBL103656 IC50 = 730.0 nM 6.14
CHEMBL267473 DAZOXIBEN IC50 = 1200.0 nM 5.92
CHEMBL100607 IC50 > 1000.0 nM -
CHEMBL101861 IC50 > 1000.0 nM -
CHEMBL318342 IC50 > 1000.0 nM -
CHEMBL193 NIFEDIPINE IC50 > 10000.0 nM -
CHEMBL101234 IC50 > 1000.0 nM -
CHEMBL102156 IC50 > 1000.0 nM -
CHEMBL555860 IC50 > 1000.0 nM -
CHEMBL101942 IC50 > 1000.0 nM -