dazoxiben [Ligand Id: 5175] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL267473 (Dazoxiben, UK-37248)
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP11B1/Cytochrome P450 11B1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4970] [GtoPdb: 1359] [UniProtKB: P15393]
ChEMBL Inhibition of rat adrenal 11-beta-hydroxylase B 4 pIC50 >100000 nM IC50 J Med Chem (1986) 29: 1643-1650 [PMID:3091830]
ChEMBL Inhibition of rat adrenal 11-beta-hydroxylase B 4 pIC50 >100000 nM IC50 J Med Chem (1985) 28: 1427-1432 [PMID:3930740]
ChEMBL Inhibition of 11 beta-hydroxylase from rat adrenal gland B 4 pIC50 >100000 nM IC50 J Med Chem (1986) 29: 342-346 [PMID:3081722]
CYP8A1/Prostaglandin I2 synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4428] [GtoPdb: 1356] [UniProtKB: Q16647]
ChEMBL Inhibition of porcine aorta prostacyclin PGI-2 synthetase B 4 pIC50 >100000 nM IC50 J Med Chem (1986) 29: 1643-1650 [PMID:3091830]
ChEMBL Inhibition of porcine aorta prostacyclin PGI-2 synthase B 4 pIC50 >100000 nM IC50 J Med Chem (1985) 28: 1427-1432 [PMID:3930740]
ChEMBL Inhibition of PGI-2 synthetase from porcine aorta B 4 pIC50 >100000 nM IC50 J Med Chem (1986) 29: 342-346 [PMID:3081722]
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL Inhibition of Thromboxane A2 synthase after oral administration of 0.03 mmol/kg B 5.6 pIC50 2500 nM IC50 J Med Chem (1990) 33: 646-652 [PMID:2299629]
ChEMBL Tested for inhibitory activity against intact human platelet TXA2 formation F 5.89 pIC50 1290 nM IC50 J Med Chem (1987) 30: 1588-1595 [PMID:3305945]
ChEMBL Inhibition of Thromboxane B2 formation in collagen-stimulated human platelets in platelet rich plasma. F 5.89 pIC50 1290 nM IC50 J Med Chem (1987) 30: 1812-1818 [PMID:3656356]
ChEMBL Inhibition of Thromboxane-A synthase B 5.96 pIC50 1100 nM IC50 J Med Chem (2000) 43: 1841-1851 [PMID:10794700]
ChEMBL Inhibition of thromboxane synthase P450 TXA2 B 5.96 pIC50 1100 nM IC50 J Med Chem (2000) 43: 4437-4445 [PMID:11087568]
ChEMBL Inhibition of platelet microsomal thromboxane A synthetase in humans B 6.21 pIC50 620 nM IC50 J Med Chem (1989) 32: 1265-1272 [PMID:2724299]
ChEMBL Inhibitory activity to inhibit Inophore-induced arachidonic acid metabolism (inhibition of TXB2 formation) in rat F 6.52 pIC50 300 nM IC50 J Med Chem (1989) 32: 1842-1860 [PMID:2547071]
ChEMBL Inhibition of human platelet thromboxane synthase (TXA2) was determined in human platelets B 6.6 pIC50 250 nM IC50 J Med Chem (1987) 30: 185-193 [PMID:2879917]
ChEMBL Inhibition of platelet microsomal thromboxane A synthetase in rabbits B 6.97 pIC50 106 nM IC50 J Med Chem (1989) 32: 1265-1272 [PMID:2724299]
ChEMBL In vitro inhibitory activity against human microsomal thromboxane synthase. B 7.15 pIC50 70 nM IC50 J Med Chem (1995) 38: 1608-1628 [PMID:7752186]
ChEMBL In vitro inhibition of Thromboxane synthase using [14C]arachidonic acid as radioligand B 7.55 pIC50 28 nM IC50 J Med Chem (1991) 34: 1790-1797 [PMID:1829485]
GtoPdb - - 8.5 pIC50 - - - Thromb Res (1981) 23: 145-62 [PMID:6795753]
ChEMBL Inhibition of TXA2 synthetase from human platelets B 8.52 pIC50 3 nM IC50 J Med Chem (1986) 29: 342-346 [PMID:3081722]
ChEMBL Inhibition of thromboxane TXA2 synthetase from human platelets B 8.52 pIC50 3 nM IC50 J Med Chem (1986) 29: 1643-1650 [PMID:3091830]
ChEMBL Inhibitory activity against thromboxane A2 synthetase B 8.52 pIC50 3 nM IC50 J Med Chem (1985) 28: 1427-1432 [PMID:3930740]
ChEMBL In vitro inhibition of thromboxane synthase from human platelets. B 8.52 pIC50 3 nM IC50 J Med Chem (1986) 29: 1637-1643 [PMID:3746813]
CYP5A1/Thromboxane-A synthase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4028] [GtoPdb: 1353] [UniProtKB: P49430]
ChEMBL Inhibition of thromboxane formation at a concentration of 10e -6 M. B 5.82 pIC50 1500 nM IC50 J Med Chem (1987) 30: 1036-1040 [PMID:3585902]
ChEMBL Compound was tested for inhibitory activity against thromboxane synthetase B 5.82 pIC50 1500 nM IC50 J Med Chem (1986) 29: 523-530 [PMID:3959030]
ChEMBL Compound was tested for the inhibition of thromboxane formation (thromboxane synthetase) in platelets at a concentration of 10e-4 M F 5.82 pIC50 1500 nM IC50 J Med Chem (1986) 29: 816-819 [PMID:3517332]
ChEMBL In vitro inhibition of thromboxane B2 production in rat whole blood. F 5.92 pIC50 1200 nM IC50 J Med Chem (1993) 36: 2964-2972 [PMID:8411014]
ChEMBL Tested for inhibition of thromboxane synthetase from spontaneously hypertensive rats B 6.82 pIC50 150 nM IC50 J Med Chem (1987) 30: 2277-2283 [PMID:3681898]
ChEMBL Inhibition of thromboxane A2 synthetase B 6.97 pIC50 106 nM IC50 J Med Chem (1989) 32: 1265-1272 [PMID:2724299]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]