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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]