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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 |
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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]