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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 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]