ozagrel [Ligand Id: 9866] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL11662 (KCT-0809, Ozagrel, Ozagrel sodium) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TP receptor/Thromboxane A2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2069] [GtoPdb: 346] [UniProtKB: P21731] | ||||||||
| ChEMBL | In vitro thromboxane-A2 receptor binding affinity to displace by 50% [3H]-SQ 29548 binding from washed human platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1994) 37: 3588-3604 [PMID:7932586] |
| CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] | ||||||||
| ChEMBL | Inhibitory activity against Thromboxane A2 synthase in human platelet microsome | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1087-1090 |
| ChEMBL | Inhibition of thromboxane A2 synthetase as reduced ADP-induced aggregation of human platelet rich plasma in the presence of pig aortal microsomes | F | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (1989) 32: 890-897 [PMID:2704033] |
| ChEMBL | Tested in vitro against TXA2 synthetase inhibitory activity in human whole blood | B | 6.05 | pIC50 | 900 | nM | IC50 | J Med Chem (1993) 36: 4061-4068 [PMID:8258828] |
| ChEMBL | Tested in vitro against TXA2 synthetase inhibitory activity in human platelet | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (1993) 36: 4061-4068 [PMID:8258828] |
| ChEMBL | Tested in vitro against TXA2 synthetase inhibitory activity in human microsome | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (1993) 36: 4061-4068 [PMID:8258828] |
| ChEMBL | In vitro inhibition of TXB2 production by incubating prostaglandin H2 with human platelet microsomes. | F | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 341-344 [PMID:11814792] |
| ChEMBL | In vitro inhibition of thromboxane synthase (TXA2) in human platelet microsomes [reduced formation of TXB2 from prostaglandin H2(PGH2)] | F | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 771-774 [PMID:11858999] |
| ChEMBL | Thromboxane A2 synthase inhibitory activity was measured from inhibition of thromboxane B2 production in human platelet microsomes | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1383-1386 [PMID:11992782] |
| GtoPdb | Inhibition of TXAB2 synthesis by microsome of human platelets. | - | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1996) 39: 3148-57 [PMID:8759636] |
| GtoPdb | Inhibition of thromboxane A2 synthetase activity in human washed platelets. | - | 8.4 | pIC50 | 4 | nM | IC50 | Jpn J Pharmacol (1986) 41: 393-401 [PMID:3093741] |
| CYP5A1/Thromboxane-A synthase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4028] [GtoPdb: 1353] [UniProtKB: P49430] | ||||||||
| ChEMBL | In vitro inhibition of thromboxane-A2 synthase in rat whole blood during clotting at 37 degrees Centigrade | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (1994) 37: 3588-3604 [PMID:7932586] |
| ChEMBL | Tested in vitro against TXA2 synthetase inhibitory activity in rat platelet | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1993) 36: 4061-4068 [PMID:8258828] |
| ChEMBL | Tested in vitro against TXA2 synthetase inhibitory activity in rat whole blood | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1993) 36: 4061-4068 [PMID:8258828] |
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]
