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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 |
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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 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]