pitavastatin [Ligand Id: 3035] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1201753 (Itavastatin, NSC-760423, Pitavastatin, Pitavastatina, Pitavastatine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639] | ||||||||
| GtoPdb | Note this assay used the pitavastatin calcium salt. | - | 5.05 | pKi | 8900 | nM | Ki | Bioorg Med Chem (2009) 17: 7915-23 [PMID:19879766] |
| ChEMBL | Inhibition of HMG-CoA reductase in rat liver microsomes assessed as reduction in [14C]-HMG-CoA conversion to [14C]-mevalonic acid after 15 mins by column filtration method | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2016) 59: 8712-8756 [PMID:27299736] |
| Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5002] [GtoPdb: 630] [UniProtKB: P43354] | ||||||||
| ChEMBL | Agonist activity at human Nurr1 measured by Gal4-Nurr1 hybrid reporter gene assay | B | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2022) 65: 9548-9563 [PMID:35797147] |
| ChEMBL | Agonist activity at Gal4-fused human full length Nurr1 transfected in human HEK293T cells co-transfected with pFR-Luc/pRL-SV40 assessed as activation of luciferase activity incubated for 16 hrs by Dual-Glo luciferase assay | B | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2023) 66: 13556-13567 [PMID:37751901] |
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]
