flupentixol [Ligand Id: 948] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL54661 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D1 receptor in Human [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| GtoPdb | Note that this assay uses the cis form of the compound, whereas the approved drug is a racemic mixture of cis and trans molecules. | - | 8.4 | pKi | - | - | - |
Nature (1991) 350: 614-9 [PMID:1826762]; J Biol Chem (1994) 269: 27925-31 [PMID:7525564] |
| D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vivo binding affinity against dopamine (D1) receptor in rat caudate-putamen tissue using [3H]SCH-23390 as radioligand | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497] |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | The compound was tested for affinity towards sigma-3 receptor | B | 8.65 | pIC50 | 2.24 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
| D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| GtoPdb | - | - | 8.82 | pKi | 1.5 | nM | Ki | J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582] |
| D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 8.96 | pKi | 1.1 | nM | Ki | J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582] |
| D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
ChEMBL data shown on this page come from version 36:
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]
