trans-flupenthixol [Ligand Id: 968] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL42055 (.beta.-flupenthixol, E-flupenthixol, E-flupentixol, Flupentixol, (e)-, Flupentixole, Trans-flupenthixol, Trans-flupentixol) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D(1A) dopamine receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Binding affinity of compound towards Dopamine receptor D1 using [3H]SCH-23390 (0.5 nM) ligand in striatum bovine was determined | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (1997) 40: 952-960 [PMID:9083484] |
| D1 receptor/D(1A) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Binding affinity which represents concentration giving half-maximal inhibition of [3H]SCH-23390 (Dopamine receptor D1) binding to rat tissue homogenate | B | 7.42 | pKi | 37.8 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
| δ receptor/Delta-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity against opioid receptor delta 1 using [3H]naltrindole as radioligand in guinea pig brain membranes. | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2004) 47: 165-174 [PMID:14695830] |
| Kappa-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
| ChEMBL | Binding affinity against opioid receptor kappa 1 using [3H]-U-69,593 as radioligand in guinea pig brain membranes. | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2004) 47: 165-174 [PMID:14695830] |
| Mu-type opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
| ChEMBL | Binding affinity against opioid receptor mu 1 using [3H]DAMGO as radioligand in guinea pig brain membranes. | B | 7.05 | pKi | 90 | nM | Ki | J Med Chem (2004) 47: 165-174 [PMID:14695830] |
| 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 | 7.83 | pIC50 | 14.79 | nM | IC50 | J Med Chem (1994) 37: 4109-4117 [PMID:7990111] |
| D2 receptor in Human [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| GtoPdb | - | - | 6.92 | pKi | 120 | nM | Ki | J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582] |
| D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| GtoPdb | - | - | 6.52 | pKi | 300 | nM | Ki | J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582] |
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]
