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ChEMBL ligand: CHEMBL644 (7162 RP, 7162-RP, IL 6001, IL-6001, Surmontil, Trimeproprimine, Trimipramina, Trimipramine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.56 | pIC50 | 27700 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
Cav2.2/Voltage-gated N-type calcium channel alpha-1B subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4478] [GtoPdb: 533] [UniProtKB: Q00975] | ||||||||
ChEMBL | Inhibition of endogenous human CaV2.2 in human SH-SY5Y cells in presence of nifedipine by Calcium 4 dye based calcium influx fluorescence-imaging assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | RSC Med Chem (2022) 13: 183-195 [PMID:35308021] |
NET in Human [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
GtoPdb | - | - | 5.61 | pKi | 2450 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
DAT in Human [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
GtoPdb | - | - | 5.42 | pKi | 3780 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
SERT in Human [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
GtoPdb | - | - | 6.83 | pKi | 149 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
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]