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ChEMBL ligand: CHEMBL827 (Dexmethylphenidate, Methylphenidate d-threo-form) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
GtoPdb | Displacement of [3H]WIN-35428 from human DAT stably expressed in mouse N2A cells | - | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem (2011) 19: 504-12 [PMID:21129986] |
ChEMBL | Displacement of [3H]WIN-35428 from human DAT stably expressed in mouse N2A cells by scintillation countnig | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem (2011) 19: 504-512 [PMID:21129986] |
ChEMBL | Displacement of [3H]WIN-35,428 from human DAT expressed in mouse N2A cells after 15 mins by liquid scintillation counting | B | 7.8 | pKi | 16 | nM | Ki | ACS Med Chem Lett (2012) 3: 378-382 [PMID:23066448] |
ChEMBL | Inhibition of [3H]dopamine uptake at human DAT expressed in mouse N2A cells | B | 6.81 | pIC50 | 156 | nM | IC50 | Bioorg Med Chem (2011) 19: 504-512 [PMID:21129986] |
ChEMBL | Inhibition of [3H]WIN-35428 Binding to the Dopamine Transporter in Rhesus (Macaca mulatta) orCynomolgus Monkey (Macaca fascicularis) Caudate-Putamen | B | 7.06 | pIC50 | 88 | nM | IC50 | J Med Chem (2003) 46: 1538-1545 [PMID:12672255] |
DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
ChEMBL | Displacement of [3H]WIN 35428 from Sprague-Dawley rat striatal tissue after 2 hrs by liquid scintillation counting | B | 7.08 | pIC50 | 83.18 | nM | IC50 | Bioorg Med Chem (2010) 18: 7221-7238 [PMID:20846865] |
ChEMBL | The compound was tested for its affinity at the rat striatal dopamine transporter by the displacement of [3H]WIN-35428 | B | 7.08 | pIC50 | 83 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 1213-1218 |
ChEMBL | Inhibitory potency against dopamine (DA) transporter using [3H]WIN-35428 (WIN-) binding assay. | B | 7.08 | pIC50 | 83 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
ChEMBL | Displacement of [3H]WIN 35428 from Sprague-Dawley rat striatal tissue after 2 hrs by liquid scintillation counting | B | 7.08 | pIC50 | 83 | nM | IC50 | Bioorg Med Chem (2010) 18: 7221-7238 [PMID:20846865] |
ChEMBL | Inhibitory potency against [3H]DA uptake using [3H]WIN-35428 (WIN-) binding assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
ChEMBL | Selectivity for the norepinephrine transporter using [3H]nisoxetine binding assay | B | 6 | pIC50 | 989 | nM | IC50 | J Med Chem (1999) 42: 4836-4843 [PMID:10579846] |
NET in Rat [GtoPdb: 926] | ||||||||
GtoPdb | Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat cortical tissue. | - | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2007) 50: 2718-31 [PMID:17489581] |
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]