dexmethylphenidate [Ligand Id: 7554] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL827 (Dexmethylphenidate, Methylphenidate d-threo-form)
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  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • NET in Rat [GtoPdb: 926]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]