methylphenidate [Ligand Id: 7236] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL796 (Concerta, Cotempla xr-odt, Daytrana, Methylin, Methylphenidate, Methylphenidate extended release, Metilfenidato, Prc-063, Threo-dl-methylphenidate)
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
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]
ChEMBL Displacement of [125I]RTI-55 from human DAT expressing HEK293 cells B 6.96 pKi 110 nM Ki J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL Displacement of [3H]WIN 35,428 from human DAT expressed in HEK293E cells after 1 hr by liquid scintillation counting B 7.47 pKi 34 nM Ki ACS Med Chem Lett (2014) 5: 760-765 [PMID:25050161]
GtoPdb - - 7.1 pIC50 79 nM IC50 J Med Chem (2007) 50: 219-32 [PMID:17228864]
ChEMBL Inhibition of [3H]DA uptake at human DAT expressing HEK293 cells B 7.1 pIC50 79 nM IC50 J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL Inhibition of [3H]WIN-35428 Binding to the Dopamine Transporter in Rhesus (Macaca mulatta) orCynomolgus Monkey (Macaca fascicularis) Caudate-Putamen B 7.77 pIC50 17 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 Tested for the ability to bind stereoselectively and enantioselectively to the dopamine transporter (DAT); Value ranges from 34 - 83 nM B 7.08 pIC50 83 nM IC50 J Med Chem (2003) 46: 1538-1545 [PMID:12672255]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL Displacement of [125I]RTI-55 from human NET expressing HEK293 cells B 6.18 pKi 660 nM Ki J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL Displacement of [3H]Nisoxetine from human NET expressed in HEK293E cells after 1 hr by liquid scintillation counting B 6.47 pKi 340 nM Ki ACS Med Chem Lett (2014) 5: 760-765 [PMID:25050161]
GtoPdb - - 7.21 pIC50 61 nM IC50
ChEMBL Inhibition of [3H]NE uptake into human NET expressing HEK293 cells B 7.21 pIC50 61 nM IC50 J Med Chem (2007) 50: 219-232 [PMID:17228864]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Displacement of [125I]RTI-55 from human SERT expressing HEK293 cells B 4.19 pKi 65000 nM Ki J Med Chem (2007) 50: 219-232 [PMID:17228864]
ChEMBL Displacement of [3H]Citolapram from human SERT expressed in HEK293E cells after 1 hr by liquid scintillation counting B 5 pKi >10000 nM Ki ACS Med Chem Lett (2014) 5: 760-765 [PMID:25050161]
ChEMBL Inhibition of [3H]5-HT uptake into human SERT expressing HEK293 cells B 5.29 pIC50 5100 nM IC50 J Med Chem (2007) 50: 219-232 [PMID:17228864]

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]