GT-0198 [Ligand Id: 11297] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3325507
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GlyT2/Glycine transporter 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3060] [GtoPdb: 936] [UniProtKB: Q9Y345]
ChEMBL Inhibition of human GlyT2 transfected in HEK293 cells assessed as [3H]glycine uptake after 2 hrs B 6.98 pIC50 105 nM IC50 Bioorg Med Chem Lett (2014) 24: 4603-4606 [PMID:25176190]
ChEMBL Inhibition of human GlyT-2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake B 6.98 pIC50 105 nM IC50 J Med Chem (2018) 61: 2652-2679 [PMID:28876062]
ChEMBL Reversible inhibition of recombinant human GlyT2 expressed in HEK293 cells assessed as reduction in [3H]-glycine uptake after 2 hrs by top count assay B 6.98 pIC50 105 nM IC50 J Med Chem (2019) 62: 2466-2484 [PMID:30714733]
GtoPdb - - 8.8 pIC50 1.6 nM IC50 J Pharmacol Sci (2015) 127: 377-81 [PMID:25837937]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]