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 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]