N-methyl-SSR504734 [Ligand Id: 4604] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1939495
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GlyT1/Glycine transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2337] [GtoPdb: 935] [UniProtKB: P48067]
ChEMBL Inhibition of GlyT1 in human JAR cells assessed as inhibition of [3H]glycine uptake preincubated for 1 mins measured after 2 hrs by liquid scintillation counting B 8.12 pIC50 7.51 nM IC50 Bioorg Med Chem (2011) 19: 6245-6253 [PMID:21975065]
ChEMBL Inhibition of recombinant human GlyT1 expressed in CHO cells assessed as reduction in [3H]glycine uptake pretreated for 15 mins followed by [3H]glycine addition measured after 2 hrs by Topcount method B 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2018) 28: 1043-1049 [PMID:29486970]
GtoPdb - - 8.6 pIC50 2.5 nM IC50
ChEMBL Inhibition of human GlyT1 expressed in CHO cells assessed as inhibition of [3H]glycine uptake preincubated for 1 mins measured after 2 hrs by liquid scintillation counting B 8.6 pIC50 2.5 nM IC50 Bioorg Med Chem (2011) 19: 6245-6253 [PMID:21975065]

ChEMBL data shown on this page come from version 33:

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]