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 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]