trans-4-hydroxy-proline [Ligand Id: 4704] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL352418
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  • Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Amino acid transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562161] [UniProtKB: Q9Z1J7]
ChEMBL Inhibition of ASCT2 mediated [3H]-D-serine uptake in rat hippocampal astrocytes B 4.41 pIC50 38900 nM IC50 US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014)
ChEMBL Inhibition of ASCT2 in rat hippocampal astrocytes at high affinity component 1 assessed as reduction in [3H]-D-serine uptake after 5 mins by beta counting analysis B 4.76 pIC50 17200 nM IC50 US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014)
ChEMBL Inhibition of ASCT2 mediated [3H]-L-serine uptake at high affinity component in rat hippocampal astrocytes after 5 mins by beta counting analysis B 4.8 pIC50 16000 nM IC50 US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014)
Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8]
ChEMBL Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting B 0.95 pKi -0.95 mM pKi Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456]

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]