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 US8741955B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (null)
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 US8741955B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (null)
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 US8741955B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (null)
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]