(S)-4CPG [Ligand Id: 1418] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL94990 ((S)-4-(Amino(Carboxy)Methyl)Benzoic Acid, (S)-4-Carboxyphenylglycine, S-4-Carboxyphenylglycine)
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Cystine/glutamate transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075149] [GtoPdb: 902] [UniProtKB: Q9UPY5]
ChEMBL Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting B 4.82 pIC50 15000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 6184-6187 [PMID:21889337]
ChEMBL Inhibition of amino acid transport system xc- B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2680-2683 [PMID:20303751]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Agonist potency against cloned human metabotropic glutamate receptor 1 F 4.08 pKi 84000 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Inhibitory concentration for half maximal inhibition of PI hydrolysis (mGluR1a) B 4.19 pIC50 65000 nM IC50 J. Med. Chem. (1996) 39: 3998-4006 [PMID:8831765]
ChEMBL Compound was tested for functional response of human metabotropic glutamate receptor mGluR1-alpha expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis F 4.24 pIC50 58000 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 2777-2780
ChEMBL Antagonist activity at mGlu1 receptor F 5 pIC50 10000 nM IC50 J. Med. Chem. (2007) 50: 2563-2568 [PMID:17489573]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 5.4 pKi - - - Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537]
ChEMBL Inhibition of binding to rat mGluR1a (metabotropic glutamate receptor) expressed in HEK-293 cells B 5.43 pKi 3700 nM Ki J. Med. Chem. (2002) 45: 3171-3183 [PMID:12109902]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 4.6 pIC50 - - - J Neurochem (2000) 75: 2590-601 [PMID:11080213]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]