(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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| 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 | Antagonist activity at mGluR1alpha (unknown origin) | B | 4.19 | pIC50 | 65000 | nM | IC50 | J Med Chem (2021) 64: 14046-14128 [PMID:34591488] |
| 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 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]
