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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 |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]