LY367385 [Ligand Id: 1379] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL94631 (LY-367385)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor in Rat [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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 4.72 pIC50 19000 nM IC50 Bioorg Med Chem Lett (1997) 7: 2777-2780
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 5.06 pIC50 8800 nM IC50 Bioorg Med Chem Lett (1997) 7: 2777-2780
ChEMBL Compound was tested for its agonist activity against Ser165 and Thr188 (Metabotropic glutamate receptor 1) receptor. F 5.06 pIC50 8800 nM IC50 J Med Chem (1999) 42: 5390-5401 [PMID:10639281]
ChEMBL Negative allosteric modulation of human mGluR1alpha expressed in syrian hamster AV-12 cells assessed as inhibition of quisqualate-induced phosphoinositide hydrolysis B 5.1 pIC50 8000 nM IC50 Bioorg Med Chem (2015) 23: 3880-3906 [PMID:25638496]
GtoPdb - - 5.1 pIC50 8800 nM IC50 Bioorg Med Chem Lett (1997) 7: 2777-2780
mGlu1 receptor in Rat [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 5.9 pKi 1260 nM Ki Mol Pharmacol (2003) 63: 1082-93 [PMID:12695537]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Compound was tested for functional response of human metabotropic glutamate receptor mGluR5a expressed in AV-12 cells by measuring inhibitory concentration towards quisqualate induced PI hydrolysis F 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1997) 7: 2777-2780
ChEMBL Compound was tested for it's antagonist activity against Ser152 and Thr175 (Metabotropic glutamate receptor 5) F 4 pIC50 >100000 nM IC50 J Med Chem (1999) 42: 5390-5401 [PMID:10639281]

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]