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 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]