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ChEMBL ligand: CHEMBL94631 (LY-367385) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]