Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL94631 (LY-367385) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]