LSP1-2111 [Ligand Id: 6739] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3114672 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
| ChEMBL | Displacement of [3H]-L-AP4 from human mGlu4 receptor | B | 5.07 | pIC50 | 8600 | nM | IC50 | ACS Med Chem Lett (2014) 5: 119-123 [PMID:24900783] |
| ChEMBL | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 5.66 | pEC50 | 2200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| ChEMBL | Agonist activity at human mGlu4 receptor by FLIPR assay relative to control | B | 5.82 | pEC50 | 1500 | nM | EC50 | ACS Med Chem Lett (2014) 5: 119-123 [PMID:24900783] |
| ChEMBL | Agonist activity at mGlu4 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay | F | 6.05 | pEC50 | 900 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105794] [GtoPdb: 292] [UniProtKB: Q68EF4] | ||||||||
| ChEMBL | Agonist activity at mGlu4 in C57/Bl6 mouse GP neurons assessed as inhibition of striatopallidal GABAergic inhibitory postsynaptic current amplitude by whole cell patch clamp assay | B | 6.7 | pEC50 | 200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Agonist activity at mGlu4 assessed as decrease in PF-induced presynaptic calcium amplitude in rat coronal slices by Fluo-4FF-AM dye based fluorescence assay | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| GtoPdb | - | - | 5.66 | pEC50 | 2200 | nM | EC50 | FASEB J (2009) 23: 3619-28 [PMID:19525404] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
| ChEMBL | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay | F | 5.49 | pEC50 | 3200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| ChEMBL | Agonist activity at mGlu6 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 5.77 | pEC50 | 1700 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu6 receptor in Rat [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| GtoPdb | - | - | 5.77 | pEC50 | 1700 | nM | EC50 | FASEB J (2009) 23: 3619-28 [PMID:19525404] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| ChEMBL | Agonist activity at mGlu7 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 4.28 | pEC50 | 53000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu7 receptor in Rat [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| GtoPdb | - | - | 4.28 | pEC50 | 53000 | nM | EC50 | FASEB J (2009) 23: 3619-28 [PMID:19525404] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as [3H]inositol phosphate accumulation after 30 mins by scintillation and luminescence counting method | F | 4.18 | pEC50 | 66000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| ChEMBL | Agonist activity at mGlu8 (unknown origin) expressed in HEK293 cells coexpressing chimeric Gq/i protein assessed as increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay | F | 4.71 | pEC50 | 19400 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
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]
