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 |
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| 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 35:
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]
