LSP4-2022 [Ligand Id: 6706] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3114673 |
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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 | 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 | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| GtoPdb | - | - | 6.96 | pEC50 | 110 | nM | EC50 | FASEB J (2012) 26: 1682-93 [PMID:22223752] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Agonist activity against rat mGlu4 S160A mutant | B | 4.58 | pEC50 | 26200 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity against rat mGlu4 S160D mutant | B | 4.73 | pEC50 | 18500 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity against rat mGlu4 R60A mutant | B | 5.04 | pEC50 | 9070 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity at rat mGlu4 R258A mutant | B | 5.31 | pEC50 | 4910 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity against wild type rat mGlu4 | F | 6.08 | pEC50 | 833 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. | F | 6.96 | pEC50 | 110 | nM | EC50 | US-9212196-B2. Hypophosphorous acid derivatives having antihyperalgic activity and biological applications thereof (2015) |
| ChEMBL | Agonist activity against rat mGlu4 K74A mutant | B | 7.62 | pEC50 | 24 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
| GtoPdb | - | - | 5.36 | pEC50 | 4400 | nM | EC50 | FASEB J (2012) 26: 1682-93 [PMID:22223752] |
| 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 | 5.38 | pEC50 | 4200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| ChEMBL | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. | F | 5.38 | pEC50 | 4200 | nM | EC50 | US-9212196-B2. Hypophosphorous acid derivatives having antihyperalgic activity and biological applications thereof (2015) |
| mGlu7 receptor in Human [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| GtoPdb | - | - | 4.94 | pEC50 | 11600 | nM | EC50 | FASEB J (2012) 26: 1682-93 [PMID:22223752] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| ChEMBL | Agonist activity at rat mGlu7 N74K mutant | B | 4.33 | pEC50 | 47000 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity at rat mGlu7 N74A mutant | B | 4.49 | pEC50 | 32000 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity at wild type rat mGlu7 | F | 4.67 | pEC50 | 21379.62 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity at wild type rat mGlu7 | F | 4.67 | pEC50 | 21200 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Antagonist activity against LSP4-202-induced rat mGlu7 activation transfected in HEK293 cells co-transfected with chimeric Gqi9 assessed as decrease in LSP4-202 potency by measuring LSP4-202 pEC50 incubated for 24 hrs by IP-one HTRF assay | F | 4.71 | pEC50 | 19498.45 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Agonist activity at rat mGlu7 Q258A mutant | B | 4.74 | pEC50 | 18200 | nM | EC50 | J Med Chem (2024) 67: 11662-11687 [PMID:38691510] |
| ChEMBL | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. | F | 4.94 | pEC50 | 11600 | nM | EC50 | US-9212196-B2. Hypophosphorous acid derivatives having antihyperalgic activity and biological applications thereof (2015) |
| 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 increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay | F | 4.53 | pEC50 | 29200 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579] | ||||||||
| ChEMBL | Pharmacological Assay: Metabotropic glutamate receptors were transiently transfected in HEK293 cells by electroporation as described elsewhere (Brabet I. et al., 1998) and plated in 96-well microplates. The high affinity glutamate transporter EAAC1 was co-transfected with the receptor in order to avoid any influence of glutamate released by the cells in the assay medium. In the experiments carried out by the inventors, Group-III mGluRs were co-transfected with a chimeric G-protein which couples the activation of the receptor to the phospholipase-C (PLC) pathway. Thus receptor activation induces production of inositol phosphate (IP) which in turn induces intracellular Ca2+ release. Receptor activity was then determined by measurement of the IP production or Ca release as already described (Goudet C. et al., PNAS 2004). For intracellular calcium measurements, cells expressing mGluRs were loaded with Ca2+-sensitive fluorescent dye Fluo-4 AM (Invitrogen, Cergy-Pontoise, France) dissolved in Hanks' balanced Salt Solution. | F | 4.53 | pEC50 | 29200 | nM | EC50 | US-9212196-B2. Hypophosphorous acid derivatives having antihyperalgic activity and biological applications thereof (2015) |
ChEMBL data shown on this page come from version 36:
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]
