[3H]AP4 [Ligand Id: 1412] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL33567
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Human [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
  • mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743]
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Metabotropic glutamate receptor 1 agonist activity as basal [3H]- IP formation in rat F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422]
ChEMBL Metabotropic glutamate receptor 3 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
ChEMBL Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) F 6.04 pKi 910 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Binding affinity at Metabotropic glutamate receptor 4 B 6.33 pKi 470 nM Ki J. Med. Chem. (2002) 45: 3171-3183 [PMID:12109902]
ChEMBL Displacement of [3H]Quisqualate from human mGluR4 receptor expressed in BHK cells B 6.8 pKi 160 nM Ki Bioorg. Med. Chem. (2009) 17: 242-250 [PMID:19042134]
ChEMBL Agonist activity at mGlu4 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production F 6.16 pEC50 690 nM EC50 J. Med. Chem. (2007) 50: 3585-3595 [PMID:17602546]
ChEMBL Agonistic activity at Metabotropic glutamate receptor 4 expressed in mammalian cells by GTPgammaS binding assay B 6.3 pEC50 500 nM EC50 Bioorg. Med. Chem. Lett. (2000) 10: 1447-1450 [PMID:10888329]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR4a in human B 6.7 pEC50 200 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
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 B 6.89 pEC50 130 nM EC50 J Med Chem (2018) 61: 1969-1989 [PMID:29397723]
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 B 7 pEC50 100 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]
GtoPdb - - 6.3 pKd - - - J. Biol. Chem. (1999) 274: 10008-13 [PMID:10187777]
ChEMBL Displacement of [3H]L-AP4 from rat mGluR4 expressed in BHK cells B 6.8 pKi 160 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 196-199 [PMID:16213710]
ChEMBL Displacement of [3H]L-AP4 from rat recombinant mGluR4 expressed in BHK cells by SPA assay B 6.8 pKi 160 nM Ki Bioorg. Med. Chem. (2007) 15: 3161-3170 [PMID:17350267]
ChEMBL Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Active F 4 pEC50 <100000 nM EC50 J. Med. Chem. (2005) 48: 2534-2547 [PMID:15801843]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat B 5.92 pEC50 1200 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Effect on Metabotropic glutamate receptor 4 B 6.04 pEC50 910 nM EC50 J. Med. Chem. (1997) 40: 3700-3705 [PMID:9357538]
ChEMBL Functional activity at rat mGluR4 F 6.29 pEC50 510 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 196-199 [PMID:16213710]
ChEMBL Agonist activity at rat recombinant mGluR4 expressed in BHK cells F 6.29 pEC50 510 nM EC50 Bioorg. Med. Chem. (2007) 15: 3161-3170 [PMID:17350267]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR4a in rat B 6.3 pEC50 500 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Stimulation od [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells F 6.49 pEC50 320 nM EC50 J. Med. Chem. (2005) 48: 2534-2547 [PMID:15801843]
ChEMBL Metabotropic glutamate receptor 4 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 6.49 pEC50 320 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
ChEMBL Effective concentration against Metabotropic glutamate receptor 4 B 6.7 pEC50 200 nM EC50 J. Med. Chem. (2005) 48: 2534-2547 [PMID:15801843]
ChEMBL Agonist activity at rat mGlu4 receptor expressed in HEK293 cells coexpressing Gq/Gi and EAAC1 assessed as intracellular calcium production measured every 1.5 secs for 60 secs by Fluo-4-AM based fluorometry F 6.89 pEC50 130 nM EC50 Bioorg. Med. Chem. (2012) 20: 4716-4726 [PMID:22750138]
ChEMBL Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader F 6.89 pEC50 130 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Agonist activity at rat mGlu4 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting F 7.02 pEC50 96 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Agonist activity at rat mGluR4 receptor expressed HEK293 cells assessed as effect on inositol phosphate production F 7.1 pEC50 80 nM EC50 J. Med. Chem. (2007) 50: 4656-4664 [PMID:17722902]
ChEMBL Agonist activity at rat mGluR4 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay B 7.52 pEC50 30 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2523-2526 [PMID:25958247]
ChEMBL Agonist activity at rat mGlu4 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay B 7.52 pEC50 30 nM EC50 J. Med. Chem. (2016) 59: 914-924 [PMID:26814576]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Metabotropic glutamate receptor 5 agonist activity as basal [3H]- IP formation in rat F 4 pEC50 >100000 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 6 (mGluR-6). F 6.05 pKi 900 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
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 B 5.62 pEC50 2400 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 increase in intracellular calcium accumulation by Fluo-4 AM dye based fluorescence assay B 6 pEC50 1000 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 Agonist activity at rat mGluR6 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay B 5.46 pEC50 3450 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2523-2526 [PMID:25958247]
ChEMBL Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting F 5.48 pEC50 3300 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Agonist activity at rat mGluR6 receptor expressed HEK293 cells assessed as effect on inositol phosphate production F 5.68 pEC50 2080 nM EC50 J. Med. Chem. (2007) 50: 4656-4664 [PMID:17722902]
ChEMBL Agonist activity at rat mGlu6 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay B 5.72 pEC50 1910 nM EC50 J. Med. Chem. (2016) 59: 914-924 [PMID:26814576]
ChEMBL Agonist activity at rat mGlu6 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader F 6 pEC50 1000 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR6 in rat B 6.05 pEC50 900 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
ChEMBL Effect on Metabotropic glutamate receptor 6 B 6.24 pEC50 570 nM EC50 J. Med. Chem. (1997) 40: 3700-3705 [PMID:9357538]
ChEMBL Activity at rat recombinant mGluR6 expressed in CHO cells assessed as cAMP production B 6.47 pEC50 340 nM EC50 Bioorg. Med. Chem. (2007) 15: 3161-3170 [PMID:17350267]
ChEMBL Activity at rat mGluR6 by measuring cAMP formation in CHO cells F 6.47 pEC50 340 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 196-199 [PMID:16213710]
ChEMBL Metabotropic glutamate receptor 6 agonist activity to influence forskolin stimulated c-AMP formation in rat non neuronal cells F 7.26 pEC50 55 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
GtoPdb - - 6.7 pKd - - - Brain Res. Mol. Brain Res. (1999) 67: 201-10 [PMID:10216218]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). F 7.21 pKi 61 nM Ki J. Med. Chem. (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Agonist activity at mGlu8 receptor expressed in HEK 293 cells assessed as effect on inositol phosphate production F 6.25 pEC50 560 nM EC50 J. Med. Chem. (2007) 50: 3585-3595 [PMID:17602546]
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 B 6.54 pEC50 290 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 B 6.54 pEC50 290 nM EC50 J Med Chem (2018) 61: 1969-1989 [PMID:29397723]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4626] [GtoPdb: 296] [UniProtKB: P47743]
ChEMBL Concentration for half maximal activation of metabotropic glutamate mGluR8 in mouse B 6.4 pEC50 400 nM EC50 J. Med. Chem. (1995) 38: 1417-1426 [PMID:7738999]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2718] [GtoPdb: 296] [UniProtKB: P70579]
ChEMBL Displacement of [3H]LY341495 from rat mGluR8 expressed in BHK cells B 5.72 pKi 1900 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 196-199 [PMID:16213710]
ChEMBL Displacement of [3H]LY341495 from rat recombinant mGluR8 expressed in BHK cells by SPA assay B 5.72 pKi 1900 nM Ki Bioorg. Med. Chem. (2007) 15: 3161-3170 [PMID:17350267]
ChEMBL Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular calcium level after 1 hr by fluorescence microplate reader F 6.52 pEC50 300 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Agonist activity at rat mGlu8 receptor expressed in HEK293 cells co-transfected with G-protein alpha and EAAC1 assessed as increase in intracellular inositol phosphate accumulation after 1 hr by scintillation counting F 6.62 pEC50 240 nM EC50 J. Med. Chem. (2010) 53: 2797-2813 [PMID:20218620]
ChEMBL Agonist activity at rat mGluR8 receptor expressed HEK293 cells assessed as effect on inositol phosphate production F 6.89 pEC50 128 nM EC50 J. Med. Chem. (2007) 50: 4656-4664 [PMID:17722902]
ChEMBL Agonist activity at rat mGluR8 expressed in HEK293 cells assessed as induction of inositol phosphate production by HTRF assay B 6.96 pEC50 110 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2523-2526 [PMID:25958247]
ChEMBL Agonist activity at rat mGlu8 receptor expressed in HEK293 cells assessed as IP1 accumulation by IP-One functional assay B 7.15 pEC50 70 nM EC50 J. Med. Chem. (2016) 59: 914-924 [PMID:26814576]
ChEMBL Metabotropic glutamate receptor 8 agonist activity against forskolin stimulated c-AMP formation in rat non neuronal cells F 7.22 pEC50 60 nM EC50 J. Med. Chem. (2004) 47: 456-466 [PMID:14711315]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]