[3H]AP4 [Ligand Id: 1412] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL33567 |
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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 | Activation of human metabotropic glutamate 4 receptor expressed in golden hamster AV12-664 cells | B | 6.51 | pEC50 | 310 | nM | EC50 | J Med Chem (2018) 61: 10040-10052 [PMID:30365309] |
| 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| ChEMBL | Activation of human metabotropic glutamate 6 receptor expressed in golden hamster AV12-664 cells | B | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2018) 61: 10040-10052 [PMID:30365309] |
| 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 6.54 | pEC50 | 290 | nM | EC50 | J Med Chem (2018) 61: 1969-1989 [PMID:29397723] |
| ChEMBL | Activation of human metabotropic glutamate 8 receptor expressed in golden hamster AV12-664 cells | B | 7.22 | pEC50 | 60 | nM | EC50 | J Med Chem (2018) 61: 10040-10052 [PMID:30365309] |
| 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 | F | 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 | F | 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 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]
