[3H]AP4 [Ligand Id: 1412] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL33567 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 34:
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]
