LY341495 [Ligand Id: 1378] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL432038 (LY-341495) |
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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 Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
| ChEMBL | Agonist potency against cloned human metabotropic glutamate receptor 1 | F | 5.17 | pKi | 6800 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | Neuropharmacology (1998) 37: 1-12 [PMID:9680254] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 1 (mGluR1) was evaluated | F | 5.11 | pIC50 | 7800 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 1 activity of rat expressed in CHO cells | B | 5.05 | pIC50 | 8990 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 1 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
| ChEMBL | Antagonist potency against cloned Metabotropic glutamate receptor 2 | F | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]-LY459477 from recombinant human mGlu2 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Antagonistic activity against stimulation of GTP (gamma) 35 S binding by glutamate in membranes from CHO cells expressing human mGluR2 | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 3179-3182 [PMID:11720869] |
| ChEMBL | Antagonist activity at human recombinant mGlu2 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay | F | 7.57 | pIC50 | 26.7 | nM | IC50 | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| ChEMBL | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 2 | F | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (1998) 41: 358-378 [PMID:9464367] |
| ChEMBL | Antagonist activity at human mGLUR2 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP | F | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| ChEMBL | Antagonist activity at human recombinant mGlu2 receptor stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay | F | 8.11 | pIC50 | 7.8 | nM | IC50 | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| ChEMBL | Displacement of [3H]-MGS0008 from mGluR2 expressed in CHO cells | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem (2008) 16: 4359-4366 [PMID:18348906] |
| mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421] | ||||||||
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 8.5 | pKi | 3.13 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| GtoPdb | - | - | 9 | pKi | - | - | - |
Br J Pharmacol (1998) 123: 497-504 [PMID:9504391]; Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 2 (mGluR2) was evaluated | F | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 2 activity of rat expressed in CHO cells | B | 7.63 | pIC50 | 23.2 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 2 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). | F | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Displacement of [3H]-LY459477 from recombinant human mGlu3 receptor expressed in hamster AV12 cell membranes co-expressing rat EAAT1 incubated for 90 mins by top count scintillation method | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - | Neuropharmacology (1999) 38: 1519-29 [PMID:10530814] |
| ChEMBL | Antagonist activity at human mGLUR3 expressed in RGT cells assessed as inhibition of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP | F | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1958-1962 [PMID:22318160] |
| ChEMBL | Effect on 1S,3R-ACPD-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells expressing human Metabotropic glutamate receptor 3 | F | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1998) 41: 358-378 [PMID:9464367] |
| ChEMBL | Antagonist activity at human recombinant mGlu3 receptor stably expressed in golden hamster AV12 cells co-expressing rat EAAT1 assessed as reduction in DCG IV-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by incubation with cAMP-d2 conjugate and anti-cAMP cryptate for 1 hr by HTRF assay | F | 8.11 | pIC50 | 7.7 | nM | IC50 | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| ChEMBL | Antagonist activity at human recombinant mGlu3 stably expressed in golden hamster AV12 cell membrane co-expressing Galpha15 assessed as assessed as reduction in glutamate-induced calcium influx incubated for 90 to 120 min by Fluo-4-AM dye based FLIPR assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2016) 59: 10974-10993 [PMID:28002967] |
| mGlu3 receptor/Metabotropic glutamate receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3067] [GtoPdb: 291] [UniProtKB: P31422] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | Neuropharmacology (2000) 39: 1700-6 [PMID:10884552] |
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 8.52 | pKi | 3.04 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]glutamate against rat recombinant mGluR3 receptors expressed in HEK293 cells | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 3179-3182 [PMID:11720869] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 3 (mGluR3) was evaluated | F | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 3 activity of rat expressed in CHO cells | B | 7.85 | pIC50 | 14.2 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 3 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| 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 | 4.66 | pKi | 22000 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 4 (mGluR4) was evaluated | F | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| GtoPdb | - | - | 4.7 | pIC50 | - | - | - | Neuropharmacology (1995) 34: 887-94 [PMID:8532170] |
| mGlu4 receptor/Metabotropic glutamate receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2787] [GtoPdb: 292] [UniProtKB: P31423] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 4 activity of rat expressed in CHO cells | B | 5.58 | pIC50 | 2650 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594] | ||||||||
| ChEMBL | Agonist potency against cloned metabotropic glutamate receptor 5 | F | 5.09 | pKi | 8200 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 5 (mGluR5) was evaluated | F | 5.09 | pIC50 | 8200 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| GtoPdb | - | - | 5.1 | pIC50 | - | - | - | Neuropharmacology (1998) 37: 1-12 [PMID:9680254] |
| mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 5 activity of rat expressed in CHO cells | B | 4.94 | pIC50 | 11400 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 5 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu6 receptor/Metabotropic glutamate receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349] | ||||||||
| ChEMBL | Concentration required to inhibit metabotropic glutamate receptor 6 activity of rat expressed in CHO cells | B | 5.94 | pIC50 | 1140 | nM | IC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| ChEMBL | Effective concentration for agonistic activity towards metabotropic glutamate receptor 6 of rat expressed in CHO cells | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 7 (mGluR-7). | F | 6 | pKi | 990 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2000) 362: 546-54 [PMID:11138847] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 7 (mGluR7) was evaluated | F | 6 | pIC50 | 990 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400] | ||||||||
| ChEMBL | Binding affinity towards metabotropic glutamate receptor 7 of rat expressed in CHO cells was determined by using [3H]MGS-0008 | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (2004) 47: 4570-4587 [PMID:15317467] |
| mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
| ChEMBL | Agonist potency against cloned Metabotropic glutamate receptor 8 (mGluR-8). | F | 6.77 | pKi | 170 | nM | Ki | J Med Chem (2000) 43: 2609-2645 [PMID:10893301] |
| ChEMBL | Antagonistic activity against metabotropic glutamate receptor 8 (mGluR8) was evaluated | F | 6.77 | pIC50 | 170 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 2849-2854 [PMID:9873635] |
| GtoPdb | - | - | 6.8 | pIC50 | - | - | - | Neuropharmacology (1998) 37: 1-12 [PMID:9680254] |
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]
