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 | Antagonist activity at mGluR7 (unknown origin) assessed as inhibition of L-AP4 stimulated decrease in forskolin induced cAMP response by CRE-Luc assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | ACS Med Chem Lett (2023) 14: 442-449 [PMID:37077399] |
| 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 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]
