LY341495 [Ligand Id: 1378] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL432038 (LY-341495)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
  • 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 Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • 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 Rat [ChEMBL: CHEMBL3842] [GtoPdb: 294] [UniProtKB: P35349]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Rat [ChEMBL: CHEMBL3879] [GtoPdb: 295] [UniProtKB: P35400]
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  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
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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]
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 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 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]
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]
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 28:

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]