compound 22a [PMID: 21688779] [Ligand Id: 6231] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1830707
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
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  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.55 pIC50 28000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Negative allosteric modulation of mGlu1 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
ChEMBL Positive allosteric modulation of mGlu1 receptor assessed as potentiation of glutamate-induced calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Negative allosteric modulation of mGlu2 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
ChEMBL Positive allosteric modulation of mGlu2 receptor assessed as potentiation of glutamate-induced calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Negative allosteric modulation of mGlu3 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
ChEMBL Positive allosteric modulation of mGlu3 receptor assessed as potentiation of glutamate-induced calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
ChEMBL Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay F 8.05 pEC50 9 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
GtoPdb - - 8.1 pEC50 9 nM EC50 J Med Chem (2011) 54: 5070-81 [PMID:21688779]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Negative allosteric modulation of mGlu5 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
ChEMBL Positive allosteric modulation of mGlu5 receptor assessed as potentiation of glutamate-induced calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
ChEMBL Negative allosteric modulation of mGlu7 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]
ChEMBL Positive allosteric modulation of mGlu7 receptor assessed as potentiation of glutamate-induced calcium mobilization F 5 pEC50 >10000 nM EC50 J Med Chem (2011) 54: 5070-5081 [PMID:21688779]

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]