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 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]