AZD6538 [Ligand Id: 6440] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2164552 (AZD-6538)
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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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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 by IonWorks assay B 5.2 pIC50 6350 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
GtoPdb - - 7.55 pKi 28 nM Ki Bioorg Med Chem Lett (2012) 22: 6974-9 [PMID:23046966]
ChEMBL Displacement of [3H]MPEP from human mGluR5 expressed in HEK293 cell membranes expressing GLAST after 1 hr by scintillation counter B 7.55 pKi 28 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
ChEMBL Displacement of [3H]AZD9272 from human mGluR5 expressed in HEK293 cell membranes expressing GLAST after 1 hr by scintillation counter B 7.75 pKi 17.9 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
ChEMBL Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of glutamate-stimulated IP accumulation incubated for 10 mins prior to glutamate challenge measured 30 mins post glutamate challenge by scintillation counter in presence of [3H]myo-inositol F 7.29 pIC50 51 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
GtoPdb - - 7.87 pIC50 13.4 nM IC50 Bioorg Med Chem Lett (2012) 22: 6974-9 [PMID:23046966]
ChEMBL Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay F 7.87 pIC50 13.4 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Displacement of [3H]AZD9272 from mGluR5 in Sprague-Dawley rat striatum by autoradiographic analysis B 7.84 pIC50 14.5 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]
ChEMBL Negative allosteric modulation of rat recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay F 8.49 pIC50 3.2 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6974-6979 [PMID:23046966]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]