AZD6538 [Ligand Id: 6440] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2164552 (AZD-6538) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
