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 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]
