VU0285683 [Ligand Id: 6398] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2164544
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2012) 22: 6974-6979 [PMID:23046966]
mGlu5 receptor in Rat [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.8 pKi 16 nM Ki Mol Pharmacol (2010) 78: 1105-23 [PMID:20923853]
GtoPdb - - 7.61 pIC50 24.4 nM IC50 Mol Pharmacol (2010) 78: 1105-23 [PMID:20923853]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by IonWorks assay B 4.48 pIC50 >33000 nM IC50 Bioorg Med Chem Lett (2012) 22: 6974-6979 [PMID:23046966]

ChEMBL data shown on this page come from version 36:

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]