compound 11s [PMID: 19433355] [Ligand Id: 6215] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1783876
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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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 expressed in CHO-K1 cells by whole cell patch-clamp assay B 4.51 pIC50 31000 nM IC50 Eur J Med Chem (2014) 85: 629-637 [PMID:25127154]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Antagonist activity at mGluR1 (unknown origin) expressed in Chem-3 cells assessed as inhibition of glutamate-induced increased intracellular calcium ion level after 18 hrs by fluorescence-based FDSS6000 assay F 8.17 pIC50 6.7 nM IC50 Eur J Med Chem (2014) 85: 629-637 [PMID:25127154]
ChEMBL Antagonist activity at human mGluR1 F 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]
GtoPdb - - 8.68 pIC50 2.1 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-203 [PMID:19433355]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
GtoPdb - - 8.33 pKi 4.7 nM Ki Bioorg Med Chem Lett (2009) 19: 3199-203 [PMID:19433355]
ChEMBL Antagonist activity at rat mGluR1 F 8.46 pKi 3.5 nM Ki Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Antagonist activity at human mGluR5 F 5.52 pIC50 >3000 nM IC50 Bioorg Med Chem Lett (2009) 19: 3199-3203 [PMID:19433355]

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]