MK-5435 [Ligand Id: 6335] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL579062
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 1pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat0246810Highcharts.com
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • mGlu8 receptor/Metabotropic glutamate receptor 8 in Human [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 8pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Antagonist activity at human mGluR1 receptor quisqualic acid binding site expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5310-5313 [PMID:19692242]
GtoPdb - - 8.37 pIC50 4.3 nM IC50 Synapse (2011) 65: 125-35 [PMID:20524178]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4477] [GtoPdb: 289] [UniProtKB: P23385]
ChEMBL Antagonist activity at rat mGluR1 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR F 8.44 pIC50 3.6 nM IC50 Bioorg Med Chem Lett (2009) 19: 5310-5313 [PMID:19692242]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Antagonist activity at human mGluR2 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5310-5313 [PMID:19692242]
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222]
ChEMBL Antagonist activity at human mGluR8 receptor expressed in CHO cell membranes assessed as inhibition of L-glutamate-induced calcium mobilization by FLIPR F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2009) 19: 5310-5313 [PMID:19692242]

ChEMBL data shown on this page come from version 35:

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]