Ro64-5229 [Ligand Id: 3955] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL305406 (Ro-645229)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 1pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 2pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • mGlu3 receptor/Metabotropic glutamate receptor 3 in Human [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 3pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • mGlu4 receptor/Metabotropic glutamate receptor 4 in Human [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 4pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
Created with Highcharts 10.3.3ValuesChart context menuMetabotropic glutamate receptor 5pKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.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 Agonist potency against cloned human metabotropic glutamate receptor 1 F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Antagonist potency against cloned Metabotropic glutamate receptor 2 F 6.96 pKi 110 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
ChEMBL Non-competitive antagonist activity at human recombinant mGluR2 expressed in Chem-1 cell membrane assessed as inhibition of L-glutamate-induced [35S]GTPgammaS binding after 30 mins by liquid scintillation counting analysis F 6.27 pIC50 533 nM IC50 Medchemcomm (2013) 4: 1118-1123
mGlu2 receptor/Metabotropic glutamate receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2851] [GtoPdb: 290] [UniProtKB: P31421]
ChEMBL Inhibition of [3H]-DCG IV binding on rat mGluR2 transfected cell membranes from CHO cells B 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (1999) 9: 2173-2176 [PMID:10465539]
ChEMBL Inhibition of 10 uM 1S, 3R-ACPD stimulated GTP gamma 35S binding to rat mGluR2 expressed in CHO cells B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (1999) 9: 2173-2176 [PMID:10465539]
GtoPdb - - 7 pIC50 110 nM IC50 Bioorg Med Chem Lett (1999) 9: 2173-6 [PMID:10465539]
mGlu3 receptor/Metabotropic glutamate receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2888] [GtoPdb: 291] [UniProtKB: Q14832]
ChEMBL Agonist potency against cloned Metabotropic glutamate receptor 3 (mGluR-3). F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833]
ChEMBL Agonist potency against cloned human Metabotropic glutamate receptor 4 (mGluR-4) F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
ChEMBL Agonist potency against cloned metabotropic glutamate receptor 5 F 4 pKi >100000 nM Ki J Med Chem (2000) 43: 2609-2645 [PMID:10893301]

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]