compound 16m [PMID: 19931453] [Ligand Id: 6429] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL593590
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  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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  • mGlu2 receptor/Metabotropic glutamate receptor 2 in Human [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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  • mGlu7 receptor/Metabotropic glutamate receptor 7 in Human [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7]
ChEMBL Displacement of radioligand from glutamate and glycine binding site of NMDA receptor in rat brain membrane B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
ChEMBL Inhibition of human mGluR1 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416]
ChEMBL Inhibition of human mGluR2 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
GtoPdb - - 7.42 pKi 38 nM Ki Bioorg Med Chem Lett (2010) 20: 184-8 [PMID:19931453]
ChEMBL Displacement of [3H]ABP688 from human recombinant mGluR5 expressed in CHO cells B 7.42 pKi 38 nM Ki Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
ChEMBL Antagonist activity at human mGluR5 assessed as inhibition of quisqualate-induced intracellular inositol phosphate accumulation F 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
GtoPdb - - 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-8 [PMID:19931453]
ChEMBL Antagonist activity at human mGluR5 assessed as inhibition of glutamate-induced elevation of intracellular calcium concentration F 7.49 pIC50 32 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
ChEMBL Displacement of [3H]ABP688 from mGluR5 in rat brain cortex B 7.52 pKi 30 nM Ki Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]
mGlu7 receptor/Metabotropic glutamate receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3777] [GtoPdb: 295] [UniProtKB: Q14831]
ChEMBL Inhibition of human mGluR7 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2010) 20: 184-188 [PMID:19931453]

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]