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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]