[3H]fenobam [Ligand Id: 1433] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL239800 (Fenobam, MCN-3377-98)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
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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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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 F 8.17 pKi 6.7 nM Ki Bioorg Med Chem Lett (2010) 20: 4371-4375 [PMID:20615697]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
GtoPdb - - 7.5 pKd - - - J Pharmacol Exp Ther (2005) 315: 711-21 [PMID:16040814]
ChEMBL Displacement of [3H]MPEP from human cloned mGluR5 receptor expressed in CHO-T-Rex cells after 60 mins by liquid scintillation spectrometry B 6.79 pKi 162.2 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]MPEP from human mGlu5 receptor expressed in CHO-TREx cell membranes after 60 mins by liquid scintillation spectrometric analysis B 6.79 pKi 162.2 nM Ki J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
ChEMBL Displacement of MPEP from mGluR5 (unknown origin) after 3 hrs by liquid scintillation counting method B 7.48 pKi 33 nM Ki Bioorg Med Chem (2018) 26: 4797-4803 [PMID:30143366]
ChEMBL Displacement of MPEP from mGluR5 (unknown origin) after 3 hrs by liquid scintillation counting method B 7.5 pKi 31.62 nM Ki Bioorg Med Chem (2018) 26: 4797-4803 [PMID:30143366]
ChEMBL Binding affinity to human mGluR5 B 8.17 pKi 6.76 nM Ki Bioorg Med Chem Lett (2010) 20: 3737-3741 [PMID:20483612]
ChEMBL Inhibition of glutamate-induced calcium influx in human mGluR5d by FLIPR F 6.48 pIC50 330 nM IC50 Bioorg Med Chem Lett (2006) 16: 1142-1145 [PMID:16380255]
ChEMBL Displacement of [3H]MPEP from mGlu5 receptor B 7.21 pIC50 61 nM IC50 Bioorg Med Chem Lett (2007) 17: 1307-1311 [PMID:17196387]
ChEMBL Displacement of [3H]-MPEP from human mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis B 7.29 pIC50 51 nM IC50 Bioorg Med Chem Lett (2016) 26: 1249-1252 [PMID:26774652]
ChEMBL Antagonist activity at human mGluR5 expressed in CHO-K1 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization F 7.37 pIC50 43 nM IC50 ACS Med Chem Lett (2011) 2: 882-884 [PMID:22523618]
ChEMBL Antagonist activity at mGluR5 by FLIPR F 7.42 pIC50 38 nM IC50 Bioorg Med Chem Lett (2007) 17: 1307-1311 [PMID:17196387]
ChEMBL Negative allosteric modulatory activity at human cloned mGluR5 receptor expressed in CHO-T-Rex cells assessed as inhibiton of quisqualate-induced calcium mobilization treated 10 mins prior to agonist application by fluorescence analysis F 7.44 pIC50 36.3 nM IC50 Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Negative allosteric modulation of human mGlu5 receptor expressed in CHO-TREx cell membranes assessed as reduction in quisqualate-induced Ca2+ mobilization incubated for 18 hrs and measured every 1.5 secs intervals for 60 secs by Fluo-4/AM dye-based fluorescence analysis F 7.44 pIC50 36.3 nM IC50 J Med Chem (2019) 62: 1246-1273 [PMID:30624919]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
GtoPdb - - 7.3 pKd - - - J Pharmacol Exp Ther (2005) 315: 711-21 [PMID:16040814]
ChEMBL Displacement of [3H]MPEP from mGluR5 receptor in Sprague-Dawley rat forebrain membrane after 60 mins by liquid scintillation spectrometry B 6.5 pKi 312.7 nM Ki Bioorg Med Chem (2015) 23: 3040-3058 [PMID:26014480]
ChEMBL Displacement of [3H]MPEP from mGluR5d in rat brain membrane B 6.34 pIC50 460 nM IC50 Bioorg Med Chem Lett (2006) 16: 1142-1145 [PMID:16380255]
ChEMBL Displacement of [3H]-MPEP from rat mGlu5 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting analysis B 7.29 pIC50 51 nM IC50 Bioorg Med Chem Lett (2016) 26: 1249-1252 [PMID:26774652]

ChEMBL data shown on this page come from version 32:

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]