fenobam [Ligand Id: 1434] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL239800 (MCN-3377-98, Fenobam)
  • mGlu1 receptor/Metabotropic glutamate receptor 1 in Human [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255]
  • This target only has 1 pki data point
1 CHEMBL239800_lig_chart_1 Metabotropic glutamate receptor 1 Human
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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]
2 CHEMBL239800_lig_chart_2 Metabotropic glutamate receptor 5 HumanRat
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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]
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 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]
GtoPdb - - 7.2 pIC50 - - - J. Pharmacol. Exp. Ther. (2005) 315: 711-21 [PMID:16040814]
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 B 7.44 pIC50 36.3 nM IC50 Bioorg. Med. Chem. (2015) 23: 3040-3058 [PMID:26014480]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424]
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]