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

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ChEMBL ligand: CHEMBL239800 (Fenobam anhydrous, NPL-2009, NPL2009)
  • Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • 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
Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
ChEMBL Inhibition of FTO (unknown origin) demethylation activity using m6A7-Broccoli RNA as substrate incubated for 3 mins under shaking condition and measured after 2 hrs by fluorescence based analysis B 5.48 pIC50 3310 nM IC50 J Med Chem (2021) 64: 16974-17003 [PMID:34792334]
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate B 6.17 pIC50 678.2 nM IC50 HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators
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 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]