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ChEMBL ligand: CHEMBL239800 (Fenobam, MCN-3377-98) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]