TMP-301 [Ligand Id: 14266] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3603923
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  • mGlu5 receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5.5 pIC50 >3162.28 nM IC50 J Med Chem (2015) 58: 6653-6664 [PMID:26225459]
mGlu5 receptor/Metabotropic glutamate receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3227] [GtoPdb: 293] [UniProtKB: P41594]
GtoPdb Determined in a [3H]-M-MPEP competition radioligand binding assay - 9.27 pKi 0.54 nM Ki WO2015008073A1. 4-(3-cyanophenyl)-6-pyridinylpyrimidine mglu5 modulators (2015)
ChEMBL Displacement of [3H]-M-MPEP from human mGlu5 receptor expressed in HEK293 cells after 90 mins by scintillation spectroscopy analysis B 9.3 pKi 0.5 nM Ki J Med Chem (2015) 58: 6653-6664 [PMID:26225459]
ChEMBL Negative allosteric modulation at human mGlu5 receptor expressed in HEK293 cells assessed as inhibition of L-quisqualic acid-induced inositol phosphate turnover preincubated for 45 mins before L-quisqualic acid challenge measured after 15 mins by IPone assay F 9.2 pIC50 0.63 nM IC50 J Med Chem (2015) 58: 6653-6664 [PMID:26225459]
ChEMBL Inhibition of mGLU5 (unknown origin) B 9.3 pIC50 0.5 nM IC50 J Med Chem (2019) 62: 3036-3050 [PMID:30807144]

ChEMBL data shown on this page come from version 35:

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]