KB-130015 [Ligand Id: 7659] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL157885
  • Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
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  • Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
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  • Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
ChEMBL Concentration required to inhibit 50% of binding of [125I]-T3 to human Thyroid hormone receptor alpha-1 in CHO-K1 cells B 5.35 pIC50 4500 nM IC50 J Med Chem (2002) 45: 623-630 [PMID:11806713]
ChEMBL Inhibitory activity against human Thyroid hormone receptor alpha B 5.35 pIC50 4500 nM IC50 J Med Chem (2005) 48: 3114-3117 [PMID:15857115]
ChEMBL Inhibitory activity against human TRAFalpha B 5.66 pIC50 2200 nM IC50 J Med Chem (2005) 48: 3114-3117 [PMID:15857115]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL Inhibition of human thyroid hormone receptor beta 1 B 5.29 pIC50 5128.61 nM IC50 Bioorg Med Chem (2007) 15: 5251-5261 [PMID:17524652]
ChEMBL Concentration required to inhibit 50% of binding of [125I]T3 to human Thyroid hormone receptor beta 1 in CHO-K1 cells B 5.29 pIC50 5100 nM IC50 J Med Chem (2002) 45: 623-630 [PMID:11806713]
ChEMBL Inhibitory activity against human Thyroid hormone receptor beta B 5.29 pIC50 5100 nM IC50 J Med Chem (2005) 48: 3114-3117 [PMID:15857115]
ChEMBL Inhibitory activity against human TRAFbeta B 5.39 pIC50 4100 nM IC50 J Med Chem (2005) 48: 3114-3117 [PMID:15857115]
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809]
GtoPdb - - 4.9 pEC50 - - - Eur J Pharmacol (2010) 632: 52-9 [PMID:20097192]

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]