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ChEMBL ligand: CHEMBL41036 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] | ||||||||
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay | B | 8.11 | pKi | 7.79 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
ChEMBL | Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay | B | 8.14 | pKi | 7.18 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314] |
ChEMBL | Binding affinity to TRalpha1 | B | 8.14 | pKi | 7.18 | nM | Ki | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Inhibition of thyroid hormone receptor alpha | B | 7.6 | pIC50 | 25.12 | nM | IC50 | Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994] |
GtoPdb | - | - | 7.6 | pIC50 | - | - | - | J Med Chem (2003) 46: 1580-8 [PMID:12699376] |
ChEMBL | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor alpha) was determined | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Inhibitory concentration against cloned human thyroid hormone receptor alpha 1 | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653] |
ChEMBL | Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524] |
ChEMBL | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined | B | 7.96 | pEC50 | 11 | nM | EC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
ChEMBL | Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay | F | 8.35 | pEC50 | 4.5 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912] |
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
ChEMBL | Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay | B | 9.43 | pKi | 0.37 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314] |
ChEMBL | Binding affinity to TRbeta1 | B | 9.43 | pKi | 0.37 | nM | Ki | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay | B | 9.62 | pKi | 0.24 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
ChEMBL | Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined | B | 8.96 | pIC50 | 1.1 | nM | IC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Inhibitory concentration against cloned human thyroid hormone receptor beta 1 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653] |
ChEMBL | Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524] |
GtoPdb | - | - | 8.96 | pIC50 | - | - | - | Proc Natl Acad Sci USA (2003) 100: 10067-72 [PMID:12888625] |
ChEMBL | Inhibition of human thyroid hormone receptor beta 1 | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2007) 15: 5251-5261 [PMID:17524652] |
ChEMBL | Inhibition of thyroid hormone receptor beta | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994] |
ChEMBL | Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay | B | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
ChEMBL | Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined | B | 8.46 | pEC50 | 3.5 | nM | EC50 | J Med Chem (2003) 46: 1580-1588 [PMID:12699376] |
ChEMBL | Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay | F | 8.95 | pEC50 | 1.12 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912] |
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]