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ChEMBL ligand: CHEMBL107400 (GC-1, QRX-431, Sobetirome) |
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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 | Binding affinity to human TRalpha1 | B | 8.6 | pKd | 2.5 | nM | Kd | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Binding affinity against human Thyroid hormone receptor alpha-1 (hTRalpha1) using radiolabeled T3 | B | 8.74 | pKd | 1.8 | nM | Kd | J Med Chem (2002) 45: 3310-3320 [PMID:12109914] |
ChEMBL | Binding affinity of compound was determined against Thyroid hormone receptor alpha1 | B | 9.18 | pKd | 0.66 | nM | Kd | J Med Chem (2003) 46: 3152-3161 [PMID:12825953] |
GtoPdb | - | - | 9.36 | pKd | - | - | - | Mol Endocrinol (1990) 4: 227-34 [PMID:2158622] |
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay | B | 8.96 | pKi | 1.09 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
ChEMBL | Half-maximum activation of human Thyroid hormone receptor alpha-1 (hTRalpha1) | B | 7.35 | pEC50 | 45 | nM | EC50 | J Med Chem (2002) 45: 3310-3320 [PMID:12109914] |
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 | 8.52 | pEC50 | 3 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
ChEMBL | Binding affinity to human TRbeta1 | B | 9.7 | pKd | 0.2 | nM | Kd | J Med Chem (2012) 55: 5649-5675 [PMID:22512468] |
ChEMBL | Binding affinity against human Thyroid hormone receptor beta 1 (hTRbeta1) using radiolabeled T3 | B | 10 | pKd | 0.1 | nM | Kd | J Med Chem (2002) 45: 3310-3320 [PMID:12109914] |
ChEMBL | Binding affinity of compound was determined against thyroid hormone receptor beta 1 | B | 10 | pKd | 0.1 | nM | Kd | J Med Chem (2003) 46: 3152-3161 [PMID:12825953] |
GtoPdb | - | - | 10.17 | pKd | - | - | - |
Proc Natl Acad Sci USA (1977) 74: 3365-9 [PMID:269396]; Chem Biol (1998) 5: 299-306 [PMID:9653548] |
ChEMBL | Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2008) 51: 7075-7093 [PMID:18975928] |
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 | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2014) 57: 3912-3923 [PMID:24712661] |
ChEMBL | Half-maximum activation of human Thyroid hormone receptor beta 1 (hTRbeta1) | B | 8.15 | pEC50 | 7 | nM | EC50 | J Med Chem (2002) 45: 3310-3320 [PMID:12109914] |
ChEMBL data shown on this page come from version 32:
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]