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ChEMBL ligand: CHEMBL107400 (QRX-431, Sobetirome, GC-1) |
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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. U.S.A. (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 27:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]