ChEMBL ligand: CHEMBL107400 (GC-1, QRX-431, Sobetiroma, Sobetirome)
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]

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	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 34:

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]