ChEMBL ligand: CHEMBL3261331 (Mgl-3196, MGL-3196, Resmetirom, Rezdiffra, VIA-3196)
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] There should be some charts here, you may need to enable JavaScript!
Thyroid hormone receptor-β/Thyroid hormone receptor beta in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] There should be some charts here, you may need to enable JavaScript!

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	Agonist activity at THR-alpha in HEK293T cells incubated for 18 to 24 hrs by EnSpire plate reader analysis	B	5.23	pEC50	5930	nM	EC50	J Med Chem (2024) 67: 14840-14851 [PMID:39221768]
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	5.43	pEC50	3740	nM	EC50	J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
GtoPdb	Determined in acell free coactivator recruitment assay	-	5.43	pEC50	3740	nM	EC50	J Med Chem (2014) 57: 3912-23 [PMID:24712661]
ChEMBL	Agonist activity at human THRalpha transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay	B	5.55	pEC50	2850	nM	EC50	J Med Chem (2023) 66: 3284-3300 [PMID:36799411]
ChEMBL	Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay	B	5.56	pEC50	2735	nM	EC50	J Med Chem (2022) 65: 7193-7211 [PMID:35507418]
ChEMBL	Agonist activity at full length GST-tagged human THR-alpha LBD incubated for 1 hr in presence of fluorescein labeled SRC2-2 peptide by Lanthascreen TR-FRET assay	B	6.03	pEC50	934	nM	EC50	J Med Chem (2024) 67: 14840-14851 [PMID:39221768]
Thyroid hormone receptor-β/Thyroid hormone receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL	Agonist activity at THR-beta in HEK293T cells incubated for 18 to 24 hrs by EnSpire plate reader analysis	B	5.63	pEC50	2370	nM	EC50	J Med Chem (2024) 67: 14840-14851 [PMID:39221768]
ChEMBL	Agonist activity at human THRbeta transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay	B	6	pEC50	990	nM	EC50	J Med Chem (2023) 66: 3284-3300 [PMID:36799411]
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	6.68	pEC50	210	nM	EC50	J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
GtoPdb	Determined in a cell free coactivator recruitment assay	-	6.68	pEC50	210	nM	EC50	J Med Chem (2014) 57: 3912-23 [PMID:24712661]
ChEMBL	Affinity On-target Cellular interaction: (Reporter gene assay (HEK293T cells)) EUB0001081a THRB	F	6.7	pEC50	200	nM	EC50	Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL	Agonist activity at human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay	B	6.78	pEC50	167.1	nM	EC50	J Med Chem (2022) 65: 7193-7211 [PMID:35507418]
ChEMBL	Agonist activity at full length GST-tagged human THR-beta LBD incubated for 1 hr in presence of fluorescein labeled SRC2-2 peptide by Lanthascreen TR-FRET assay	B	7.14	pEC50	73	nM	EC50	J Med Chem (2024) 67: 14840-14851 [PMID:39221768]

ChEMBL data shown on this page come from version 36:

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]