resmetirom [Ligand Id: 12026] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3261331 (Mgl-3196, MGL-3196, Resmetirom, VIA-3196) |
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| 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 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] |
| Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
| 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 | 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 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]
