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] |
| 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 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 data shown on this page come from version 33:
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]
