T4 [Ligand Id: 2635] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1624 (Levothyroxine, NSC-36397)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • Malate dehydrogenase, mitochondrial in Human [ChEMBL: CHEMBL5917] [UniProtKB: P40926]
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  • OATP4C1/Solute carrier organic anion transporter family member 4C1 in Human [ChEMBL: CHEMBL2073690] [GtoPdb: 1227] [UniProtKB: Q6ZQN7]
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  • Thyroid hormone receptor-β in Human [GtoPdb: 589] [UniProtKB: P10828]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay B 5.1 pIC50 7860 nM IC50 Bioorg. Med. Chem. (2013) 21: 4266-4278 [PMID:23688559]
Malate dehydrogenase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5917] [UniProtKB: P40926]
ChEMBL Inhibition of MDH2 (unknown origin) B 4.36 pIC50 43600 nM IC50 J Med Chem (2017) 60: 8631-8646 [PMID:28991459]
Proliferating cell nuclear antigen in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2346488] [UniProtKB: P12004]
ChEMBL Inhibition of human recombinant PCNA interaction with PIP box protein N-5-carboxyfluorescein-SAVLQKKITDYFHPKK after 30 mins by fluorescence polarization assay B 4.3 pIC50 >50000 nM IC50 Bioorg. Med. Chem. (2013) 21: 1972-1977 [PMID:23395113]
OATP4C1/Solute carrier organic anion transporter family member 4C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073690] [GtoPdb: 1227] [UniProtKB: Q6ZQN7]
ChEMBL TP_TRANSPORTER: inhibition of Triiodothyronine uptake in OATP4C1-expressing MDCK cells F 5.1 pIC50 8000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2004) 101: 3569-3574 [PMID:14993604]
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL Inhibition of TTR mediated fibrillogenesis assessed as acid-induced protein aggregation turbidity after 1.5 hrs by turbidimetric assay B 4.98 pIC50 10500 nM IC50 Bioorg. Med. Chem. Lett. (2009) 19: 5270-5273 [PMID:19651509]
ChEMBL Stabilization of recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid beta formation by measuring turbidity preincubated for 30 mins followed by lowering pH from 7.2 to 4.4 measured after 72 hrs by microplate spectrophotometric method B 5.66 pIC50 2200 nM IC50 Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
ChEMBL Stabilization of recombinant human wild type TTR expressed in Escherichia coli BL21 (DE3) assessed as inhibition of amyloid beta formation by measuring turbidity preincubated for 30 mins followed by lowering pH from 7.2 to 4.4 measured after 72 hrs by microplate spectrophotometric method B 5.66 pIC50 2187.76 nM IC50 Eur J Med Chem (2016) 121: 823-840 [PMID:27020050]
Thyroid hormone receptor-β in Human [GtoPdb: 589] [UniProtKB: P10828]
GtoPdb - - 8.52 pIC50 - - - Mol Endocrinol (1990) 4: 227-34 [PMID:2158622]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]