T4 [Ligand Id: 2635] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1624 (Levothyroxin, Levothyroxine, L-thyroxine, NSC-36397, Synthetic levothyroxine, Thyroxine, l-) |
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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] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Binding affinity to recombinant PPARgamma LBD (unknown origin) by isothermal titration calorimetry | B | 6.4 | pKd | 400 | nM | Kd | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| ChEMBL | Agonist activity at recombinant human pFA-CMV fused PPARgamma expressed in HEK293T cells transfected with pFR-luciferase plasmid and pRL-SV40 plasmid incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay | B | 4.92 | pEC50 | 12000 | nM | EC50 | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| 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] |
| Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
| ChEMBL | Binding affinity to RXRalpha LBD (unknown origin) by isothermal titration calorimetry | B | 6.03 | pKd | 930 | nM | Kd | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| ChEMBL | Agonist activity at recombinant human pFA-CMV fused RXRalpha LBD expressed in HEK293T cells transfected with pFR-luciferase plasmid and pRL-SV40 plasmid incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay | B | 4.81 | pEC50 | 15400 | nM | EC50 | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| 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] |
| Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] | ||||||||
| ChEMBL | Agonist activity at THRalpha (unknown origin) incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay | B | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
| GtoPdb | - | - | 8.52 | pIC50 | - | - | - | Mol Endocrinol (1990) 4: 227-34 [PMID:2158622] |
| ChEMBL | Agonist activity at THRbeta (unknown origin) incubated for 14 to 16 hrs by dual glo luciferase reporter gene assay | B | 6.62 | pEC50 | 240 | nM | EC50 | J Med Chem (2020) 63: 6727-6740 [PMID:32356658] |
| 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] |
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]
