triiodothyronine [Ligand Id: 2634] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1544 (3,5,3'-triiodothyronine, l-, Cyronine, Cytomel, Euthroid-0.5, Euthroid-1, Euthroid-2, Euthroid-3, Levothyroxine sodium related compound liothyronine, Liothyronine, NSC-80203, Rathyronine, Rathyronine, (s)-, Tertroxin, Thyrolar-0.25, Thyrolar-0.5, Thyrolar-1, Thyrolar-2, Thyrolar-3, Thyrolar-5, Triiodothyronine (T3 Or Liothyronine, Active) (6-11%), Triostat)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
There should be some charts here, you may need to enable JavaScript!
  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
There should be some charts here, you may need to enable JavaScript!
  • OATP1C1/Solute carrier organic anion transporter family member 1C1 in Mouse [ChEMBL: CHEMBL2073688] [GtoPdb: 1222] [UniProtKB: Q9ERB5]
There should be some charts here, you may need to enable JavaScript!
  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
There should be some charts here, you may need to enable JavaScript!
  • 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-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
  • Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Rat [ChEMBL: CHEMBL3917] [GtoPdb: 589] [UniProtKB: P18113]
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
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 6.62 pKi 239.7 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 6.39 pIC50 410.9 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
ChEMBL Transcriptional activity at human androgen receptor BF3 site stably transfected in eGFP-expressing human LNCAP cells after 5 days by fluorometric analysis B 4.3 pIC50 >50000 nM IC50 J Med Chem (2011) 54: 8563-8573 [PMID:22047606]
GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88]
ChEMBL Direct channel-gating action blocked by picrotoxin B 4.64 pIC50 23000 nM IC50 J Med Chem (2000) 43: 1427-1447 [PMID:10780899]
GABAA receptor π subunit/GABAA receptor β1 subunit/GABAA receptor δ subunit/GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor γ1 subunit/GABAA receptor α2 subunit/GABAA receptor α4 subunit/GABAA receptor γ3 subunit/GABAA receptor α6 subunit/GABAA receptor α1 subunit/GABAA receptor β3 subunit/GABAA receptor β2 subunit/GABAA receptor ε subunit/GABA-A receptor; anion channel in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907607] [GtoPdb: 419, 410, 416, 414, 408, 406, 413, 405, 407, 415, 409, 404, 412, 411, 417] [UniProtKB: O09028, P15431, P18506, P18508, P19969, P20236, P23574, P23576, P28471, P28473, P30191, P62813, P63079, P63138, Q91ZM7, Q9ES14]
ChEMBL Non-competitive inhibitory activity against recombinant Gamma-aminobutyric acid A (GABA-A) receptor B 5.15 pEC50 7000 nM EC50 J Med Chem (2000) 43: 1427-1447 [PMID:10780899]
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 6.15 pKd 710 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 5.24 pEC50 5800 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 5.44 pIC50 3600 nM IC50 Bioorg Med Chem (2013) 21: 1972-1977 [PMID:23395113]
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin uptake in Xenopus laevis oocytes F 4.3 pIC50 50400 nM IC50 J Pharmacol Exp Ther (2001) 299: 261-267 [PMID:11561088]
OATP1C1/Solute carrier organic anion transporter family member 1C1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073688] [GtoPdb: 1222] [UniProtKB: Q9ERB5]
ChEMBL TP_TRANSPORTER: inhibition of L-T4 uptake in Oatp14-expressing HEK293 cells F 4.62 pKi 24200 nM Ki Endocrinology (2004) 145: 4384-4391 [PMID:15166123]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Agonist activity at human THRbeta expressed in CHO cells after 24 hrs by luciferase assay B 8.21 pEC50 6.2 nM EC50 J Med Chem (2020) 63: 6727-6740 [PMID:32356658]
ChEMBL Agonist activity at GST-labelled THRbeta ( 202 to 461 residues) (unknown origin) incubated for 2 hrs in presence SRC1-2 co-activator peptide by Alphascreen assay B 8.92 pEC50 1.2 nM EC50 J Med Chem (2020) 63: 6727-6740 [PMID:32356658]
ChEMBL Agonist activity at human THRbeta expressed in green monkey CV1 cells after 24 hrs by luciferase assay B 8.92 pEC50 1.2 nM EC50 J Med Chem (2020) 63: 6727-6740 [PMID:32356658]
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
ChEMBL Binding affinity towards thyroid hormone receptor (hTR alpha 1) B 9.77 pKd 0.17 nM Kd Bioorg Med Chem Lett (2001) 11: 2821-2825 [PMID:11597408]
GtoPdb - - 10 pKd - - - J Med Chem (2002) 45: 3310-20 [PMID:12109914]
ChEMBL Binding affinity against human Thyroid hormone receptor alpha-1 (hTRalpha1) using radiolabeled T3 B 10 pKd 0.1 nM Kd J Med Chem (2002) 45: 3310-3320 [PMID:12109914]
ChEMBL Binding affinity of compound was determined against Thyroid hormone receptor alpha1 B 10.22 pKd 0.06 nM Kd J Med Chem (2003) 46: 3152-3161 [PMID:12825953]
ChEMBL Displacement of [125I]T3 from human TRalpha receptor B 10.24 pKd 0.06 nM Kd Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
ChEMBL Displacement of [125I]T3 from human recombinant thyroid harmone receptor alpha after 16 to 48 hrs by gamma-ray detection B 8.63 pKi 2.33 nM Ki Bioorg Med Chem (2012) 20: 3622-3634 [PMID:22542282]
ChEMBL Displacement of [125I]-T3 from human TRalpha expressed in insect cells after 16 to 48 hrs by gamma-counting B 8.63 pKi 2.33 nM Ki Bioorg Med Chem (2013) 21: 592-607 [PMID:23276448]
ChEMBL Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay B 9.48 pKi 0.33 nM Ki J Med Chem (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay B 9.66 pKi 0.22 nM Ki Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL Displacement of [125I]-Triiodothyronine from human recombinant TRalpha1 ligand binding domain after 2 to 3 hrs by beta counting B 8.49 pIC50 3.2 nM IC50 Bioorg Med Chem (2014) 22: 488-498 [PMID:24290064]
ChEMBL Inhibitory concentration against cloned human thyroid hormone receptor alpha 1 B 9.62 pIC50 0.24 nM IC50 Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells B 9.62 pIC50 0.24 nM IC50 Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524]
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 8 pEC50 10 nM EC50 J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL Agonist activity at human THRalpha expressed in CHO cells after 24 hrs by luciferase assay B 8.47 pEC50 3.4 nM EC50 J Med Chem (2020) 63: 6727-6740 [PMID:32356658]
ChEMBL Effect on human TRalpha transactivation activity in U2OS cells by luciferase reporter assay B 8.62 pEC50 2.4 nM EC50 Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
ChEMBL Effect on human TRalpha transactivation activity in HeLa cells by luciferase reporter assay B 8.62 pEC50 2.4 nM EC50 Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
ChEMBL Agonist activity at human recombinant TRalpha1 transfected in CV-1 cells after 8 to 10 hrs by alkaline phosphatase reporter gene assay B 8.68 pEC50 2.1 nM EC50 Bioorg Med Chem (2014) 22: 488-498 [PMID:24290064]
ChEMBL Half-maximum activation of human Thyroid hormone receptor alpha-1 (hTRalpha1) B 8.7 pEC50 2 nM EC50 J Med Chem (2002) 45: 3310-3320 [PMID:12109914]
ChEMBL Effective concentration binding towards TRalpha in E25B2 cells (agonistic activity) B 8.7 pEC50 2 nM EC50 Bioorg Med Chem Lett (2003) 13: 379-382 [PMID:12565933]
ChEMBL Agonist activity at human THRalpha expressed in baculovirus infected SF9 cells after 15 mins by gel electrophoresis B 9.3 pEC50 0.5 nM EC50 J Med Chem (2020) 63: 6727-6740 [PMID:32356658]
ChEMBL Agonist activity at human thyroid hormone receptor alpha expressed in HEK293 cells by luciferase reporter gene assay B 9.39 pEC50 0.41 nM EC50 Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL Binding affinity towards thyroid hormone receptor (hTR beta 1) B 9.85 pKd 0.14 nM Kd Bioorg Med Chem Lett (2001) 11: 2821-2825 [PMID:11597408]
ChEMBL Binding affinity against human Thyroid hormone receptor beta 1 (hTRbeta1) using radiolabeled T3 B 10 pKd 0.1 nM Kd J Med Chem (2002) 45: 3310-3320 [PMID:12109914]
ChEMBL Binding affinity of compound was determined against thyroid hormone receptor beta 1 B 10.06 pKd 0.09 nM Kd J Med Chem (2003) 46: 3152-3161 [PMID:12825953]
ChEMBL Displacement of [125I]T3 from human TRbeta receptor B 10.09 pKd 0.08 nM Kd Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
GtoPdb - - 10.1 pKd - - - J Med Chem (2002) 45: 3310-20 [PMID:12109914]
ChEMBL Displacement of [125I]T3 from human recombinant thyroid harmone receptor beta after 16 to 48 hrs by gamma-ray detection B 8.64 pKi 2.29 nM Ki Bioorg Med Chem (2012) 20: 3622-3634 [PMID:22542282]
ChEMBL Displacement of [125I]-T3 from human TRbeta expressed in insect cells after 16 to 48 hrs by gamma-counting B 8.64 pKi 2.29 nM Ki Bioorg Med Chem (2013) 21: 592-607 [PMID:23276448]
ChEMBL Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay B 9.17 pKi 0.68 nM Ki J Med Chem (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay B 9.26 pKi 0.55 nM Ki Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL Inhibitory activity against [125I]T3 binding to human TRbeta1 receptor B 10.1 pKi 0.08 nM Ki Bioorg Med Chem Lett (2003) 13: 379-382 [PMID:12565933]
ChEMBL Displacement of [125I]-Triiodothyronine from human recombinant TRbeta1 ligand binding domain after 2 to 3 hrs by beta counting B 8.54 pIC50 2.9 nM IC50 Bioorg Med Chem (2014) 22: 488-498 [PMID:24290064]
ChEMBL Inhibitory concentration against cloned human thyroid hormone receptor beta 1 B 9.59 pIC50 0.26 nM IC50 Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells B 9.59 pIC50 0.26 nM IC50 Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524]
ChEMBL Inhibition of human thyroid hormone receptor beta 1 B 9.59 pIC50 0.26 nM IC50 Bioorg Med Chem (2007) 15: 5251-5261 [PMID:17524652]
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 7.82 pEC50 15 nM EC50 J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL Effect on human TRbeta transactivation activity in U2OS cells by luciferase reporter assay B 7.96 pEC50 11 nM EC50 Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
ChEMBL Effect on human TRbeta transactivation activity in HeLa cells by luciferase reporter assay B 8.62 pEC50 2.4 nM EC50 Bioorg Med Chem (2008) 16: 762-770 [PMID:17988877]
ChEMBL Half-maximum activation of human Thyroid hormone receptor beta 1 (hTRbeta1) B 8.7 pEC50 2 nM EC50 J Med Chem (2002) 45: 3310-3320 [PMID:12109914]
ChEMBL Effective concentration binding towards TR-beta-1 in E25B2 cells (agonistic activity) B 8.7 pEC50 2 nM EC50 Bioorg Med Chem Lett (2003) 13: 379-382 [PMID:12565933]
ChEMBL Agonist activity at human recombinant TRbeta1 transfected in CV-1 cells after 8 to 10 hrs by alkaline phosphatase reporter gene assay B 8.7 pEC50 2 nM EC50 Bioorg Med Chem (2014) 22: 488-498 [PMID:24290064]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3917] [GtoPdb: 589] [UniProtKB: P18113]
ChEMBL In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptor B 6.3 pIC50 500 nM IC50 J Med Chem (1995) 38: 695-707 [PMID:7861417]
ChEMBL In vitro inhibition of bound [125I]L-T3 rat plasma membrane 3,5,3'' L-triiodothyronine receptor B 7 pIC50 100 nM IC50 J Med Chem (1995) 38: 695-707 [PMID:7861417]
ChEMBL In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptor B 8.36 pIC50 4.4 nM IC50 J Med Chem (1995) 38: 695-707 [PMID:7861417]
ChEMBL In vitro inhibition of the bound [125I]L-T3 rat liver nuclear L-triiodothyronine receptor B 8.74 pIC50 1.8 nM IC50 J Med Chem (1995) 38: 695-707 [PMID:7861417]

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]