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 (Levothyroxine sodium related compound liothyronine, Euthroid-1, Triostat, Rathyronine, Euthroid-2, Thyrolar-5, Triiodothyronine (T3 Or Liothyronine, Active) (6-11%), Liothyronine, Thyrolar-0.5, Cytomel, Thyrolar-0.25, Thyrolar-2, Tertroxin, Euthroid-0.5, Thyrolar-1, Euthroid-3, Thyrolar-3, NSC-80203)
  • 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!
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!
  • 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: 419416404410414412408406405411407417409413415418] [UniProtKB: O00591O14764P14867P18505P18507P28472P31644P34903P47869P47870P48169P78334Q16445Q8N1C3Q99928Q9UN88]
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: 419410416414408406413405407415409404412411417] [UniProtKB: O09028P15431P18506P18508P19969P20236P23574P23576P28471P28473P30191P62813P63079P63138Q91ZM7Q9ES14]
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]
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]
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 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 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 28:

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