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

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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]
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  • Androgen receptor/Androgen Receptor in Human [ChEMBL: CHEMBL1871] [GtoPdb: 628] [UniProtKB: P10275]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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  • OATP1C1/Solute carrier organic anion transporter family member 1C1 in Mouse [ChEMBL: CHEMBL2073688] [GtoPdb: 1222] [UniProtKB: Q9ERB5]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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  • Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
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  • 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]
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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]
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 human THR-alpha expressed in CHO-K1 cells by PathHunter assay B 7.52 pEC50 30 nM EC50 J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
ChEMBL Agonist activity at wild type human TR alpha LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay B 7.53 pEC50 29.7 nM EC50 J Med Chem (2022) 65: 7193-7211 [PMID:35507418]
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 HeLa 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 U2OS 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 transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay B 9.15 pEC50 0.7 nM EC50 J Med Chem (2023) 66: 3284-3300 [PMID:36799411]
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 human TR beta LBD (202 to 461 residues) expressed in Escherichia coli BL21 (DE3) cells assessed as induction of N-terminal biotinylated coactivator SRC2-3 peptide recruitment by alphascreen assay B 7.45 pEC50 35.2 nM EC50 J Med Chem (2022) 65: 7193-7211 [PMID:35507418]
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 Agonist activity at human THR-beta expressed in CHO-K1 cells by PathHunter assay B 8 pEC50 10 nM EC50 J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
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]
ChEMBL Agonist activity at human THRbeta transfected in Huh7 cells co-transfected with luciferase reporter plasmid assessed as reduction in luciferase activity incubated for 16 hrs by Steady-Glo luciferase assay B 8.96 pEC50 1.1 nM EC50 J Med Chem (2023) 66: 3284-3300 [PMID:36799411]
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 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]