Details of the Target

General Information of Target

Target ID LDTP02524
Target Name Thyroid hormone receptor alpha (THRA)
Gene Name THRA
Gene ID 7067
Synonyms
EAR7; ERBA1; NR1A1; THRA1; THRA2; Thyroid hormone receptor alpha; Nuclear receptor subfamily 1 group A member 1; V-erbA-related protein 7; EAR-7; c-erbA-1; c-erbA-alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
Target Type
Successful
Target Bioclass
Transcription factor
Family
Nuclear hormone receptor family, NR1 subfamily
Subcellular location
Cytoplasm; Nucleus
Function
[Isoform Alpha-1]: Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.; [Isoform Alpha-2]: Does not bind thyroid hormone and functions as a weak dominant negative inhibitor of thyroid hormone action.
TTD ID
T79591
Uniprot ID
P10827
DrugMap ID
TTTSEPU
Ensemble ID
ENST00000264637.8
HGNC ID
HGNC:11796
ChEMBL ID
CHEMBL1860

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
DBIA
 Probe Info  		C334(2.62)  LDD3364  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 AGS C334(1.80)  LDD2263  [2]
 LDCM0023  KB03 AGS C334(2.88)  LDD2680  [2]
 LDCM0024  KB05 NCI-N87 C334(2.62)  LDD3364  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CD160 antigen (CD160) . O95971
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Angiomotin-like protein 2 (AMOTL2) Angiomotin family Q9Y2J4
cAMP-dependent protein kinase type I-beta regulatory subunit (PRKAR1B) CAMP-dependent kinase regulatory chain family P31321
Centrosomal protein of 76 kDa (CEP76) CEP76 family Q8TAP6
Mediator of RNA polymerase II transcription subunit 1 (MED1) Mediator complex subunit 1 family Q15648
Lethal(3)malignant brain tumor-like protein 3 (L3MBTL3) . Q96JM7
Synapse-associated protein 1 (SYAP1) . Q96A49

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amiodarone Small molecular drug DB01118
Dextrothyroxine Small molecular drug DB00509
Dextrothyroxine Sodium Small molecular drug D03TPR
Dronedarone Small molecular drug DB04855
Levothyroxine Small molecular drug D06RGG
Liothyronine Small molecular drug D0S6JG
Liotrix Small molecular drug DB01583
Thyroid Porcine . DB09100
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bct303 . D03KVY
Clinical trial
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tiratricol Small molecular drug D0J6XC
Investigative
Click To Hide/Show 16 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(3,5-dibromo-4-hexyloxy-phenyl)-acetic Acid Small molecular drug D05FRX
(E)-1-(4-heptylphenyl)But-2-en-1-one Small molecular drug D0I7DH
(Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic Acid Small molecular drug D0J0MD
1-(4-hexylphenyl)-3-morpholinopropan-1-one Small molecular drug D06IJW
3-(3,5-dibromo-4-hexyloxy-phenyl)-propionic Acid Small molecular drug D01NTN
3-(4-(Benzyloxy)-3,5-dibromophenyl)Propanoic Acid Small molecular drug D0Q9ZN
3-(Dibutylamino)-1-(4-hexylphenyl)Propan-1-one Small molecular drug D01HAZ
3-(Dimethylamino)-1-(4-hexylphenyl)Propan-1-one Small molecular drug D03VOM
3-bromo-1-(4-hexylphenyl)Propan-1-one Small molecular drug D09XOC
4-(4-hexylphenyl)-4-oxobut-2-enoic Acid Small molecular drug D04FQZ
4-hexylphenyl Propiolate Small molecular drug D0ZX0Y
Detrothyronine Small molecular drug D0I2GK
Rt3 Small molecular drug D0Q0YS
Eprotirome . DB05035
Kb-141 . DB03176
Nrp409 . DB05235

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840