General Information of the Protein
Protein ID
PT01591
Protein Name
Thyroid hormone receptor alpha
Secondarily
Protein Name
Nuclear receptor subfamily 1 group A member 1
V-erbA-related protein 7
c-erbA-1
c-erbA-alpha
Gene Name
THRA
Secondarily
Gene Name
EAR7
ERBA1
NR1A1
THRA1
THRA2
Sequence
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKATGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGMAMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNAQGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFSELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIFELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNIPHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQLGEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVCEDLAGNAASP
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 1
>
Nuclear hormone receptor subfamily 1 group A
>
Nuclear hormone receptor subfamily 1 group A member 1
Function
Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
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Uniprot ID
Primary ID:
P10827

Secondarily ID:
A8K3B5
P21205
Q8N6A1
Q96H73
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Ensembl ID
ENSG00000126351
HGNC ID
HGNC:11796
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0026502
(2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid
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C15H12I3NO4
 2
1
EC50 = 30 nM
   TI
   LI
   LO
   TS
2
IC50 = 0.24 nM
   TI
   LI
   LO
   TS
CP0019816
2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid
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C17H16Br2O4
 1
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0461452
(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid
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C22H25Br2NO5
 1
1
IC50 = 4.3 nM
   TI
   LI
   LO
   TS
CP0509442
(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-2-phenylacetic acid
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C25H23Br2NO5
 1
1
IC50 = 5.5 nM
   TI
   LI
   LO
   TS
CP0458611
(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-2-phenylacetic acid
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C25H23Br2NO5
 1
1
IC50 = 7.5 nM
   TI
   LI
   LO
   TS
CP0461450
(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid
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C22H25Br2NO5
 1
1
IC50 = 9.8 nM
   TI
   LI
   LO
   TS
CP0503686
(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)propanoic acid
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C20H21Br2NO5
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0021463
2-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid
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C17H16Cl2O4
 1
1
IC50 = 25 nM
   TI
   LI
   LO
   TS
CP0434329
2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)acetic acid
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C19H19Br2NO5
 1
1
IC50 = 26 nM
   TI
   LI
   LO
   TS
CP0458612
(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)propanoic acid
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C20H21Br2NO5
 1
1
IC50 = 83 nM
   TI
   LI
   LO
   TS
CP0434328
(2S)-2-(1-{3,5-dibromo-4-[3-fluoro-4-hydroxy-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid
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C22H24Br2FNO5
 1
1
IC50 = 88 nM
   TI
   LI
   LO
   TS
CP0893895
(R)-2-(2-(3,5-dibromo-4-(4-hydroxy-3-isopropylphenoxy)phenyl)acetamido)succinic acid
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C21H21Br2NO7
 1
1
IC50 = 168 nM
   TI
   LI
   LO
   TS
CP0505564
(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)butanedioic acid
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C21H21Br2NO7
 1
1
IC50 = 460 nM
   TI
   LI
   LO
   TS
CP0461451
(2S)-2-(1-{3,5-dibromo-4-[3-chloro-4-hydroxy-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid
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C22H24Br2ClNO5
 1
1
IC50 = 670 nM
   TI
   LI
   LO
   TS
CP0528458
(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-methyl-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid
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C23H27Br2NO5
 1
1
IC50 = 1500 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0026502
(2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid
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C15H12I3NO4
 9
1 EC50 = 2 nM
2 IC50 = 0.24 nM
3 IC50 = 3.2 nM
4 Kd = 0.058 nM
5 Kd = 0.06 nM
6 Kd = 0.1 nM
7 Kd = 0.17 nM
8 Ki = 0.33 nM
9 Ki = 2.33 nM
CP0020161
3-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}propanoic acid
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C18H18Cl2O4
 2
1 IC50 = 0.7586 nM
2 IC50 = 0.76 nM
CP0019816
2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid
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C17H16Br2O4
 2
1 IC50 = 1.4 nM
2 IC50 = 1.549 nM
CP0021463
2-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid
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C17H16Cl2O4
 4
1 IC50 = 25 nM
2 IC50 = 25.12 nM
3 Ki = 7.18 nM
4 Ki = 7.79 nM
CP0025831
3-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)-5-[(E)-2-(pyridin-4-yl)ethenyl]phenoxy]phenyl}propanoic acid
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C25H23Br2NO4
 1
1 IC50 = 36 nM
CP0295571
3-(3,5-dibromo-4-{[3-(ethylamino)phenyl]methoxy}phenyl)propanoic acid
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C18H19Br2NO3
 1
1 IC50 = 78 nM
CP0034916
3-{3,5-dibromo-4-[(3-bromophenyl)methoxy]phenyl}propanoic acid
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C16H13Br3O3
 1
1 IC50 = 99 nM
CP0024613
3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]benzoic acid
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C16H14Cl2O4
 2
1 IC50 = 128.82 nM
2 IC50 = 130 nM
CP0076899
3-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]propanoic acid
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C22H25NO3
 1
1 IC50 = 1300 nM
CP0078043
2-(2,6-diiodo-4-((2-methylbenzofuran-3-yl)methyl)phenoxy)acetic acid
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C18H14I2O4
 2
1 IC50 = 2200 nM
2 IC50 = 4500 nM
CP0262114
4-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]butanoic acid
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C23H27NO3
 1
1 IC50 = 3400 nM
CP0154335
5-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]pentanoic acid
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C24H29NO3
 1
1 IC50 > 10000 nM
CP0646460
5-(4-(4-hydroxy-3-isopropylphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C19H18I2N2O4
 1
1 Kd = 1.2 nM
CP0823542
5-(4-(3-ethyl-4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C18H16I2N2O4
 1
1 Kd = 15 nM
CP0843267
5-(3,5-dibromo-4-(4-hydroxy-3-isopropylphenoxy)benzyl)imidazolidine-2,4-dione
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C19H18Br2N2O4
 1
1 Kd = 17 nM
CP0748742
5-(4-(4-hydroxy-3-iodophenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C16H11I3N2O4
 1
1 Kd = 24 nM
CP0733970
5-(4-(3-cyclopropyl-4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C19H16I2N2O4
 1
1 Kd = 25 nM
CP0647090
5-(4-(4-hydroxy-3-methylphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C17H14I2N2O4
 1
1 Kd = 42 nM
CP0647089
5-(4-(4-hydroxy-3-bromophenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C16H11BrI2N2O4
 1
1 Kd = 43 nM
CP0700404
5-(4-(4-hydroxy-3-methoxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C17H14I2N2O5
 1
1 Kd = 82 nM
CP0893813
5-(4-(4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione
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C16H12I2N2O4
 1
1 Kd = 1700 nM
CP0063047
(3,5-dimethyl-4-(4-hydroxy-3-isopropylbenzyl)phenoxy)methylphosphonicacid
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C19H25O5P
 1
1 Ki = 35.2 nM
Clinical Information about the Protein
Target 1 ( Thyroid hormone receptor alpha (THRA) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 High blood cholesterol level [ICD-11: 5C80.00]
2 Hypothyroidism [ICD-11: 5A00]
3 Wound healing [ICD-11: EL8Y]
Approved Drug(s) 3 Approved Drugs  3
1 Dextrothyroxine Sodium Approved
High blood cholesterol level
2 Levothyroxine Approved
Hypothyroidism
3 Liothyronine Approved
Hypothyroidism
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 tiratricol Clinical trial
Wound healing
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06742 Gag polyprotein Avian erythroblastosis virus (strain ES4)