Protein Information

General Information of the Protein

Protein ID	PT01018
Protein Name	Thyroid hormone receptor beta
Secondarily Protein Name	Nuclear receptor subfamily 1 group A member 2 c-erbA-2 c-erbA-beta
Gene Name	THRB
Secondarily Gene Name	ERBA2 NR1A2 THR1
Sequence	MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQTTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYRCITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVLDDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWKQKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCEDQIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSLSSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPKLLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED Show/Hide
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 2
Function	Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine. Show/Hide
Uniprot ID	Primary ID: P10828 Secondarily ID: B3KU79 P37243 Q13986 Q3KP35 Q6WGL2 Q9UD41 Show/Hide
Ensembl ID	ENSG00000151090
HGNC ID	HGNC:11799
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

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0026502 Compound Info	(2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid Show/Hide	C15H12I3NO4	2
1	EC50 = 10 nM Bioactivity Info	TI LI LO TS
2	IC50 = 0.26 nM Bioactivity Info	TI LI LO TS
CP0556818 Compound Info	[3,5-dichloro-4-(4-methoxy-3-propan-2-ylphenoxy)phenyl]methanol Show/Hide	C17H18Cl2O3	1
1	EC50 = 54 nM Bioactivity Info	TI LI LO TS
CP0553179 Compound Info	N-[3,5-dichloro-4-(4-methoxy-3-propan-2-ylphenoxy)phenyl]-2-(1-methylsulfonylpyrazol-4-yl)acetamide Show/Hide	C22H23Cl2N3O5S	1
1	EC50 = 1793 nM Bioactivity Info	TI LI LO TS
CP0556947 Compound Info	N-[3,5-dichloro-4-(4-methoxy-3-propan-2-ylphenoxy)phenyl]-2-pyridin-4-ylacetamide Show/Hide	C23H22Cl2N2O3	1
1	EC50 = 4711 nM Bioactivity Info	TI LI LO TS
CP0535107 Compound Info	N-[3,5-dichloro-4-(4-methoxy-3-propan-2-ylphenoxy)phenyl]-2-phenylacetamide Show/Hide	C24H23Cl2NO3	1
1	EC50 = 6700 nM Bioactivity Info	TI LI LO TS
CP0572187 Compound Info	N-[3,5-dichloro-4-(4-methoxy-3-propan-2-ylphenoxy)phenyl]-2-pyridin-3-ylacetamide Show/Hide	C23H22Cl2N2O3	1
1	EC50 = 10000 nM Bioactivity Info	TI LI LO TS
CP0019816 Compound Info	2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid Show/Hide	C17H16Br2O4	1
1	IC50 = 0.095 nM Bioactivity Info	TI LI LO TS
CP0461452 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid Show/Hide	C22H25Br2NO5	1
1	IC50 = 0.27 nM Bioactivity Info	TI LI LO TS
CP0509442 Compound Info	(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-2-phenylacetic acid Show/Hide	C25H23Br2NO5	1
1	IC50 = 0.6 nM Bioactivity Info	TI LI LO TS
CP0461450 Compound Info	(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid Show/Hide	C22H25Br2NO5	1
1	IC50 = 0.71 nM Bioactivity Info	TI LI LO TS
CP0458611 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)-2-phenylacetic acid Show/Hide	C25H23Br2NO5	1
1	IC50 = 0.78 nM Bioactivity Info	TI LI LO TS
CP0021463 Compound Info	2-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid Show/Hide	C17H16Cl2O4	1
1	IC50 = 1.1 nM Bioactivity Info	TI LI LO TS
CP0503686 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)propanoic acid Show/Hide	C20H21Br2NO5	1
1	IC50 = 1.3 nM Bioactivity Info	TI LI LO TS
CP0434329 Compound Info	2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)acetic acid Show/Hide	C19H19Br2NO5	1
1	IC50 = 2.7 nM Bioactivity Info	TI LI LO TS
CP0458612 Compound Info	(2R)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)propanoic acid Show/Hide	C20H21Br2NO5	1
1	IC50 = 5.9 nM Bioactivity Info	TI LI LO TS
CP0434328 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[3-fluoro-4-hydroxy-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid Show/Hide	C22H24Br2FNO5	1
1	IC50 = 12 nM Bioactivity Info	TI LI LO TS
CP0893895 Compound Info	(R)-2-(2-(3,5-dibromo-4-(4-hydroxy-3-isopropylphenoxy)phenyl)acetamido)succinic acid Show/Hide	C21H21Br2NO7	1
1	IC50 = 26 nM Bioactivity Info	TI LI LO TS
CP0505564 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetamido)butanedioic acid Show/Hide	C21H21Br2NO7	1
1	IC50 = 290 nM Bioactivity Info	TI LI LO TS
CP0461451 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[3-chloro-4-hydroxy-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid Show/Hide	C22H24Br2ClNO5	1
1	IC50 = 1400 nM Bioactivity Info	TI LI LO TS
CP0528458 Compound Info	(2S)-2-(1-{3,5-dibromo-4-[4-hydroxy-3-methyl-5-(propan-2-yl)phenoxy]phenyl}acetamido)-3-methylbutanoic acid Show/Hide	C23H27Br2NO5	1
1	IC50 = 2600 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000044 , CV-1

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000063 , Hep-G2

Cell Line Info

Cell Line ID: CL000043 , U2OS

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0026502 Compound Info	(2R)-2-amino-3-[4-(4-hydroxy-3-iodophenoxy)-3,5-diiodophenyl]propanoic acid Show/Hide	C15H12I3NO4	11
1	EC50 = 2 nM
2	IC50 = 0.257 nM
3	IC50 = 0.26 nM
4	IC50 = 2.9 nM
5	Kd = 0.081 nM
6	Kd = 0.087 nM
7	Kd = 0.1 nM
8	Kd = 0.14 nM
9	Ki = 0.08 nM
10	Ki = 0.68 nM
11	Ki = 2.29 nM
CP0019816 Compound Info	2-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid Show/Hide	C17H16Br2O4	2
1	IC50 = 0.095 nM
2	IC50 = 0.0955 nM
CP0020161 Compound Info	3-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}propanoic acid Show/Hide	C18H18Cl2O4	2
1	IC50 = 0.15 nM
2	IC50 = 0.1514 nM
CP0021463 Compound Info	2-{3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]phenyl}acetic acid Show/Hide	C17H16Cl2O4	4
1	IC50 = 1.096 nM
2	IC50 = 1.1 nM
3	Ki = 0.24 nM
4	Ki = 0.37 nM
CP0024613 Compound Info	3,5-dichloro-4-[4-hydroxy-3-(propan-2-yl)phenoxy]benzoic acid Show/Hide	C16H14Cl2O4	2
1	IC50 = 20.89 nM
2	IC50 = 21 nM
CP0025831 Compound Info	3-{3,5-dibromo-4-[4-hydroxy-3-(propan-2-yl)-5-[(E)-2-(pyridin-4-yl)ethenyl]phenoxy]phenyl}propanoic acid Show/Hide	C25H23Br2NO4	1
1	IC50 = 22 nM
CP0295571 Compound Info	3-(3,5-dibromo-4-{[3-(ethylamino)phenyl]methoxy}phenyl)propanoic acid Show/Hide	C18H19Br2NO3	1
1	IC50 = 23 nM
CP0154337 Compound Info	2-[[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-4-yl]amino]-2-oxoacetic acid Show/Hide	C21H22N2O4	1
1	IC50 = 40 nM
CP0363634 Compound Info	2-[[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-7-methylindol-4-yl]amino]-2-oxoacetic acid Show/Hide	C21H22N2O4	1
1	IC50 = 54 nM
CP0034916 Compound Info	3-{3,5-dibromo-4-[(3-bromophenyl)methoxy]phenyl}propanoic acid Show/Hide	C16H13Br3O3	1
1	IC50 = 60 nM
CP0076900 Compound Info	2-[[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]indol-4-yl]amino]-2-oxoacetic acid Show/Hide	C20H20N2O4	1
1	IC50 = 170 nM
CP0363635 Compound Info	3-[[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-4-yl]amino]-3-oxopropanoic acid Show/Hide	C22H24N2O4	1
1	IC50 = 230 nM
CP0476563 Compound Info	3-[[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-7-methylindol-4-yl]amino]-3-oxopropanoic acid Show/Hide	C22H24N2O4	1
1	IC50 = 240 nM
CP0262114 Compound Info	4-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]butanoic acid Show/Hide	C23H27NO3	1
1	IC50 = 290 nM
CP0076899 Compound Info	3-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]propanoic acid Show/Hide	C22H25NO3	1
1	IC50 = 760 nM
CP0154335 Compound Info	5-[1-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-2-methylindol-3-yl]pentanoic acid Show/Hide	C24H29NO3	1
1	IC50 = 1400 nM
CP0078043 Compound Info	2-(2,6-diiodo-4-((2-methylbenzofuran-3-yl)methyl)phenoxy)acetic acid Show/Hide	C18H14I2O4	3
1	IC50 = 4100 nM
2	IC50 = 5100 nM
3	IC50 = 5128.61 nM
CP0646460 Compound Info	5-(4-(4-hydroxy-3-isopropylphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C19H18I2N2O4	1
1	Kd = 1.7 nM
CP0823542 Compound Info	5-(4-(3-ethyl-4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C18H16I2N2O4	1
1	Kd = 18 nM
CP0843267 Compound Info	5-(3,5-dibromo-4-(4-hydroxy-3-isopropylphenoxy)benzyl)imidazolidine-2,4-dione Show/Hide	C19H18Br2N2O4	1
1	Kd = 18.4 nM
CP0748742 Compound Info	5-(4-(4-hydroxy-3-iodophenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C16H11I3N2O4	1
1	Kd = 36 nM
CP0733970 Compound Info	5-(4-(3-cyclopropyl-4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C19H16I2N2O4	1
1	Kd = 49 nM
CP0647090 Compound Info	5-(4-(4-hydroxy-3-methylphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C17H14I2N2O4	1
1	Kd = 53 nM
CP0647089 Compound Info	5-(4-(4-hydroxy-3-bromophenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C16H11BrI2N2O4	1
1	Kd = 68 nM
CP0700404 Compound Info	5-(4-(4-hydroxy-3-methoxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C17H14I2N2O5	1
1	Kd = 119 nM
CP0893813 Compound Info	5-(4-(4-hydroxyphenoxy)-3,5-diiodobenzyl)imidazolidine-2,4-dione Show/Hide	C16H12I2N2O4	1
1	Kd = 2000 nM
CP0063047 Compound Info	(3,5-dimethyl-4-(4-hydroxy-3-isopropylbenzyl)phenoxy)methylphosphonicacid Show/Hide	C19H25O5P	1
1	Ki = 2.95 nM

Clinical Information about the Protein

Target 1 ( Thyroid hormone receptor beta (THRB) )

Target Type	Successful Target
Disease	4 Target-related Diseases				4
1	High blood cholesterol level [ICD-11: 5C80.00]
2	Hyperlipidaemia [ICD-11: 5C80]
3	Familial hypercholesterolemia [ICD-11: 5C80.00]
4	Wound healing [ICD-11: EL8Y]
Approved Drug(s)	1 Approved Drug				1
1	Dextrothyroxine Sodium	Drug Info	Approved	High blood cholesterol level
Clinical Trial Drug(s)	4 Clinical Trial Drugs				4
1	MB-07811	Drug Info	Phase 2	Hyperlipidaemia
2	Axitirome	Drug Info	Phase 1	Hyperlipidaemia
3	MGL-3196	Drug Info	Phase 2	Familial hypercholesterolemia
4	tiratricol	Drug Info	Clinical trial	Wound healing

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han