General Information of the Protein
Protein ID
PT01475
Protein Name
Retinoic acid receptor alpha
Secondarily
Protein Name
Nuclear receptor subfamily 1 group B member 1
Gene Name
RARA
Secondarily
Gene Name
NR1B1
Sequence
MASNSSSCPTPGGGHLNGYPVPPYAFFFPPMLGGLSPPGALTTLQHQLPVSGYSTPSPATIETQSSSSEEIVPSPPSPPPLPRIYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKEVPKPECSESYTLTPEVGELIEKVRKAHQETFPALCQLGKYTTNNSSEQRVSLDIDLWDKFSELSTKCIIKTVEFAKQLPGFTTLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNAGFGPLTDLVFAFANQLLPLEMDDAETGLLSAICLICGDRQDLEQPDRVDMLQEPLLEALKVYVRKRRPSRPHMFPKMLMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGLDTLSGQPGGGGRDGGGLAPPPGSCSPSLSPSSNRSSPATHSP
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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 B
>
Nuclear hormone receptor subfamily 1 group B member 1
Function
Receptor for retinoic acid (PubMed:19850744, PubMed:16417524, PubMed:20215566). Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes (PubMed:28167758). The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (PubMed:28167758, PubMed:19398580). In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone deacetylation, chromatin condensation and transcriptional suppression (PubMed:16417524). On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation (PubMed:9267036, PubMed:19850744, PubMed:20215566). Formation of a complex with histone deacetylases might lead to inhibition of RARE DNA element binding and to transcriptional repression (PubMed:28167758). Transcriptional activation and RARE DNA element binding might be supported by the transcription factor KLF2 (PubMed:28167758). RARA plays an essential role in the regulation of retinoic acid-induced germ cell development during spermatogenesis (By similarity). Has a role in the survival of early spermatocytes at the beginning prophase of meiosis (By similarity). In Sertoli cells, may promote the survival and development of early meiotic prophase spermatocytes (By similarity). In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function (By similarity). Together with RXRA, positively regulates microRNA-10a expression, thereby inhibiting the GATA6/VCAM1 signaling response to pulsatile shear stress in vascular endothelial cells (PubMed:28167758). In association with HDAC3, HDAC5 and HDAC7 corepressors, plays a role in the repression of microRNA-10a and thereby promotes the inflammatory response (PubMed:28167758).
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Uniprot ID
Primary ID:
P10276

Secondarily ID:
B8Y636
P78456
Q13440
Q13441
Q96S41
Q9NQS0
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HGNC ID
HGNC:9864
Subcellular Location
Nucleus
Cytoplasm
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: CL000044 , CV-1
Compound ID Compound Name Compound Formula
CP0723268
3'-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-biphenyl-4-carboxylic acid
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C27H28O2
 1
1
AC50 = 1 nM
   TI
   LI
   LO
   TS
CP0718144
4-[3-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5-dihydro-isoxazol-5-yl]-benzoic acid
   Show/Hide
C25H29NO3
 1
1
AC50 = 14 nM
   TI
   LI
   LO
   TS
CP0042977
9-cis retinoic acid
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C20H28O2
 3
1
AC50 = 19 nM
   TI
   LI
   LO
   TS
2
EC50 = 191 nM
   TI
   LI
   LO
   TS
3
EC50 = 220 nM
   TI
   LI
   LO
   TS
CP0742222
4'-Methyl-3'-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-biphenyl-4-carboxylic acid
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C28H30O2
 1
1
AC50 = 79 nM
   TI
   LI
   LO
   TS
CP0041093
(E)-4-(2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-enyl)benzoic acid
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C24H28O2
 2
1
AC50 = 200 nM
   TI
   LI
   LO
   TS
2
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0648950
4-[6-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-pyridin-2-yl]-benzoic acid
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C26H27NO2
 1
1
AC50 = 370 nM
   TI
   LI
   LO
   TS
CP0041422
4-[2-Methyl-1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
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C25H30O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0049341
4-[2-Methyl-1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
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C26H32O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0299470
4-[Cyclopropylidene-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-methyl]-benzoic acid
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C26H30O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0730002
5',5',8',8'-Tetramethyl-5',6',7',8'-tetrahydro-[1,2']binaphthalenyl-6-carboxylic acid
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C25H26O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0734985
4-[(Z)-3-Methyl-1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-but-1-enyl]-benzoic acid
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C26H32O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0756887
4-[Cyclopropylidene-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-methyl]-benzoic acid
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C25H28O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0042771
5',5',8',8'-Tetramethyl-5',6',7',8'-tetrahydro-[2,2']binaphthalenyl-6-carboxylic acid
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C25H26O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0715557
4-[2-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-thiazol-5-yl]-benzoic acid
   Show/Hide
C25H27NO2S
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0742480
4'-Methyl-3'-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-biphenyl-4-carboxylic acid
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C29H32O2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0806169
4-[6-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-pyridin-2-yl]-benzoic acid
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C27H29NO2
 1
1
AC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0092667
4-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
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C23H26O3
 2
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
2
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0004259
4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl]benzoic acid
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C24H28O2
 2
1
EC50 = 6 nM
   TI
   LI
   LO
   TS
2
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0040160
9-cis-retinoic acid (9cRA)
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C20H28O2
 3
1
EC50 = 7 nM
   TI
   LI
   LO
   TS
2
EC50 = 350 nM
   TI
   LI
   LO
   TS
3
EC50 = 436 nM
   TI
   LI
   LO
   TS
CP0042976
(2E,4E)-3-Methyl-6-[1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-hexa-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1
EC50 = 59 nM
   TI
   LI
   LO
   TS
CP0073370
4-[(E)-2-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
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C25H30O2
 1
1
EC50 = 340 nM
   TI
   LI
   LO
   TS
CP0403151
4-[(E)-2-(3,3-Dimethyl-2,3-dihydro-benzo[b]thiophen-5-yl)-propenyl]-benzoic acid
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C20H20O2S
 1
1
EC50 = 420 nM
   TI
   LI
   LO
   TS
CP0377308
4-[(E)-2-(4,4-Dimethyl-thiochroman-6-yl)-propenyl]-benzoic acid methyl ester
   Show/Hide
C22H24O2S
 1
1
EC50 = 620 nM
   TI
   LI
   LO
   TS
CP0063990
(2E,4E)-6-[1-(3,5-Di-tert-butyl-phenyl)-cyclopropyl]-3-methyl-hexa-2,4-dienoic acid
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C24H34O2
 1
1
EC50 = 733 nM
   TI
   LI
   LO
   TS
CP0414842
(2E,4E,6E)-7-(4,4-Dimethyl-chroman-6-yl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C20H24O3
 1
1
EC50 = 740 nM
   TI
   LI
   LO
   TS
CP0449565
(2E,4E,6E)-7-(3,3-Dimethyl-2,3-dihydro-benzofuran-5-yl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C19H22O3
 1
1
EC50 = 800 nM
   TI
   LI
   LO
   TS
CP0372864
(2E,4E,6E)-7-(3,3-Dimethyl-2,3-dihydro-benzo[b]thiophen-5-yl)-3-methyl-octa-2,4,6-trienoic acid
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C19H22O2S
 1
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
CP0448523
4-[(E)-2-(4,4-Dimethyl-chroman-6-yl)-propenyl]-benzoic acid methyl ester
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C22H24O3
 1
1
EC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0493334
4-[(E)-2-(4,4-Dimethyl-chroman-6-yl)-propenyl]-benzoic acid
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C21H22O3
 1
1
EC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0377408
(2E,4E,6E)-7-(4,4-Dimethyl-thiochroman-6-yl)-3-methyl-octa-2,4,6-trienoic acid
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C20H24O2S
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0061828
4-[(E)-2-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
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C26H32O2
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0377756
4-[(E)-2-(3,3-Dimethyl-2,3-dihydro-benzofuran-5-yl)-propenyl]-benzoic acid
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C20H20O3
 1
1
EC50 = 2300 nM
   TI
   LI
   LO
   TS
CP0184156
4-(3-Fluoro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
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C22H23FO3
 1
1
EC50 = 2856 nM
   TI
   LI
   LO
   TS
CP0041092
4-(3-Hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
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C22H24O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0047977
4-[1-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
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C23H26O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0049287
4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
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C22H24O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0063697
4-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
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C24H28O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0063793
4-[1-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C26H32O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0063958
4-[1-(3-Bromo-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25BrO2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0076318
4-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C25H30O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0100503
4-[1-(3-Hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H26O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0100726
4-(5,5,8,8-Tetramethyl-3-propyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C25H30O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0105911
4-[1-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C24H28O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0111163
4-[1-(3-Chloro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25ClO2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0123457
4-[1-(5,5,8,8-Tetramethyl-3-propyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C26H32O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0144133
4-(3-Chloro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H23ClO3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0149843
4-[1-(3-Fluoro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25FO2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0149955
4-[1-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C25H30O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0186182
4-(3-Bromo-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H23BrO3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0209249
4-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C23H26O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0148476
4-[(E)-2-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
   Show/Hide
C27H34O2
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0078638
(E)-3-[5-Methyl-4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-ylmethyl)-furan-2-yl]-acrylic acid
   Show/Hide
C23H28O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0183099
(E)-3-[4-(5,5,8,8-Tetramethyl-3-propoxy-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C28H36O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0211342
3-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl]-propionic acid
   Show/Hide
C25H32O2S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0279537
(E)-3-[4-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C26H32O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0316932
(E)-3-[4-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-4,5,6,7-tetrahydro-1-benzofuran-2-yl]but-2-enoic acid
   Show/Hide
C26H32O3
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0321600
(E)-3-[4-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C26H32O4
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0358617
(E)-3-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl]-acrylic acid
   Show/Hide
C25H30O2S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0683244
5-[1-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-meth-(E)-ylidene]-thiazolidine-2,4-dione
   Show/Hide
C26H29NO3S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0095234
(E)-3-Methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0134367
(E)-3-Methyl-5-[2-methyl-2-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid
   Show/Hide
C25H34O2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0215028
(2Z,4E)-3-methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0280492
(2Z,4E)-3-methyl-5-[2-methyl-2-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid
   Show/Hide
C25H34O2
 1
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0006755
(2E,4E,6Z)-7-[3,5-Di-tert-butyl-2-(2,2-difluoro-ethoxy)-phenyl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C25H34F2O3
 1
1
Ki = 54 nM
   TI
   LI
   LO
   TS
CP0044243
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL]PYRIDINE-3-CARBOXYLIC ACID
   Show/Hide
C24H29NO2
 1
1
Ki = 1550 nM
   TI
   LI
   LO
   TS
CP0465377
(2E,4E,6Z)-7-(3-Isopropyl-5-pentafluoroethyl-2-propoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C23H27F5O3
 1
1
Ki = 2500 nM
   TI
   LI
   LO
   TS
CP0403927
(2E,4E,6Z)-7-(2-Butoxy-3-isopropyl-5-pentafluoroethyl-phenyl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C24H29F5O3
 1
1
Ki = 2750 nM
   TI
   LI
   LO
   TS
CP0395224
(2E,4E,6E)-7-(2-Butoxy-3,5-diisopropyl-phenyl)-6-fluoro-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C25H35FO3
 1
1
Ki = 3730 nM
   TI
   LI
   LO
   TS
CP0377464
(2E,4E,6Z)-7-[2-(2,2-Difluoro-ethoxy)-3-isopropyl-5-thiophen-2-yl-phenyl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C24H26F2O3S
 1
1
Ki = 4555 nM
   TI
   LI
   LO
   TS
CP0448038
(2E,4E,6Z)-7-[4-(2,2-Difluoro-ethoxy)-4'-fluoro-5-isopropyl-biphenyl-3-yl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C26H27F3O3
 1
1
Ki = 4555 nM
   TI
   LI
   LO
   TS
CP0406456
(2E,4E,6Z)-7-[2-(2,2-Difluoro-ethoxy)-5-isopropyl-biphenyl-3-yl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C26H28F2O3
 1
1
Ki = 4659 nM
   TI
   LI
   LO
   TS
CP0397600
(2E,4E,6E)-7-[3,5-Di-tert-butyl-2-(2,2,2-trifluoro-ethoxy)-phenyl]-6-fluoro-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C25H32F4O3
 1
1
Ki = 4663 nM
   TI
   LI
   LO
   TS
CP0401559
(2E,4E,6E)-7-[2-(2,2-Difluoro-ethoxy)-3,5-bis-(1,1-dimethyl-propyl)-phenyl]-6-fluoro-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C27H37F3O3
 1
1
Ki = 6592 nM
   TI
   LI
   LO
   TS
CP0420322
(2E,4E,6Z)-7-[4-(2,2-Difluoro-ethoxy)-2'-fluoro-5-isopropyl-biphenyl-3-yl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C26H27F3O3
 1
1
Ki = 6756 nM
   TI
   LI
   LO
   TS
CP0004953
(2E,4E,6E)-7-[3,5-Di-tert-butyl-2-(2,2-difluoro-ethoxy)-phenyl]-6-fluoro-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C25H33F3O3
 1
1
Ki = 8300 nM
   TI
   LI
   LO
   TS
CP0377687
(2E,4E,6Z)-7-[4-(2,2-Difluoro-ethoxy)-3'-fluoro-5-isopropyl-biphenyl-3-yl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C26H27F3O3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0384182
(2E,4E,6Z)-7-[4-(2,2-Difluoro-ethoxy)-3',5'-difluoro-5-isopropyl-biphenyl-3-yl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C26H26F4O3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0394545
(2E,4E,6Z)-7-(2-Ethoxy-3-isopropyl-5-pentafluoroethyl-phenyl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C22H25F5O3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
CP0397602
(2E,4E,6Z)-7-(5-Isopropyl-3-pentafluoroethyl-2-propoxy-phenyl)-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C23H27F5O3
 1
1
Ki > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0040160
9-cis-retinoic acid (9cRA)
   Show/Hide
C20H28O2
 16
1 EC50 = 5 nM
2 EC50 = 16.1 nM
3 EC50 = 27 nM
4 EC50 = 50 nM
5 EC50 = 240 nM
6 EC50 = 350 nM
7 IC50 = 0.78 nM
8 IC50 = 0.89 nM
9 IC50 = 15 nM
10 IC50 = 9000 nM
11 Kd = 14 nM
12 Kd = 15 nM
13 Kd = 16 nM
14 Ki = 0.1 nM
15 Ki = 16 nM
16 Ki = 187 nM
CP0041093
(E)-4-(2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)prop-1-enyl)benzoic acid
   Show/Hide
C24H28O2
 6
1 EC50 = 21 nM
2 EC50 = 30 nM
3 EC50 = 85 nM
4 IC50 = 36 nM
5 Kd = 36 nM
6 Ki = 21 nM
CP0042977
9-cis retinoic acid
   Show/Hide
C20H28O2
 9
1 EC50 = 23 nM
2 EC50 = 45 nM
3 EC50 = 102 nM
4 EC50 = 191 nM
5 IC50 = 7 nM
6 Kd = 11 nM
7 Kd = 90 nM
8 Kd = 93 nM
9 Ki = 22.3 nM
CP0073370
4-[(E)-2-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
   Show/Hide
C25H30O2
 2
1 EC50 = 4580 nM
2 IC50 = 638 nM
CP0004259
4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl]benzoic acid
   Show/Hide
C24H28O2
 5
1 EC50 > 10000 nM
2 Kd > 1000 nM
3 Ki = 180 nM
4 Ki = 5453 nM
5 Ki > 1000 nM
CP0076822
4-(1,1,4,4-tetramethyl-1,2,3,4-tetrahydronaphthalene-7-carboxamido)benzoic acid
   Show/Hide
C22H25NO3
 2
1 IC50 = 41 nM
2 Kd = 36 nM
CP0061828
4-[(E)-2-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
   Show/Hide
C26H32O2
 1
1 IC50 = 100 nM
CP0148476
4-[(E)-2-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-propenyl]-benzoic acid
   Show/Hide
C27H34O2
 1
1 IC50 > 1000 nM
CP0042976
(2E,4E)-3-Methyl-6-[1-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-hexa-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1 Kd = 644 nM
CP0047977
4-[1-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H26O2
 2
1 Kd = 944 nM
2 Ki = 944 nM
CP0103897
(2E,4E)-3-Methyl-5-[(1R,2R)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1 Kd = 5750 nM
CP0095234
(E)-3-Methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1 Kd = 9500 nM
CP0041092
4-(3-Hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H24O4
 1
1 Kd > 1000 nM
CP0049287
4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H24O3
 1
1 Kd > 1000 nM
CP0063697
4-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C24H28O3
 1
1 Kd > 1000 nM
CP0063793
4-[1-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C26H32O2
 1
1 Kd > 1000 nM
CP0063958
4-[1-(3-Bromo-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25BrO2
 1
1 Kd > 1000 nM
CP0076318
4-(3-Isopropyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C25H30O3
 1
1 Kd > 1000 nM
CP0092667
4-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C23H26O3
 2
1 Kd > 1000 nM
2 Ki > 10000 nM
CP0100503
4-[1-(3-Hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H26O3
 1
1 Kd > 1000 nM
CP0100726
4-(5,5,8,8-Tetramethyl-3-propyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C25H30O3
 1
1 Kd > 1000 nM
CP0111163
4-[1-(3-Chloro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25ClO2
 1
1 Kd > 1000 nM
CP0123457
4-[1-(5,5,8,8-Tetramethyl-3-propyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C26H32O2
 1
1 Kd > 1000 nM
CP0144133
4-(3-Chloro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H23ClO3
 1
1 Kd > 1000 nM
CP0149843
4-[1-(3-Fluoro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C23H25FO2
 1
1 Kd > 1000 nM
CP0149955
4-[1-(3-Ethyl-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C25H30O2
 1
1 Kd > 1000 nM
CP0184156
4-(3-Fluoro-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H23FO3
 1
1 Kd > 1000 nM
CP0186182
4-(3-Bromo-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C22H23BrO3
 1
1 Kd > 1000 nM
CP0209249
4-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalene-2-carbonyl)-benzoic acid
   Show/Hide
C23H26O4
 1
1 Kd > 1000 nM
CP0105911
4-[1-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-vinyl]-benzoic acid
   Show/Hide
C24H28O3
 1
1 Kd > 1000 nM
CP0134367
(E)-3-Methyl-5-[2-methyl-2-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-cyclopropyl]-penta-2,4-dienoic acid
   Show/Hide
C25H34O2
 1
1 Kd > 1000 nM
CP0215028
(2Z,4E)-3-methyl-5-[2-methyl-2-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid
   Show/Hide
C24H32O2
 1
1 Kd > 1000 nM
CP0280492
(2Z,4E)-3-methyl-5-[2-methyl-2-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)cyclopropyl]penta-2,4-dienoic acid
   Show/Hide
C25H34O2
 1
1 Kd > 1000 nM
CP0063990
(2E,4E)-6-[1-(3,5-Di-tert-butyl-phenyl)-cyclopropyl]-3-methyl-hexa-2,4-dienoic acid
   Show/Hide
C24H34O2
 1
1 Kd > 1000 nM
CP0042771
5',5',8',8'-Tetramethyl-5',6',7',8'-tetrahydro-[2,2']binaphthalenyl-6-carboxylic acid
   Show/Hide
C25H26O2
 1
1 Ki = 580 nM
CP0076073
6-(3-(1-Adamantyl)-4-methoxyphenyl)-2-naphthoic acid
   Show/Hide
C28H28O3
 1
1 Ki = 1100 nM
CP0044243
6-[1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL]PYRIDINE-3-CARBOXYLIC ACID
   Show/Hide
C24H29NO2
 1
1 Ki = 2745 nM
CP0047520
6-(3-Adamantan-1-yl-4-hydroxy-phenyl)-naphthalene-2-carboxylic acid
   Show/Hide
C27H26O3
 1
1 Ki = 6500 nM
CP0006755
(2E,4E,6Z)-7-[3,5-Di-tert-butyl-2-(2,2-difluoro-ethoxy)-phenyl]-3-methyl-octa-2,4,6-trienoic acid
   Show/Hide
C25H34F2O3
 1
1 Ki > 1000 nM
CP0078638
(E)-3-[5-Methyl-4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-ylmethyl)-furan-2-yl]-acrylic acid
   Show/Hide
C23H28O3
 1
1 Ki > 1000 nM
CP0183099
(E)-3-[4-(5,5,8,8-Tetramethyl-3-propoxy-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C28H36O4
 1
1 Ki > 1000 nM
CP0211342
3-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl]-propionic acid
   Show/Hide
C25H32O2S
 1
1 Ki > 1000 nM
CP0279537
(E)-3-[4-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C26H32O3
 1
1 Ki > 1000 nM
CP0316932
(E)-3-[4-(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)-4,5,6,7-tetrahydro-1-benzofuran-2-yl]but-2-enoic acid
   Show/Hide
C26H32O3
 1
1 Ki > 1000 nM
CP0321600
(E)-3-[4-(3-Methoxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-acrylic acid
   Show/Hide
C26H32O4
 1
1 Ki > 1000 nM
CP0358617
(E)-3-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzo[b]thiophen-2-yl]-acrylic acid
   Show/Hide
C25H30O2S
 1
1 Ki > 1000 nM
CP0683244
5-[1-[4-(5,5,8,8-Tetramethyl-5,6,7,8-tetrahydro-naphthalen-2-yl)-4,5,6,7-tetrahydro-benzofuran-2-yl]-meth-(E)-ylidene]-thiazolidine-2,4-dione
   Show/Hide
C26H29NO3S
 1
1 Ki > 1000 nM
Clinical Information about the Protein
Target 1 ( Retinoic acid receptor alpha (RARA) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 T-cell leukaemia [ICD-11: 2A90]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Acquired immune deficiency syndrome [ICD-11: 1C62.3]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Tamibarotene Phase 3
T-cell leukaemia
2 IRX-5183 Phase 1
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 LG100268 Discontinued in Phase 1
Acquired immune deficiency syndrome
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT01452 Retinoic acid receptor beta Homo sapiens, Human
PT01621 Retinoic acid receptor alpha Mus musculus, Mouse