General Information of the Protein
Protein ID
PT03033
Protein Name
Nuclear receptor ROR-beta
Secondarily
Protein Name
Nuclear receptor RZR-beta
Nuclear receptor subfamily 1 group F member 2
Retinoid-related orphan receptor-beta
Gene Name
RORB
Secondarily
Gene Name
NR1F2
RZRB
Sequence
MCENQLKTKADATAQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQQNNASYSCPRQRNCLIDRTNRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLYAEVQKHQQRLQEQRQQQSGEAEALARVYSSSISNGLSNLNNETSGTYANGHVIDLPKSEGYYNVDSGQPSPDQSGLDMTGIKQIKQEPIYDLTSVPNLFTYSSFNNGQLAPGITMTEIDRIAQNIIKSHLETCQYTMEELHQLAWQTHTYEEIKAYQSKSREALWQQCAIQITHAIQYVVEFAKRITGFMELCQNDQILLLKSGCLEVVLVRMCRAFNPLNNTVLFEGKYGGMQMFKALGSDDLVNEAFDFAKNLCSLQLTEEEIALFSSAVLISPDRAWLIEPRKVQKLQEKIYFALQHVIQKNHLDDETLAKLIAKIPTITAVCNLHGEKLQVFKQSHPEIVNTLFPPLYKELFNPDCATGCK
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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 F
Function
Nuclear receptor that binds DNA as a monomer to ROR response elements (RORE) containing a single core motif half-site 5'-AGGTCA-3' preceded by a short A-T-rich sequence. Considered to have intrinsic transcriptional activity, have some natural ligands such as all-trans retinoic acid (ATRA) and other retinoids which act as inverse agonists repressing the transcriptional activity. Required for normal postnatal development of rod and cone photoreceptor cells. Modulates rod photoreceptors differentiation at least by inducing the transcription factor NRL-mediated pathway. In cone photoreceptor cells, regulates transcription of OPN1SW. Involved in the regulation of the period length and stability of the circadian rhythm. May control cytoarchitectural patterning of neocortical neurons during development. May act in a dose-dependent manner to regulate barrel formation upon innervation of layer IV neurons by thalamocortical axons. May play a role in the suppression of osteoblastic differentiation through the inhibition of RUNX2 transcriptional activity (By similarity).
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Uniprot ID
Primary ID:
Q92753

Secondarily ID:
Q8WX73
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Ensembl ID
ENSG00000198963
HGNC ID
HGNC:10259
Subcellular Location
Nucleus
Nucleoplasm
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0234135
N-(2-methylpropyl)-N-[[5-(4-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 1
1
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0257822
N-(2-methylpropyl)-N-[[4-(4-methylsulfonylphenyl)phenyl]methyl]-1-phenylmethanesulfonamide
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C25H29NO4S2
 1
1
EC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0059785
N-[[4-[4-(methanesulfonamido)phenyl]phenyl]methyl]-N-(2-methylpropyl)-1-phenylmethanesulfonamide
   Show/Hide
C25H30N2O4S2
 1
1
EC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0059780
N-(2-methylpropyl)-N-[[5-(3-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 1
1
EC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0168528
4-[4-[[benzylsulfonyl(2-methylpropyl)amino]methyl]phenyl]benzamide
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C25H28N2O3S
 1
1
EC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0459436
5-butyl-9-chloro-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6-one
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C20H16ClF6NO2
 1
1
IC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0481996
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-hexylphenanthridin-6-one
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C22H21F6NO2
 1
1
IC50 = 5400 nM
   TI
   LI
   LO
   TS
CP0524496
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-9-hydroxyphenanthridin-6-one
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C20H17F6NO3
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0459435
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-9-(trifluoromethyl)phenanthridin-6-one
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C21H16F9NO2
 1
1
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0380839
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6-one
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C20H17F6NO2
 2
1
IC50 = 5700 nM
   TI
   LI
   LO
   TS
2
IC50 = 6500 nM
   TI
   LI
   LO
   TS
CP0389304
2-(5,5-dibutylbenzo[b][1]benzosilol-2-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol
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C23H26F6OSi
 1
1
IC50 = 6700 nM
   TI
   LI
   LO
   TS
CP0456138
2-(5-butyl-5-methylbenzo[b][1]benzosilol-2-yl)-1,1,1,3,3,3-hexafluoropropan-2-ol
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C20H20F6OSi
 1
1
IC50 = 7000 nM
   TI
   LI
   LO
   TS
CP0487873
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-9-methylphenanthridin-6-one
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C21H19F6NO2
 1
1
IC50 = 7100 nM
   TI
   LI
   LO
   TS
CP0473976
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-10-methoxyphenanthridin-6-one
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C21H19F6NO3
 1
1
IC50 = 7500 nM
   TI
   LI
   LO
   TS
CP0488049
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-9-methoxyphenanthridin-6-one
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C21H19F6NO3
 1
1
IC50 = 7700 nM
   TI
   LI
   LO
   TS
CP0380838
5-butyl-2-ethylphenanthridin-6-one
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C19H21NO
 1
1
IC50 = 7900 nM
   TI
   LI
   LO
   TS
CP0395440
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-propylphenanthridin-6-one
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C19H15F6NO2
 1
1
IC50 = 8200 nM
   TI
   LI
   LO
   TS
CP0488050
5-(cyclohexylmethyl)-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6-one
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C23H21F6NO2
 1
1
IC50 = 8800 nM
   TI
   LI
   LO
   TS
CP0467808
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-propan-2-ylphenanthridin-6-one
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C19H15F6NO2
 1
1
IC50 = 9700 nM
   TI
   LI
   LO
   TS
CP0467810
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-4-methoxyphenanthridin-6-one
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C21H19F6NO3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0116134
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-N-(4-fluorophenyl)-2-methylpropanamide
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C26H27FN2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0116135
N-(4-cyanopyridin-2-yl)-2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-2-methylpropanamide
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C26H25FN4O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0116165
N-(2,4-difluorophenyl)-2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-2-methylpropanamide
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C26H25F3N2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0262113
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-N-(4-fluorophenyl)-2-methylpropanamide
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C26H26F2N2O4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0499213
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-(2,2,2-trifluoroethyl)phenanthridin-6-one
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C18H10F9NO2
 1
1
IC50 = 10100 nM
   TI
   LI
   LO
   TS
CP0395912
5-butyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-3-methoxyphenanthridin-6-one
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C21H19F6NO3
 1
1
IC50 = 10900 nM
   TI
   LI
   LO
   TS
CP0459431
5-butyl-2-hexylphenanthridin-6-one
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C23H29NO
 1
1
IC50 = 11300 nM
   TI
   LI
   LO
   TS
CP0459432
5-(cyclopropylmethyl)-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6-one
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C20H15F6NO2
 1
1
IC50 = 11800 nM
   TI
   LI
   LO
   TS
CP0487874
5-butyl-2-tert-butylphenanthridin-6-one
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C21H25NO
 1
1
IC50 = 12800 nM
   TI
   LI
   LO
   TS
CP0417384
5-butylphenanthridin-6-one
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C17H17NO
 1
1
IC50 = 13400 nM
   TI
   LI
   LO
   TS
CP0467809
5-butyl-2-propan-2-ylphenanthridin-6-one
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C20H23NO
 1
1
IC50 = 17000 nM
   TI
   LI
   LO
   TS
CP0459433
5-butyl-2-methylphenanthridin-6-one
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C18H19NO
 1
1
IC50 = 17100 nM
   TI
   LI
   LO
   TS
CP0395918
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-nonylphenanthridin-6-one
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C25H27F6NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0395919
5-ethyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenanthridin-6-one
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C18H13F6NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0397540
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5-methylphenanthridin-6-one
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C17H11F6NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0459434
5-butyl-2-(hydroxymethyl)phenanthridin-6-one
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C18H19NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0478004
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-5H-phenanthridin-6-one
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C16H9F6NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0394583
2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-4-methyl-5H-phenanthridin-6-one
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C17H11F6NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0394584
8-fluoro-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-4-methyl-5H-phenanthridin-6-one
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C17H10F7NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0482005
8-fluoro-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-4,5-dimethylphenanthridin-6-one
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C18H12F7NO2
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0003740
N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
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C17H12F9NO3S
 1
1 IC50 > 5011.87 nM
CP0198474
3-cyano-N-[3-[1-(cyclopentanecarbonyl)piperidin-4-yl]-1-methylindol-5-yl]benzamide
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C28H30N4O2
 1
1 IC50 > 30000 nM
CP0202028
4-cyano-N-[3-[1-(cyclopentanecarbonyl)piperidin-4-yl]-1-methylindol-5-yl]pyridine-2-carboxamide
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C27H29N5O2
 1
1 IC50 > 30000 nM
CP0324037
4-cyano-N-[3-[1-(cyclohexanecarbonyl)piperidin-4-yl]-1-methylindol-5-yl]pyridine-2-carboxamide
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C28H31N5O2
 1
1 IC50 > 30000 nM
CP0361384
3-cyano-N-[3-[1-(cyclopentanecarbonyl)piperidin-4-yl]-1H-indol-5-yl]benzamide
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C27H28N4O2
 1
1 IC50 > 30000 nM
CP0341598
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-[(3,3-difluoropiperidin-1-yl)methyl]-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C26H27F8N5O5S2
 1
1 Kd = 62 nM
CP0339634
3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluorobutan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C23H27Cl2F3N2O4S2
 1
1 Kd = 115 nM
CP0525796
US10080744, Example 18
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C25H26Cl2F3N3O4S3
 1
1 Kd = 474 nM
CP0330311
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-(2-methoxy-2-methylpropyl)-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C25H28F6N4O6S2
 1
1 Kd = 675 nM
CP0516618
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C27H23F7N4O5S2
 1
1 Kd = 831 nM
CP0321517
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-(2-methylpropyl)-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C24H26F6N4O5S2
 1
1 Kd = 949 nM
CP0557575
3-[3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-1,2,4-oxadiazol-5-yl]-2,2-dimethylpropanoic acid
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C24H25Cl2F3N4O5S2
 1
1 Kd = 1000 nM
CP0521150
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-[(2S)-2-methylpiperidine-1-carbonyl]-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C27H29F6N5O6S2
 1
1 Kd = 1121 nM
CP0553969
3-[3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-1,2-oxazol-5-yl]-2,2-dimethylpropanoic acid
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C25H26Cl2F3N3O5S2
 1
1 Kd = 1555 nM
CP0526829
3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C22H25Cl2F3N2O4S2
 1
1 Kd = 1613 nM
CP0341592
3-[4-(cyclobutylmethyl)-5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluorobutan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C24H28F6N2O4S2
 1
1 Kd = 2612 nM
CP0538061
CHEMBL4634072
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C24H23Cl2F3N4O5S2
 1
1 Kd = 2955 nM
CP0339640
US10080744, Example 3/38
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C27H30F6N4O5S2
 1
1 Kd = 4484 nM
CP0557510
US10080744, Example 3/26
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C28H32F6N4O5S2
 1
1 Kd = 5259 nM
CP0330312
2,3-dichloro-4-[4-(4,4-difluoropiperidine-1-carbonyl)-2-[5-(2-hydroxypropan-2-yl)-1,3,4-oxadiazol-2-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C23H22Cl2F5N5O5S2
 1
1 Kd = 9780 nM
Clinical Information about the Protein
Target 1 ( RAR-related orphan receptor-beta (RORB) )
Target Type Patented-recorded Target
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT06515 Nuclear receptor ROR-beta Rattus norvegicus, Rat