General Information of the Protein
Protein ID
PT03628
Protein Name
Endothelial PAS domain-containing protein 1
Secondarily
Protein Name
Basic-helix-loop-helix-PAS protein MOP2
Class E basic helix-loop-helix protein 73
HIF-1-alpha-like factor
Hypoxia-inducible factor 2-alpha
Member of PAS protein 2
PAS domain-containing protein 2
Gene Name
EPAS1
Secondarily
Gene Name
BHLHE73
HIF2A
MOP2
PASD2
Sequence
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLAISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMGLTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRGRTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLDSKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKGQVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTESLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQNFEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCSTPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDFQLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPEHRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTEFLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQDLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHLPLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELTRYDCEVNVPVLGSSTLLQGGDLLRALDQAT
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
Function
Transcription factor involved in the induction of oxygen regulated genes. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBBP and probably EP300. Interaction with redox regulatory protein APEX1 seems to activate CTAD (By similarity).
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Uniprot ID
Primary ID:
Q99814

Secondarily ID:
Q86VA2
Q99630
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HGNC ID
HGNC:3374
Subcellular Location
Nucleus
Nucleus speckle
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: CL000244 , 786-O
Compound ID Compound Name Compound Formula
CP0391143
US10597366, Compound 292
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C17H11F4NO4S
 1
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
CP0331708
US10597366, Compound 185
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C17H9F6NO4S
 1
1
EC50 < 5 nM
   TI
   LI
   LO
   TS
CP0080136
US10597366, Compound 15
   Show/Hide
C17H10F5NO4S
 3
1
EC50 = 6 nM
   TI
   LI
   LO
   TS
2
EC50 = 14 nM
   TI
   LI
   LO
   TS
3
EC50 = 233 nM
   TI
   LI
   LO
   TS
CP0137306
US10597366, Compound 63
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C17H11F4NO4S
 3
1
EC50 = 9 nM
   TI
   LI
   LO
   TS
2
EC50 = 20 nM
   TI
   LI
   LO
   TS
3
EC50 = 182 nM
   TI
   LI
   LO
   TS
CP0440746
(R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy- 1,1-dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)- 5-fluorobenzonitrile
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C16H8F5NO4S
 3
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
2
EC50 = 16 nM
   TI
   LI
   LO
   TS
3
EC50 = 145 nM
   TI
   LI
   LO
   TS
CP0016801
US10597366, Compound 289
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C17H12F3NO4S
 2
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
2
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0198481
4-(Difluoromethyl)-5-(3,5-difluorophenoxy)-2,2- difluoro-3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
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C15H8F6O4S
 1
1
EC50 = 13 nM
   TI
   LI
   LO
   TS
CP0327822
US10597366, Compound 11
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C17H10F5NO4S
 1
1
EC50 = 15 nM
   TI
   LI
   LO
   TS
CP0198480
5-(3-Chloro-5-fluorophenoxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
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C15H8ClF5O4S
 1
1
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0080135
US10597366, Compound 8
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C16H10ClF5O4S
 1
1
EC50 = 20 nM
   TI
   LI
   LO
   TS
CP0198486
US10597366, Compound 163
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C17H12F3NO4S
 4
1
EC50 = 27 nM
   TI
   LI
   LO
   TS
2
EC50 = 41 nM
   TI
   LI
   LO
   TS
3
EC50 = 46 nM
   TI
   LI
   LO
   TS
4
EC50 = 158 nM
   TI
   LI
   LO
   TS
CP0230218
3-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1- dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)-5- fluorobenzonitrile
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C16H8F5NO4S
 1
1
EC50 = 32 nM
   TI
   LI
   LO
   TS
CP0327823
US10597366, Compound 25
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C15H10ClF4NO4S
 3
1
EC50 = 37 nM
   TI
   LI
   LO
   TS
2
EC50 = 65 nM
   TI
   LI
   LO
   TS
3
EC50 = 617 nM
   TI
   LI
   LO
   TS
CP0086461
US10597366, Compound 231
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C17H13F2NO4S
 1
1
EC50 = 39 nM
   TI
   LI
   LO
   TS
CP0569664
4-Bromo-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro- 3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
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C14H7BrClF3O4S
 1
1
EC50 = 43 nM
   TI
   LI
   LO
   TS
CP0068737
3-[[(1S)-7-ethylsulfonyl-2,2-difluoro-1-hydroxy-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile
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C18H14F3NO4S
 1
1
EC50 = 88 nM
   TI
   LI
   LO
   TS
CP0249912
5-(3-Chloro-5-fluorophenoxy)-2,2-difluoro-3- hydroxy-4-(trifluoromethyl)-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
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C15H7ClF6O4S
 1
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
CP0068736
US10597366, Compound 1
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C16H12ClF3O4S
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0080132
4-Chloro-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro- 3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
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C14H7Cl2F3O4S
 1
1
EC50 = 110 nM
   TI
   LI
   LO
   TS
CP0303644
US10597366, Compound 17
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C16H12ClF3O4S
 1
1
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0520066
5-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1- dioxido-2,3-dihydrobenzo[b]thiophen-5- yl)oxy)nicotinonitrile
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C15H8F4N2O4S
 1
1
EC50 = 180 nM
   TI
   LI
   LO
   TS
CP0569663
US10597366, Compound 124
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C14H7ClF6O3S
 1
1
EC50 = 240 nM
   TI
   LI
   LO
   TS
CP0068735
US10597366, Compound 74
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C14H9BrClF3O4S
 1
1
EC50 = 330 nM
   TI
   LI
   LO
   TS
CP0569665
US9884843, Compound 13
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C15H10ClF3O4S
 1
1
EC50 = 340 nM
   TI
   LI
   LO
   TS
CP0169276
US10597366, Compound 41
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C14H9Cl2F3O4S
 1
1
EC50 = 380 nM
   TI
   LI
   LO
   TS
CP0361569
US10597366, Compound 295
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C17H13F2NO4S
 1
1
EC50 = 460 nM
   TI
   LI
   LO
   TS
CP0230642
3-fluoro-5-[[(1S,2S)-2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]oxy]benzonitrile
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C17H13F2NO4S
 1
1
EC50 = 490 nM
   TI
   LI
   LO
   TS
CP0520840
N-(3,5-dimethoxyphenyl)-1,2-benzothiazol-3-amine
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C15H14N2O2S
 1
1
EC50 = 490 nM
   TI
   LI
   LO
   TS
CP0198482
5-((5-Chloropyridin-3-yl)oxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
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C14H8ClF4NO4S
 1
1
EC50 = 630 nM
   TI
   LI
   LO
   TS
CP0381193
VARIOLIN B
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C14H11N7O
 1
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0434611
US10597366, Compound 287
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C17H14FNO4S
 1
1
EC50 = 930 nM
   TI
   LI
   LO
   TS
CP0485579
N-(3-methoxyphenyl)-1,2-benzothiazol-3-amine
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C14H12N2OS
 1
1
EC50 = 1080 nM
   TI
   LI
   LO
   TS
CP0485576
N-(4-methoxyphenyl)-1,2-benzothiazol-3-amine
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C14H12N2OS
 1
1
EC50 = 1120 nM
   TI
   LI
   LO
   TS
CP0441254
HETERONEMIN
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C29H44O6
 1
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
CP0520839
N-(3,5-dibromophenyl)-1,2-benzothiazol-3-amine
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C13H8Br2N2S
 1
1
EC50 = 1350 nM
   TI
   LI
   LO
   TS
CP0533826
N-(3-bromophenyl)-1,2-benzothiazol-3-amine
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C13H9BrN2S
 1
1
EC50 = 1490 nM
   TI
   LI
   LO
   TS
CP0485575
N-(4-bromophenyl)-1,2-benzothiazol-3-amine
   Show/Hide
C13H9BrN2S
 1
1
EC50 = 1610 nM
   TI
   LI
   LO
   TS
CP0485578
N-(3,5-dibromophenyl)-1,1-dioxo-1,2-benzothiazol-3-amine
   Show/Hide
C13H8Br2N2O2S
 1
1
EC50 = 1680 nM
   TI
   LI
   LO
   TS
CP0559835
N-phenyl-1,2-benzothiazol-3-amine
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C13H10N2S
 1
1
EC50 = 1760 nM
   TI
   LI
   LO
   TS
CP0157954
US10597366, Compound 294
   Show/Hide
C17H12F3NO4S
 1
1
EC50 = 1900 nM
   TI
   LI
   LO
   TS
CP0230213
2-bromo-1-(3-chloro-5-fluorophenoxy)-4-(difluoromethylsulfonyl)benzene
   Show/Hide
C13H7BrClF3O3S
 1
1
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0441842
(2-formyl-7-methoxy-6-methyl-5,8-dioxo-1H-isoquinolin-1-yl)methyl (Z)-2-methylbut-2-enoate
   Show/Hide
C18H19NO6
 1
1
EC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0483093
(1S)-4-(3-chloro-5-fluorophenoxy)-7-(difluoromethylsulfonyl)-2,3-dihydro-1H-inden-1-ol
   Show/Hide
C16H12ClF3O4S
 1
1
EC50 = 2900 nM
   TI
   LI
   LO
   TS
CP0533827
N-(3,5-dichlorophenyl)-1,2-benzothiazol-3-amine
   Show/Hide
C13H8Cl2N2S
 1
1
EC50 = 2920 nM
   TI
   LI
   LO
   TS
CP0520836
N-(3,5-difluorophenyl)-1,2-benzothiazol-3-amine
   Show/Hide
C13H8F2N2S
 1
1
EC50 = 2980 nM
   TI
   LI
   LO
   TS
CP0778426
Puupehenone
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C21H28O3
 1
1
EC50 = 3300 nM
   TI
   LI
   LO
   TS
CP0330080
2-chloro-1-(3-chloro-5-fluorophenoxy)-4-(trifluoromethylsulfonyl)benzene
   Show/Hide
C13H6Cl2F4O3S
 1
1
EC50 = 3400 nM
   TI
   LI
   LO
   TS
CP0303643
2-bromo-1-(3-chloro-5-fluorophenoxy)-4-(trifluoromethylsulfonyl)benzene
   Show/Hide
C13H6BrClF4O3S
 1
1
EC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0493627
[(4aR,4bS,6S,6aS,7R,10aS,10bS,12aS)-8-acetyl-4a,7-diformyl-1,1,6a,10b-tetramethyl-2,3,4,4b,5,6,7,10,10a,11,12,12a-dodecahydrochrysen-6-yl] acetate
   Show/Hide
C28H40O5
 1
1
EC50 = 4200 nM
   TI
   LI
   LO
   TS
CP0559836
N-(3-bromophenyl)-1,1-dioxo-1,2-benzothiazol-3-amine
   Show/Hide
C13H9BrN2O2S
 1
1
EC50 = 5620 nM
   TI
   LI
   LO
   TS
CP0471767
US9884843, Compound 6
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C14H9BrClFO4S
 1
1
EC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0381197
(3S,4E,14S,17E,21Z,27Z,42E,44R)-hexatetraconta-4,17,21,27,42-pentaen-1,12,15,45-tetrayne-3,14,44-triol
   Show/Hide
C46H68O3
 1
1
EC50 = 8700 nM
   TI
   LI
   LO
   TS
CP0159106
US9884843, Compound 10
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C15H7ClF3NO4S
 1
1
EC50 = 9200 nM
   TI
   LI
   LO
   TS
CP0331707
2-(3-chloro-5-fluorophenoxy)-5-(trifluoromethylsulfonyl)benzonitrile
   Show/Hide
C14H6ClF4NO3S
 1
1
EC50 = 11600 nM
   TI
   LI
   LO
   TS
CP0412833
(1S,2E,4E,6S,7R,12S,14S,20R,22S,27R)-15,19-diazapentacyclo[18.7.0.06,14.07,12.022,27]heptacosa-2,4-diene
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C25H40N2
 1
1
EC50 = 14800 nM
   TI
   LI
   LO
   TS
CP0081187
AAPTAMINE
   Show/Hide
C13H12N2O2
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0218443
XESTOQUINONE
   Show/Hide
C20H14O4
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0388081
MIMOSAMYCIN
   Show/Hide
C13H13NO4
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0412543
[(1S,2R,5S,10R,11S,13R,16S,17S,18S,20S)-17-acetyl-18-hydroxy-2,6,6,20-tetramethyl-15-oxo-14-oxapentacyclo[11.6.1.02,11.05,10.016,20]icosan-10-yl]methyl acetate
   Show/Hide
C28H42O6
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0848947
O-demethylrenierone
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C16H15NO5
 1
1
EC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0339627
3-chloro-5-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]benzonitrile
   Show/Hide
C15H10ClF2NO3S2
 1
1
IC50 = 50 nM
   TI
   LI
   LO
   TS
CP0139152
(4S)-1-(3,5-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol
   Show/Hide
C14H10F4O3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0349805
4-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]-2-fluorobenzonitrile
   Show/Hide
C15H10F3NO3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0516480
6-chloro-4-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-1-yl]pyridine-2-carbonitrile
   Show/Hide
C15H11ClF2N2O3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0565364
(4S)-5,5-difluoro-3-methylsulfonyl-1-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]-6,7-dihydro-4H-2-benzothiophen-4-ol
   Show/Hide
C14H13F5N2O3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
CP0572217
(4S)-1-(2,6-difluoropyridin-4-yl)-5,5-difluoro-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol
   Show/Hide
C14H11F4NO3S2
 1
1
IC50 > 1000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0068736
US10597366, Compound 1
   Show/Hide
C16H12ClF3O4S
 1
1 IC50 < 5 nM
CP0080135
US10597366, Compound 8
   Show/Hide
C16H10ClF5O4S
 1
1 IC50 < 5 nM
CP0080136
US10597366, Compound 15
   Show/Hide
C17H10F5NO4S
 1
1 IC50 < 5 nM
CP0137306
US10597366, Compound 63
   Show/Hide
C17H11F4NO4S
 1
1 IC50 < 5 nM
CP0198480
5-(3-Chloro-5-fluorophenoxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
   Show/Hide
C15H8ClF5O4S
 1
1 IC50 < 5 nM
CP0249912
5-(3-Chloro-5-fluorophenoxy)-2,2-difluoro-3- hydroxy-4-(trifluoromethyl)-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
   Show/Hide
C15H7ClF6O4S
 1
1 IC50 < 5 nM
CP0303644
US10597366, Compound 17
   Show/Hide
C16H12ClF3O4S
 1
1 IC50 < 5 nM
CP0331708
US10597366, Compound 185
   Show/Hide
C17H9F6NO4S
 1
1 IC50 < 5 nM
CP0440746
(R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy- 1,1-dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)- 5-fluorobenzonitrile
   Show/Hide
C16H8F5NO4S
 1
1 IC50 < 5 nM
CP0569664
4-Bromo-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro- 3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
   Show/Hide
C14H7BrClF3O4S
 1
1 IC50 < 5 nM
CP0016801
US10597366, Compound 289
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C17H12F3NO4S
 1
1 IC50 = 9 nM
CP0391143
US10597366, Compound 292
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C17H11F4NO4S
 1
1 IC50 = 9 nM
CP0327822
US10597366, Compound 11
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C17H10F5NO4S
 1
1 IC50 = 10 nM
CP0198481
4-(Difluoromethyl)-5-(3,5-difluorophenoxy)-2,2- difluoro-3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
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C15H8F6O4S
 1
1 IC50 = 11 nM
CP0198486
US10597366, Compound 163
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C17H12F3NO4S
 1
1 IC50 = 12 nM
CP0230218
3-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1- dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)-5- fluorobenzonitrile
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C16H8F5NO4S
 1
1 IC50 = 14 nM
CP0080132
4-Chloro-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro- 3-hydroxy-2,3-dihydrobenzo[b]thiophene 1,1-dioxide
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C14H7Cl2F3O4S
 1
1 IC50 = 20 nM
CP0569665
US9884843, Compound 13
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C15H10ClF3O4S
 1
1 IC50 = 20 nM
CP0068737
3-[[(1S)-7-ethylsulfonyl-2,2-difluoro-1-hydroxy-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile
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C18H14F3NO4S
 1
1 IC50 = 31 nM
CP0331707
2-(3-chloro-5-fluorophenoxy)-5-(trifluoromethylsulfonyl)benzonitrile
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C14H6ClF4NO3S
 1
1 IC50 = 34 nM
CP0086461
US10597366, Compound 231
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C17H13F2NO4S
 1
1 IC50 = 41 nM
CP0169276
US10597366, Compound 41
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C14H9Cl2F3O4S
 1
1 IC50 = 46 nM
CP0159106
US9884843, Compound 10
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C15H7ClF3NO4S
 1
1 IC50 = 49 nM
CP0139152
(4S)-1-(3,5-difluorophenyl)-5,5-difluoro-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-4-ol
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C14H10F4O3S2
 1
1 IC50 < 50 nM
CP0339627
3-chloro-5-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]benzonitrile
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C15H10ClF2NO3S2
 1
1 IC50 < 50 nM
CP0349805
4-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-4,6-dihydrocyclopenta[c]thiophen-1-yl]-2-fluorobenzonitrile
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C15H10F3NO3S2
 1
1 IC50 = 50 nM
CP0516480
6-chloro-4-[(4S)-5,5-difluoro-4-hydroxy-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-1-yl]pyridine-2-carbonitrile
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C15H11ClF2N2O3S2
 1
1 IC50 < 50 nM
CP0572217
(4S)-1-(2,6-difluoropyridin-4-yl)-5,5-difluoro-3-methylsulfonyl-6,7-dihydro-4H-2-benzothiophen-4-ol
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C14H11F4NO3S2
 1
1 IC50 < 50 nM
CP0068735
US10597366, Compound 74
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C14H9BrClF3O4S
 1
1 IC50 = 55 nM
CP0327823
US10597366, Compound 25
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C15H10ClF4NO4S
 1
1 IC50 = 60 nM
CP0330080
2-chloro-1-(3-chloro-5-fluorophenoxy)-4-(trifluoromethylsulfonyl)benzene
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C13H6Cl2F4O3S
 1
1 IC50 = 140 nM
CP0520066
5-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1- dioxido-2,3-dihydrobenzo[b]thiophen-5- yl)oxy)nicotinonitrile
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C15H8F4N2O4S
 1
1 IC50 = 140 nM
CP0434611
US10597366, Compound 287
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C17H14FNO4S
 1
1 IC50 = 160 nM
CP0303643
2-bromo-1-(3-chloro-5-fluorophenoxy)-4-(trifluoromethylsulfonyl)benzene
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C13H6BrClF4O3S
 1
1 IC50 = 170 nM
CP0230213
2-bromo-1-(3-chloro-5-fluorophenoxy)-4-(difluoromethylsulfonyl)benzene
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C13H7BrClF3O3S
 1
1 IC50 = 180 nM
CP0361569
US10597366, Compound 295
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C17H13F2NO4S
 1
1 IC50 = 210 nM
CP0569663
US10597366, Compound 124
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C14H7ClF6O3S
 1
1 IC50 = 220 nM
CP0198482
5-((5-Chloropyridin-3-yl)oxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide
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C14H8ClF4NO4S
 1
1 IC50 = 350 nM
CP0230642
3-fluoro-5-[[(1S,2S)-2-fluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]oxy]benzonitrile
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C17H13F2NO4S
 1
1 IC50 = 350 nM
CP0483093
(1S)-4-(3-chloro-5-fluorophenoxy)-7-(difluoromethylsulfonyl)-2,3-dihydro-1H-inden-1-ol
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C16H12ClF3O4S
 1
1 IC50 = 460 nM
CP0157954
US10597366, Compound 294
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C17H12F3NO4S
 1
1 IC50 = 1900 nM
CP0471767
US9884843, Compound 6
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C14H9BrClFO4S
 1
1 IC50 = 2400 nM
CP0565364
(4S)-5,5-difluoro-3-methylsulfonyl-1-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]-6,7-dihydro-4H-2-benzothiophen-4-ol
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C14H13F5N2O3S2
 1
1 IC50 > 1000 nM
Clinical Information about the Protein
Target 1 ( HIF2-alpha messenger RNA (EPAS1 mRNA) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Recurrent glioblastoma [ICD-11: 2A00.00]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PT2385 Phase 2
Recurrent glioblastoma
Target 2 ( Hypoxia-inducible factor 2 alpha (HIF-2A) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Recurrent glioblastoma [ICD-11: 2A00.00]
2 Renal cell carcinoma [ICD-11: 2C90]
Approved Drug(s) 1 Approved Drug  1
1 Belzutifan Approved
Renal cell carcinoma
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PT2385 Phase 2
Recurrent glioblastoma