General Information of the Protein
Protein ID
PT05980
Protein Name
Exportin-1
Secondarily
Protein Name
Chromosome region maintenance 1 protein homolog
Gene Name
XPO1
Secondarily
Gene Name
CRM1
Sequence
MPAIMTMLADHAARQLLDFSQKLDINLLDNVVNCLYHGEGAQQRMAQEVLTHLKEHPDAWTRVDTILEFSQNMNTKYYGLQILENVIKTRWKILPRNQCEGIKKYVVGLIIKTSSDPTCVEKEKVYIGKLNMILVQILKQEWPKHWPTFISDIVGASRTSESLCQNNMVILKLLSEEVFDFSSGQITQVKSKHLKDSMCNEFSQIFQLCQFVMENSQNAPLVHATLETLLRFLNWIPLGYIFETKLISTLIYKFLNVPMFRNVSLKCLTEIAGVSVSQYEEQFVTLFTLTMMQLKQMLPLNTNIRLAYSNGKDDEQNFIQNLSLFLCTFLKEHDQLIEKRLNLRETLMEALHYMLLVSEVEETEIFKICLEYWNHLAAELYRESPFSTSASPLLSGSQHFDVPPRRQLYLPMLFKVRLLMVSRMAKPEEVLVVENDQGEVVREFMKDTDSINLYKNMRETLVYLTHLDYVDTERIMTEKLHNQVNGTEWSWKNLNTLCWAIGSISGAMHEEDEKRFLVTVIKDLLGLCEQKRGKDNKAIIASNIMYIVGQYPRFLRAHWKFLKTVVNKLFEFMHETHDGVQDMACDTFIKIAQKCRRHFVQVQVGEVMPFIDEILNNINTIICDLQPQQVHTFYEAVGYMIGAQTDQTVQEHLIEKYMLLPNQVWDSIIQQATKNVDILKDPETVKQLGSILKTNVRACKAVGHPFVIQLGRIYLDMLNVYKCLSENISAAIQANGEMVTKQPLIRSMRTVKRETLKLISGWVSRSNDPQMVAENFVPPLLDAVLIDYQRNVPAAREPEVLSTMAIIVNKLGGHITAEIPQIFDAVFECTLNMINKDFEEYPEHRTNFFLLLQAVNSHCFPAFLAIPPTQFKLVLDSIIWAFKHTMRNVADTGLQILFTLLQNVAQEEAAAQSFYQTYFCDILQHIFSVVTDTSHTAGLTMHASILAYMFNLVEEGKISTSLNPGNPVNNQIFLQEYVANLLKSAFPHLQDAQVKLFVTGLFSLNQDIPAFKEHLRDFLVQIKEFAGEDTSDLFLEEREIALRQADEEKHKRQMSVPGIFNPHEIPEEMCD
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Organism
Homo sapiens, Human
Protein Classification
Unclassified protein
Function
Mediates the nuclear export of cellular proteins (cargos) bearing a leucine-rich nuclear export signal (NES) and of RNAs. In the nucleus, in association with RANBP3, binds cooperatively to the NES on its target protein and to the GTPase RAN in its active GTP-bound form (Ran-GTP). Docking of this complex to the nuclear pore complex (NPC) is mediated through binding to nucleoporins. Upon transit of a nuclear export complex into the cytoplasm, disassembling of the complex and hydrolysis of Ran-GTP to Ran-GDP (induced by RANBP1 and RANGAP1, respectively) cause release of the cargo from the export receptor. The directionality of nuclear export is thought to be conferred by an asymmetric distribution of the GTP- and GDP-bound forms of Ran between the cytoplasm and nucleus. Involved in U3 snoRNA transport from Cajal bodies to nucleoli. Binds to late precursor U3 snoRNA bearing a TMG cap.
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Uniprot ID
Primary ID:
O14980

Secondarily ID:
A6NL14
A8K1K5
D6W5E2
Q63HP8
Q68CP3
Q99433
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Ensembl ID
ENSG00000082898
HGNC ID
HGNC:12825
Subcellular Location
Cytoplasm
Nucleus
Nucleoplasm
Nucleus
Cajal body
Nucleus
Nucleolus
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: CL000017 , HeLa
Compound ID Compound Name Compound Formula
CP0948156
2-(3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)prop-1-en-2-yl)-1,3,4-oxadiazole
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C15H9F6N5O
 1
1
EC50 = 230 nM
   TI
   LI
   LO
   TS
CP0948152
isopropyl 2-((3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)methyl)acrylate
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C17H15F6N3O2
 1
1
EC50 = 900 nM
   TI
   LI
   LO
   TS
CP0953292
2-((3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)methyl)-N'-(pyridin-2-yl)acrylohydrazide
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C19H14F6N6O
 1
1
EC50 = 900 nM
   TI
   LI
   LO
   TS
CP0948153
isopropyl 2-((3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)methyl)acrylate
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C17H18F3N3O3
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0948154
2-((3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)methyl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
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C17H12F8N4O
 1
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0958990
ethyl 2-((3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)methyl)acrylate
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C16H16F3N3O3
 1
1
EC50 = 3800 nM
   TI
   LI
   LO
   TS
CP0864823
isopropyl 2-((5-(3,5-bis(trifluoromethyl)phenyl)-2H-tetrazol-2-yl)methyl)acrylate
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C16H14F6N4O2
 1
1
EC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0948155
2-(3-(5-phenyl-2H-tetrazol-2-yl)prop-1-en-2-yl)-1,3,4-oxadiazole
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C12H10N6O
 1
1
EC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0883309
2-((5-phenyl-2H-tetrazol-2-yl)methyl)-1-(piperidin-1-yl)prop-2-en-1-one
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C16H19N5O
 1
1
EC50 > 30000 nM
   TI
   LI
   LO
   TS
CP0942286
ethyl 2-((5-(3-chlorophenyl)-2H-tetrazol-2-yl)methyl)acrylate
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C13H13ClN4O2
 1
1
EC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0953293
ethyl 2-((5-(3-(trifluoromethyl)phenyl)-2H-tetrazol-2-yl)methyl)acrylate
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C14H13F3N4O2
 1
1
EC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0010938
7-Methoxy-8-(3-methyl-but-2-enyl)-chromen-2-one
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C15H16O3
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0414885
8-(3-methylbut-2-enyl)-2H-chromen-2-one
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C14H14O2
 1
1
IC50 = 6400 nM
   TI
   LI
   LO
   TS
CP0036992
2H-chromen-2-one
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C9H6O2
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0070493
7-(methyloxy)-2H-chromen-2-one
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C10H8O3
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
CP0514009
7-methoxy-8-(3-methylbut-2-enyl)-2H-chromen-2-one
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C15H18O3
 1
1
IC50 > 25000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0259362
1-[(S)-[(E)-4-isothiocyanatobut-1-enyl]sulfinyl]-3,5-bis(trifluoromethyl)benzene
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C13H9F6NOS2
 1
1 Kd = 26.95 nM
Clinical Information about the Protein
Target 1 ( Exportin-1 (XPO1) )
Target Type Clinical trial Target
Disease 2 Target-related Diseases  2
1 Multiple myeloma [ICD-11: 2A83]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Selinexor Phase 3
Multiple myeloma
Investigative Drug(s) 1 Investigative Drug  1
1 Octahydrocurcumin Investigative
Solid tumour/cancer