General Information of the Protein
Protein ID
PT02717
Protein Name
Eukaryotic initiation factor 4A-I
Secondarily
Protein Name
ATP-dependent RNA helicase eIF4A-1
Gene Name
EIF4A1
Secondarily
Gene Name
DDX2A
EIF4A
Sequence
MSASQDSRSRDNGPDGMEPEGVIESNWNEIVDSFDDMNLSESLLRGIYAYGFEKPSAIQQRAILPCIKGYDVIAQAQSGTGKTATFAISILQQIELDLKATQALVLAPTRELAQQIQKVVMALGDYMGASCHACIGGTNVRAEVQKLQMEAPHIIVGTPGRVFDMLNRRYLSPKYIKMFVLDEADEMLSRGFKDQIYDIFQKLNSNTQVVLLSATMPSDVLEVTKKFMRDPIRILVKKEELTLEGIRQFYINVEREEWKLDTLCDLYETLTITQAVIFINTRRKVDWLTEKMHARDFTVSAMHGDMDQKERDVIMREFRSGSSRVLITTDLLARGIDVQQVSLVINYDLPTNRENYIHRIGRGGRFGRKGVAINMVTEEDKRTLRDIETFYNTSIEEMPLNVADLI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Hydrolase
Function
ATP-dependent RNA helicase which is a subunit of the eIF4F complex involved in cap recognition and is required for mRNA binding to ribosome. In the current model of translation initiation, eIF4A unwinds RNA secondary structures in the 5'-UTR of mRNAs which is necessary to allow efficient binding of the small ribosomal subunit, and subsequent scanning for the initiator codon.
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Uniprot ID
Primary ID:
P60842

Secondarily ID:
B2R6L8
D3DTP9
J3QLC4
P04765
Q5U018
Q61516
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Ensembl ID
ENSG00000161960
HGNC ID
HGNC:3282
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: CL000111 , MDA-MB-231
Compound ID Compound Name Compound Formula
CP0397395
dimethyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2,6-dicarboxylate
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C29H28O9
 2
1
EC50 = 0.2 nM
   TI
   LI
   LO
   TS
2
EC50 = 4 nM
   TI
   LI
   LO
   TS
CP0453495
(1R,2R,3S,3aR,8bS)-6-chloro-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C28H28ClNO6
 2
1
EC50 = 0.6 nM
   TI
   LI
   LO
   TS
2
EC50 = 15 nM
   TI
   LI
   LO
   TS
CP0118102
methyl (1R,2R,3S,3aR,8bS)-6-[[(2S,3R,6R)-6-[(1R)-1,2-dihydroxyethyl]-3-methoxy-1,4-dioxan-2-yl]oxy]-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C34H38O13
 2
1
EC50 = 0.8 nM
   TI
   LI
   LO
   TS
2
EC50 = 7 nM
   TI
   LI
   LO
   TS
CP0453494
(1R,2R,3S,3aR,8bS)-6-cyano-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C29H28N2O6
 2
1
EC50 = 0.8 nM
   TI
   LI
   LO
   TS
2
EC50 = 35 nM
   TI
   LI
   LO
   TS
CP0462863
methyl (1R,2R,3S,3aR,8bS)-6-cyano-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C28H25NO7
 2
1
EC50 = 0.9 nM
   TI
   LI
   LO
   TS
2
EC50 = 15 nM
   TI
   LI
   LO
   TS
CP0423624
methyl (1R,2R,3S,3aR,8bS)-6-acetyl-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C29H28O8
 2
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
2
EC50 = 30 nM
   TI
   LI
   LO
   TS
CP0462855
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,3R,6S)-6-(2-hydroxyethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C34H38O12
 2
1
EC50 = 1 nM
   TI
   LI
   LO
   TS
2
EC50 = 5 nM
   TI
   LI
   LO
   TS
CP0397393
(1R,2R,3S,3aR,8bS)-3a-(4-cyanophenyl)-1,8b-dihydroxy-6,8-dimethoxy-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C29H28N2O6
 2
1
EC50 = 1.2 nM
   TI
   LI
   LO
   TS
2
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0423642
methyl (1R,2R,3S,3aR,8bS)-3a-(4-cyanophenyl)-1,8b-dihydroxy-6,8-dimethoxy-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C28H25NO7
 2
1
EC50 = 2 nM
   TI
   LI
   LO
   TS
2
EC50 = 17 nM
   TI
   LI
   LO
   TS
CP0397396
(1R,2R,3S,3aR,8bS)-6-[[(2S,3R,6R)-6-[(1S)-1,2-dihydroxyethyl]-3-methoxy-1,4-dioxan-2-yl]oxy]-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C35H41NO12
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 = 19 nM
   TI
   LI
   LO
   TS
CP0423625
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,6S)-6-(hydroxymethyl)-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C32H34O11
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 = 40 nM
   TI
   LI
   LO
   TS
CP0423630
methyl (1R,2R,3S,3aR,8bS)-6-[[(2S,6R)-6-[(1R)-1,2-dihydroxyethyl]-1,4-dioxan-2-yl]oxy]-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O12
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 = 14 nM
   TI
   LI
   LO
   TS
CP0423641
(1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,6S)-6-(hydroxymethyl)-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C33H37NO10
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 = 23 nM
   TI
   LI
   LO
   TS
CP0462854
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,3R,6S)-6-(hydroxymethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O12
 2
1
EC50 = 3 nM
   TI
   LI
   LO
   TS
2
EC50 = 60 nM
   TI
   LI
   LO
   TS
CP0397384
methyl (1R,2R,3S,3aR,8bS)-6-chloro-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C27H25ClO7
 2
1
EC50 = 4 nM
   TI
   LI
   LO
   TS
2
EC50 = 70 nM
   TI
   LI
   LO
   TS
CP0453491
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6,8-dimethoxy-3a-(4-methylphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C28H28O7
 2
1
EC50 = 5 nM
   TI
   LI
   LO
   TS
2
EC50 > 100 nM
   TI
   LI
   LO
   TS
CP0304472
AGLAFOLIN
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C28H28O8
 2
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
2
EC50 = 90 nM
   TI
   LI
   LO
   TS
CP0423643
methyl (1R,2R,3S,3aR,8bS)-1,6,8b-trihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C27H26O8
 2
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
2
EC50 = 200 nM
   TI
   LI
   LO
   TS
CP0493559
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-6-(methylamino)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C28H29NO7
 2
1
EC50 = 11 nM
   TI
   LI
   LO
   TS
2
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0397385
methyl (1R,2R,3S,3aR,8bS)-6-carbamoyl-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C28H27NO8
 2
1
EC50 = 29 nM
   TI
   LI
   LO
   TS
2
EC50 = 450 nM
   TI
   LI
   LO
   TS
CP0397394
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2R,3R,6S)-6-(hydroxymethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O12
 2
1
EC50 = 35 nM
   TI
   LI
   LO
   TS
2
EC50 = 240 nM
   TI
   LI
   LO
   TS
CP0423628
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,3S,6S)-6-(2-hydroxyethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C34H38O12
 2
1
EC50 = 35 nM
   TI
   LI
   LO
   TS
2
EC50 = 275 nM
   TI
   LI
   LO
   TS
CP0462853
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-6-(methylcarbamoyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C29H29NO8
 2
1
EC50 = 35 nM
   TI
   LI
   LO
   TS
2
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0397388
methyl (1R,2R,3S,3aR,8bS)-6-amino-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C27H27NO7
 2
1
EC50 = 40 nM
   TI
   LI
   LO
   TS
2
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0453490
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[(2S,6S)-6-(hydroxymethyl)oxan-2-yl]oxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O10
 2
1
EC50 = 50 nM
   TI
   LI
   LO
   TS
2
EC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0397392
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[(2S,6S)-6-(hydroxymethyl)morpholin-2-yl]oxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C32H35NO10
 2
1
EC50 = 80 nM
   TI
   LI
   LO
   TS
2
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0397383
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2R,3S,6S)-6-(2-hydroxyethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
   Show/Hide
C34H38O12
 2
1
EC50 = 120 nM
   TI
   LI
   LO
   TS
2
EC50 > 2000 nM
   TI
   LI
   LO
   TS
CP0462852
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2S,3S,6S)-6-(hydroxymethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O12
 2
1
EC50 = 170 nM
   TI
   LI
   LO
   TS
2
EC50 > 2500 nM
   TI
   LI
   LO
   TS
CP0423640
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2R,3R,6S)-6-(2-hydroxyethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C34H38O12
 2
1
EC50 > 200 nM
   TI
   LI
   LO
   TS
2
EC50 > 3500 nM
   TI
   LI
   LO
   TS
CP0397390
(1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-2-methoxycarbonyl-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-6-carboxylic acid
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C28H26O9
 2
1
EC50 > 1000 nM
   TI
   LI
   LO
   TS
2
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0397381
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C27H26O7
 2
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
2
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0397382
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[[(2R,3S,6S)-6-(hydroxymethyl)-3-methoxy-1,4-dioxan-2-yl]oxy]-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C33H36O12
 2
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
2
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0397387
methyl (1R,2R,3S,3aR,8bS)-6-(dimethylamino)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
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C29H31NO7
 2
1
EC50 > 2000 nM
   TI
   LI
   LO
   TS
2
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0423636
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-(methanesulfonamido)-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
   Show/Hide
C28H29NO9S
 1
1
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0423637
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-6-methyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
   Show/Hide
C28H28O7
 1
1
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0423639
methyl (1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6-[(2S,6S)-6-(hydroxymethyl)-4-methylmorpholin-2-yl]oxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
   Show/Hide
C33H37NO10
 1
1
EC50 > 5000 nM
   TI
   LI
   LO
   TS
CP0453523
methyl (1R,2R,3S,3aR,8bS)-6-(dimethylcarbamoyl)-1,8b-dihydroxy-8-methoxy-3a-(4-methoxyphenyl)-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxylate
   Show/Hide
C30H31NO8
 1
1
EC50 > 5000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0100905
EFT-226
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C28H29N3O5
 4
1 Kd = 21 nM
2 Kd = 2430 nM
3 Kd = 3190 nM
4 Kd = 9600 nM
CP0078717
(1R,2R,3S,3aR,8bS)-1,8b-dihydroxy-6,8-dimethoxy-3a-(4-methoxyphenyl)-N,N-dimethyl-3-phenyl-2,3-dihydro-1H-cyclopenta[b][1]benzofuran-2-carboxamide
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C29H31NO7
 1
1 Kd = 156 nM