Reaction Details |
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Target | Eukaryotic initiation factor 4A-I |
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Ligand | BDBM50540861 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1983226 (CHEMBL4616488) |
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IC50 | 92±n/a nM |
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Citation | Ernst, JT; Thompson, PA; Nilewski, C; Sprengeler, PA; Sperry, S; Packard, G; Michels, T; Xiang, A; Tran, C; Wegerski, CJ; Eam, B; Young, NP; Fish, S; Chen, J; Howard, H; Staunton, J; Molter, J; Clarine, J; Nevarez, A; Chiang, GG; Appleman, JR; Webster, KR; Reich, SH Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase. J Med Chem63:5879-5955 (2020) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Eukaryotic initiation factor 4A-I |
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Name: | Eukaryotic initiation factor 4A-I |
Synonyms: | ATP-dependent RNA helicase eIF4A-1 | DDX2A | EIF4A | EIF4A1 | IF4A1_HUMAN | eIF-4A-I | eIF4A-I |
Type: | PROTEIN |
Mol. Mass.: | 46146.87 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_864983 |
Residue: | 406 |
Sequence: | MSASQDSRSRDNGPDGMEPEGVIESNWNEIVDSFDDMNLSESLLRGIYAYGFEKPSAIQQ
RAILPCIKGYDVIAQAQSGTGKTATFAISILQQIELDLKATQALVLAPTRELAQQIQKVV
MALGDYMGASCHACIGGTNVRAEVQKLQMEAPHIIVGTPGRVFDMLNRRYLSPKYIKMFV
LDEADEMLSRGFKDQIYDIFQKLNSNTQVVLLSATMPSDVLEVTKKFMRDPIRILVKKEE
LTLEGIRQFYINVEREEWKLDTLCDLYETLTITQAVIFINTRRKVDWLTEKMHARDFTVS
AMHGDMDQKERDVIMREFRSGSSRVLITTDLLARGIDVQQVSLVINYDLPTNRENYIHRI
GRGGRFGRKGVAINMVTEEDKRTLRDIETFYNTSIEEMPLNVADLI
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BDBM50540861 |
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n/a |
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Name | BDBM50540861 |
Synonyms: | EFT-226 | Eft226 | Zotatifin |
Type | Small organic molecule |
Emp. Form. | C28H29N3O5 |
Mol. Mass. | 487.547 |
SMILES | COc1cc2O[C@]3([C@@H]([C@@H](CN(C)C)[C@@H](O)[C@@]3(O)c2c(OC)n1)c1ccccc1)c1ccc(cc1)C#N |
Structure |
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