Reaction Details Report a problem with these data
Target
Eukaryotic initiation factor 4A-I
Ligand
BDBM50540861
Substrate
n/a
Meas. Tech.
ChEMBL_1983235 (CHEMBL4616497)
IC50
6.3±n/a nM
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 Chem 63:5879-5955 (2020) [PubMed]  Article 
Target
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:
MSASQDSRSRDNGPDGMEPEGVIESNWNEIVDSFDDMNLSESLLRGIYAYGFEKPSAIQQRAILPCIKGYDVIAQAQSGTGKTATFAISILQQIELDLKATQALVLAPTRELAQQIQKVVMALGDYMGASCHACIGGTNVRAEVQKLQMEAPHIIVGTPGRVFDMLNRRYLSPKYIKMFVLDEADEMLSRGFKDQIYDIFQKLNSNTQVVLLSATMPSDVLEVTKKFMRDPIRILVKKEELTLEGIRQFYINVEREEWKLDTLCDLYETLTITQAVIFINTRRKVDWLTEKMHARDFTVSAMHGDMDQKERDVIMREFRSGSSRVLITTDLLARGIDVQQVSLVINYDLPTNRENYIHRIGRGGRFGRKGVAINMVTEEDKRTLRDIETFYNTSIEEMPLNVADLI
  
Inhibitor
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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