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Target
Hypoxia-inducible factor 1-alpha inhibitor
Ligand
BDBM50495468
Substrate
n/a
Meas. Tech.
ChEMBL_1287193 (CHEMBL3112250)
IC50
>100000±n/a nM
Citation
 Rotili, D; Tomassi, S; Conte, M; Benedetti, R; Tortorici, M; Ciossani, G; Valente, S; Marrocco, B; Labella, D; Novellino, E; Mattevi, A; Altucci, L; Tumber, A; Yapp, C; King, ON; Hopkinson, RJ; Kawamura, A; Schofield, CJ; Mai, A Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities. J Med Chem 57:42-55 (2014) [PubMed]  Article 
Target
Name:
Hypoxia-inducible factor 1-alpha inhibitor
Synonyms:
FIH1 | HIF1AN | HIF1N_HUMAN | Hypoxia-inducible factor 1 (FIH) | Hypoxia-inducible factor 1-alpha inhibitor
Type:
Enzyme
Mol. Mass.:
40278.92
Organism:
Homo sapiens (Human)
Description:
Q9NWT6
Residue:
349
Sequence:
MAATAAEAVASGSGEPREEAGALGPAWDESQLRSYSFPTRPIPRLSQSDPRAEELIENEEPVVLTDTNLVYPALKWDLEYLQENIGNGDFSVYSASTHKFLYYDEKKMANFQNFKPRSNREEMKFHEFVEKLQDIQQRGGEERLYLQQTLNDTVGRKIVMDFLGFNWNWINKQQGKRGWGQLTSNLLLIGMEGNVTPAHYDEQQNFFAQIKGYKRCILFPPDQFECLYPYPVHHPCDRQSQVDFDNPDYERFPNFQNVVGYETVVGPGDVLYIPMYWWHHIESLLNGGITITVNFWYKGAPTPKRIEYPLKAHQKVAIMRNIEKMLGEALGNPQEVGPLLNTMIKGRYN
  
Inhibitor
Name:
BDBM50495468
Synonyms:
CHEMBL3108958
Type:
Small organic molecule
Emp. Form.:
C23H19F3N4O5
Mol. Mass.:
488.416
SMILES:
OC(=O)C(F)(F)F.N[C@@H]1C[C@H]1c1ccc(NC(=O)c2ccnc(c2)-c2cc(ccn2)C(O)=O)cc1 |r|
Structure:
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