Reaction Details Report a problem with these data
Target
Flap endonuclease 1 [1-336]
Ligand
BDBM50157840
Substrate
n/a
Meas. Tech.
Steady-State Kinetics
pH
7.5±n/a
IC50
46.4±4.8 nM
Comments
extracted
Citation
Exell, JC; Thompson, MJ; Finger, LD; Shaw, SJ; Debreczeni, J; Ward, TA; McWhirter, C; Siöberg, CL; Martinez Molina, D; Abbott, WM; Jones, CD; Nissink, JW; Durant, ST; Grasby, JA Cellularly active N-hydroxyurea FEN1 inhibitors block substrate entry to the active site. Nat Chem Biol 12:815-21 (2016) [PubMed] Article
More Info.:
Target
Name:
Flap endonuclease 1 [1-336]
Synonyms:
FEN1 | FEN1_HUMAN | Flap endonuclease 1 (aa 1-336) | RAD2
Type:
Protein
Mol. Mass.:
37858.07
Organism:
Homo sapiens (Human)
Description:
C-terminally truncated after residue 336
Residue:
336
Sequence:
MGIQGLAKLIADVAPSAIRENDIKSYFGRKVAIDASMSIYQFLIAVRQGGDVLQNEEGETTSHLMGMFYRTIRMMENGIKPVYVFDGKPPQLKSGELAKRSERRAEAEKQLQQAQAAGAEQEVEKFTKRLVKVTKQHNDECKHLLSLMGIPYLDAPSEAEASCAALVKAGKVYAAATEDMDCLTFGSPVLMRHLTASEAKKLPIQEFHLSRILQELGLNQEQFVDLCILLGSDYCESIRGIGPKRAVDLIQKHKSIEEIVRRLDPNKYPVPENWLHKEAHQLFLEPEVLDPESVELKWSEPNEEELIKFMCGEKQFSEERIRSGVKRLSKSRQGST
Inhibitor
Name:
BDBM50157840
Synonyms:
1-((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methyl)-3-hydroxythieno[3,2-d]pyrimidine-2,4(1H,3H)-dione (1) | 1-(2,3-Dihydro-benzo[1,4]dioxin-2-ylmethyl)-3-hydroxy-1H-thieno[3,2-d]pyrimidine-2,4-dione | CHEMBL361546
Type:
Small organic molecule
Emp. Form.:
C15H12N2O5S
Mol. Mass.:
332.331
SMILES:
On1c(=O)n(CC2COc3ccccc3O2)c2ccsc2c1=O