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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50499153
Substrate
n/a
Meas. Tech.
ChEMBL_1537758 (CHEMBL3737515)
IC50
274±n/a nM
Citation
 Sestito, S; Nesi, G; Daniele, S; Martelli, A; Digiacomo, M; Borghini, A; Pietra, D; Calderone, V; Lapucci, A; Falasca, M; Parrella, P; Notarangelo, A; Breschi, MC; Macchia, M; Martini, C; Rapposelli, S Design and synthesis of 2-oxindole based multi-targeted inhibitors of PDK1/Akt signaling pathway for the treatment of glioblastoma multiforme. Eur J Med Chem 105:274-88 (2015) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase Chk1
Synonyms:
CHEK1 | CHK1 | CHK1 checkpoint homolog | CHK1_HUMAN | Checkpoint kinase-1 (CHK1)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
54443.02
Organism:
Homo sapiens (Human)
Description:
gi_166295192
Residue:
476
Sequence:
MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINKMLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVYLHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLKRREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLALLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDFSPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLLGTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRRNNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT
  
Inhibitor
Name:
BDBM50499153
Synonyms:
CHEMBL3091673
Type:
Small organic molecule
Emp. Form.:
C25H25N5O4
Mol. Mass.:
459.4971
SMILES:
COc1cc2CCN(CC(=O)Nc3ccc4NC(=O)\C(=C/c5cnc[nH]5)c4c3)Cc2cc1OC
Structure:
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