Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50204290
Substrate
n/a
Meas. Tech.
ChEMBL_1627206 (CHEMBL3869727)
IC50
50±n/a nM
Citation
 Lam, BArikawa, YCramlett, JDong, Qde Jong, RFeher, VGrimshaw, CEFarrell, PJHoffman, IDJennings, AJones, BMatuszkiewicz, JMiura, JMiyake, HNatala, SRShi, LTakahashi, MTaylor, EWyrick, CYano, JZalevsky, JNie, Z Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett 26:5947-5950 (2016) [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:
BDBM50204290
Synonyms:
CHEMBL3979920 | US11077111, Compound IIIa | US20230295171, Example 102
Type:
Small organic molecule
Emp. Form.:
C17H21FN6O
Mol. Mass.:
344.3866
SMILES:
Cn1cc(cn1)-c1nc(N[C@@H]2CCCC[C@@H]2N)c(F)c2CNC(=O)c12 |r|
Structure:
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