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Target
Serine/threonine-protein kinase Chk1
Ligand
BDBM50555406
Substrate
n/a
Meas. Tech.
ChEMBL_2051920 (CHEMBL4706921)
IC50
5.2±n/a nM
Citation
Osborne, JD; Matthews, TP; McHardy, T; Proisy, N; Cheung, KM; Lainchbury, M; Brown, N; Walton, MI; Eve, PD; Boxall, KJ; Hayes, A; Henley, AT; Valenti, MR; De Haven Brandon, AK; Box, G; Jamin, Y; Robinson, SP; Westwood, IM; van Montfort, RL; Leonard, PM; Lamers, MB; Reader, JC; Aherne, GW; Raynaud, FI; Eccles, SA; Garrett, MD; Collins, I Multiparameter Lead Optimization to Give an Oral Checkpoint Kinase 1 (CHK1) Inhibitor Clinical Candidate: (R)-5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile (CCT245737). J Med Chem 59:5221-37 (2016) [PubMed] Article
More Info.:
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