Ki Summary

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50359807

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_791990 (CHEMBL1930050)

IC50

13±n/a nM

Citation

Reader, JC; Matthews, TP; Klair, S; Cheung, KM; Scanlon, J; Proisy, N; Addison, G; Ellard, J; Piton, N; Taylor, S; Cherry, M; Fisher, M; Boxall, K; Burns, S; Walton, MI; Westwood, IM; Hayes, A; Eve, P; Valenti, M; de Haven Brandon, A; Box, G; van Montfort, RL; Williams, DH; Aherne, GW; Raynaud, FI; Eccles, SA; Garrett, MD; Collins, I Structure-guided evolution of potent and selective CHK1 inhibitors through scaffold morphing. J Med Chem54:8328-42 (2011) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Serine/threonine-protein kinase Chk1

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:

MAVPFVEDWDLVQTLGEGAYGEVQLAVNRVTEEAVAVKIVDMKRAVDCPENIKKEICINK
MLNHENVVKFYGHRREGNIQYLFLEYCSGGELFDRIEPDIGMPEPDAQRFFHQLMAGVVY
LHGIGITHRDIKPENLLLDERDNLKISDFGLATVFRYNNRERLLNKMCGTLPYVAPELLK
RREFHAEPVDVWSCGIVLTAMLAGELPWDQPSDSCQEYSDWKEKKTYLNPWKKIDSAPLA
LLHKILVENPSARITIPDIKKDRWYNKPLKKGAKRPRVTSGGVSESPSGFSKHIQSNLDF
SPVNSASSEENVKYSSSQPEPRTGLSLWDTSPSYIDKLVQGISFSQPTCPDHMLLNSQLL
GTPGSSQNPWQRLVKRMTRFFTKLDADKSYQCLKETCEKLGYQWKKSCMNQVTISTTDRR
NNKLIFKVNLLEMDDKILVDFRLSKGDGLEFKRHFLKIKGKLIDIVSSQKIWLPAT

BDBM50359807

n/a

Name

BDBM50359807

Synonyms:

CHEMBL1928705

Type

Small organic molecule

Emp. Form.

C19H19ClN6O

Mol. Mass.

382.847

SMILES

C[C@H](CN(C)C)Oc1nc(Nc2cc3cccc(Cl)c3cn2)cnc1C#N |r|

Structure