Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50325167

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_651698 (CHEMBL1228388)

IC50

3490±n/a nM

Citation

Oza, V; Ashwell, S; Brassil, P; Breed, J; Deng, C; Ezhuthachan, J; Haye, H; Horn, C; Janetka, J; Lyne, P; Newcombe, N; Otterbien, L; Pass, M; Read, J; Roswell, S; Su, M; Toader, D; Yu, D; Yu, Y; Valentine, A; Webborn, P; White, A; Zabludoff, S; Zheng, X Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration. Bioorg Med Chem Lett20:5133-8 (2010) [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

BDBM50325167

n/a

Name

BDBM50325167

Synonyms:

8-(4-(methoxymethyl)phenyl)-5-methyl-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-one | CHEMBL1223390

Type

Small organic molecule

Emp. Form.

C19H17N3O2

Mol. Mass.

319.3572

SMILES

COCc1ccc(cc1)-c1ccc2c(C)cc3n[nH]c(=O)n3c2c1

Structure