Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50223485

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_458175 (CHEMBL924433)

IC50

2±n/a nM

Citation

Garbaccio, RM; Huang, S; Tasber, ES; Fraley, ME; Yan, Y; Munshi, S; Ikuta, M; Kuo, L; Kreatsoulas, C; Stirdivant, S; Drakas, B; Rickert, K; Walsh, ES; Hamilton, KA; Buser, CA; Hardwick, J; Mao, X; Beck, SC; Abrams, MT; Tao, W; Lobell, R; Sepp-Lorenzino, L; Hartman, GD Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase. Bioorg Med Chem Lett17:6280-5 (2007) [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

BDBM50223485

n/a

Name

BDBM50223485

Synonyms:

6-(3-aminopropyl)-N-(2-(dimethylamino)ethyl)-1-oxo-1,2-dihydrobenzo[h]isoquinoline-9-carboxamide | CHEMBL249238

Type

Small organic molecule

Emp. Form.

C21H26N4O2

Mol. Mass.

366.4567

SMILES

CN(C)CCNC(=O)c1ccc2c(CCCN)cc3cc[nH]c(=O)c3c2c1

Structure