Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50195209

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_424833 (CHEMBL908460)

IC50

1.1±n/a nM

Citation

Huang, S; Garbaccio, RM; Fraley, ME; Steen, J; Kreatsoulas, C; Hartman, G; Stirdivant, S; Drakas, B; Rickert, K; Walsh, E; Hamilton, K; Buser, CA; Hardwick, J; Mao, X; Abrams, M; Beck, S; Tao, W; Lobell, R; Sepp-Lorenzino, L; Yan, Y; Ikuta, M; Murphy, JZ; Sardana, V; Munshi, S; Kuo, L; Reilly, M; Mahan, E Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors. Bioorg Med Chem Lett16:5907-12 (2006) [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

BDBM50195209

n/a

Name

BDBM50195209

Synonyms:

6-(1-methyl-1H-pyrazol-4-yl)-3-(5-(piperidin-1-ylmethyl)-1H-indol-2-yl)quinolin-2(1H)-one | CHEMBL221864

Type

Small organic molecule

Emp. Form.

C27H27N5O

Mol. Mass.

437.5362

SMILES

Cn1cc(cn1)-c1ccc2[nH]c(=O)c(cc2c1)-c1cc2cc(CN3CCCCC3)ccc2[nH]1

Structure