Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50245691

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_511069 (CHEMBL1000361)

IC50

2±n/a nM

Citation

Smaill, JB; Baker, EN; Booth, RJ; Bridges, AJ; Dickson, JM; Dobrusin, EM; Ivanovic, I; Kraker, AJ; Lee, HH; Lunney, EA; Ortwine, DF; Palmer, BD; Quin, J; Squire, CJ; Thompson, AM; Denny, WA Synthesis and structure-activity relationships of N-6 substituted analogues of 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as inhibitors of Wee1 and Chk1 checkpoint kinases. Eur J Med Chem43:1276-96 (2008) [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

BDBM50245691

n/a

Name

BDBM50245691

Synonyms:

9-hydroxy-6-(3-(methylamino)propyl)-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione | CHEMBL455192

Type

Small organic molecule

Emp. Form.

C24H21N3O3

Mol. Mass.

399.4418

SMILES

CNCCCn1c2ccc(O)cc2c2c3C(=O)NC(=O)c3c(cc12)-c1ccccc1

Structure