Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50329197

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_674873 (CHEMBL1272502)

IC50

140±n/a nM

Citation

Belanger, DB; Williams, MJ; Curran, PJ; Mandal, AK; Meng, Z; Rainka, MP; Yu, T; Shih, NY; Siddiqui, MA; Liu, M; Tevar, S; Lee, S; Liang, L; Gray, K; Yaremko, B; Jones, J; Smith, EB; Prelusky, DB; Basso, AD Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett20:6739-43 (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

BDBM50329197

n/a

Name

BDBM50329197

Synonyms:

3-((R)-1-((2S,6R)-2,6-dimethylmorpholino)ethyl)-N-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)isothiazol-5-amine | CHEMBL1270399

Type

Small organic molecule

Emp. Form.

C21H26N8OS

Mol. Mass.

438.549

SMILES

C[C@@H](N1C[C@H](C)O[C@H](C)C1)c1cc(Nc2nc(C)cn3c(cnc23)-c2cn[nH]c2)sn1 |r|

Structure