Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50214577

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_457402 (CHEMBL941921)

IC50

1.6±n/a nM

Citation

Tong, Y; Przytulinska, M; Tao, ZF; Bouska, J; Stewart, KD; Park, C; Li, G; Claiborne, A; Kovar, P; Chen, Z; Merta, PJ; Bui, MH; Olson, A; Osterling, D; Zhang, H; Sham, HL; Rosenberg, SH; Sowin, TJ; Lin, NH Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability. Bioorg Med Chem Lett17:5665-70 (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

BDBM50214577

n/a

Name

BDBM50214577

Synonyms:

4'-(6,7-dimethoxy-1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol | 4'-(6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)biphenyl-4-ol | 4'-(6,7-dimethoxy-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol | CHEMBL245796 | Chk1_115

Type

Small organic molecule

Emp. Form.

C24H20N2O3

Mol. Mass.

384.4272

SMILES

COc1cc2Cc3c(n[nH]c3-c2cc1OC)-c1ccc(cc1)-c1ccc(O)cc1

Structure