Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase Chk1

Ligand

BDBM50307506

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_611988 (CHEMBL1072195)

IC50

>10000±n/a nM

Citation

Traquandi, G; Ciomei, M; Ballinari, D; Casale, E; Colombo, N; Croci, V; Fiorentini, F; Isacchi, A; Longo, A; Mercurio, C; Panzeri, A; Pastori, W; Pevarello, P; Volpi, D; Roussel, P; Vulpetti, A; Brasca, MG Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. J Med Chem53:2171-87 (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

BDBM50307506

n/a

Name

BDBM50307506

Synonyms:

1-Methyl-8-{[1-(phenylcarbonyl)piperidin-4-yl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL599428

Type

Small organic molecule

Emp. Form.

C23H25N7O2

Mol. Mass.

431.4903

SMILES

Cn1nc(C(N)=O)c2CCc3cnc(NC4CCN(CC4)C(=O)c4ccccc4)nc3-c12

Structure