Reaction Details
Report a problem with these data
Report a problem with these dataTarget
Cyclin-dependent kinase 1/G2/mitotic-specific cyclin-B
Ligand
BDBM5566
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
Ki
2500±400 nM
Comments
To obtain Ki value, the assay was performed in the absence of inhibitor and at two fixed inhibitor concentrations, 5 and 10 uM, with ATP concentrations ranging from 6.25 to 800 uM. Data were fitted to the Michaelis-Menten equation using unweighted nonlinear least squares regression.
Citation
Arris, CE; Boyle, FT; Calvert, AH; Curtin, NJ; Endicott, JA; Garman, EF; Gibson, AE; Golding, BT; Grant, S; Griffin, RJ; Jewsbury, P; Johnson, LN; Lawrie, AM; Newell, DR; Noble, ME; Sausville, EA; Schultz, R; Yu, W Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem 43:2797-804 (2000) [PubMed] Article More Info.:
Target
Name:
Cyclin-dependent kinase 1/G2/mitotic-specific cyclin-B
Synonyms:
CDK1/Cyclin B | Cyclin-Dependent Kinase 1 (CDK1) | p34cdc2/Cyclin B
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
p34cdc2/cyclin B was purified from M-phase starfish oocytes by affinity chromatography.
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 1
Synonyms:
CDK1_ORYLA | Cell division control protein 2 (cdc2) | P34 protein kinase | cdc2 | cdk1
Type:
Enzyme Subunit
Mol. Mass.:
34693.35
Organism:
Marthasterias glacialis (starfish)
Description:
Q9DGD3 {empty hard to find)
Residue:
303
Sequence:
MEDYVKIEKIGEGTYGVVYKGRHKSTGQVVAMKKIRLESEEEGVPSTAVREVSLLQELKHPNVVRLLDVLMQESRLYLIFEFLSMDLKKYLDSIPSGQYMDPMLVKSYLYQILEGIYFCHRRRVLHRDLKPQNLLIDNKGVIKLADFGLARAFGVPVRVYTHEVVTLWYRAPEVLLGSPRYSTPVDVWSTGTIFAELATKKPLFHGDSEIDQLFRIFRTLGTPNNDVWPDVESLPDYKNTFPKWKEGSLSSMVKNLDKNGLDLLAKMLIYNPPKRISAREAMTHPYFDDLDKSTLPAACINGV
Component 2
Name:
G2/mitotic-specific cyclin-B
Synonyms:
CCNB_MARGL | Cyclin B | G2/mitotic-specific cyclin-B1
Type:
Enzyme Subunit
Mol. Mass.:
43790.28
Organism:
Marthasterias glacialis (starfish)
Description:
n/a
Residue:
388
Sequence:
MLNGENVDSRIMGKVATRASSKGVKSTLGTRGALENISNVARNNLQAGAKKELVKAKRGMTKSKATSSLQSVMGLNVEPMEKAKPQSPEPMDMSEINSALEAFSQNLLEGVEDIDKNDFDNPQLCSEFVNDIYQYMRKLEREFKVRTDYMTIQEITERMRSILIDWLVQVHLRFHLLQETLFLTIQILDRYLEVQPVSKNKLQLVGVTSMLIAAKYEEMYPPEIGDFVYITDNAYTKAQIRSMECNILRRLDFSLGKPLCIHFLRRNSKAGGVDGQKHTMAKYLMELTLPEYAFVPYDPSEIAAAALCLSSKILEPDMEWGTTLVHYSAYSEDHLMPIVQKMALVLKNAPTAKFQAVRKKYSSAKFMNVSTISALTSSTVMDLADQMC
Inhibitor
Name:
BDBM5566
Synonyms:
2,6-Diamino-4-cyclohexylmethoxy-5-nitrosopyrimidine | 6-(cyclohexylmethoxy)-5-nitrosopyrimidine-2,4-diamine | NU6027 | pyrimidine deriv.
Type:
Small organic molecule
Emp. Form.:
C11H17N5O2
Mol. Mass.:
251.285
SMILES:
Nc1nc(N)c(N=O)c(OCC2CCCCC2)n1
Structure:
Substrate
Name:
Histone H1
Synonyms:
Sigma Type IIIS
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
12.5 uM ATP as co-substrate.
Residue:
3
Sequence:
NA