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TargetCDK2/Cyclin A/Cyclin A1
LigandBDBM50307507
Substrate/Competitorn/a
Meas. Tech.ChEMBL_611970
IC50 2±n/a nM
Citation Traquandi GCiomei MBallinari DCasale EColombo NCroci VFiorentini FIsacchi ALongo AMercurio CPanzeri APastori WPevarello PVolpi DRoussel PVulpetti ABrasca MG Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors. J Med Chem 53:2171-87 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
CDK2/Cyclin A/Cyclin A1
Name:CDK2/Cyclin A/Cyclin A1
Synonyms:Cyclin A1/A2/dependent kinase 2 | Cyclin-dependent kinase 2/cyclin A
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of EBI is 42813
Components:This complex has 3 components.
Component 1
Name:Cyclin-A2
Synonyms:CCN1 | CCNA | CCNA1 | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:n/a
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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Component 2
Name:Cyclin-A1/Cyclin-dependent kinase 4
Synonyms:CDK2/Cyclin A1 | Cyclin-A1
Type:Enzyme
Mol. Mass.:52343.37
Organism:Homo sapiens (Human)
Description:P78396
Residue:465
Sequence:
METGFPAIMYPGSFIGGWGEEYLSWEGPGLPDFVFQQQPVESEAMHCSNPKSGVVLATVA
RGPDACQILTRAPLGQDPPQRTVLGLLTANGQYRRTCGQGITRIRCYSGSENAFPPAGKK
ALPDCGVQEPPKQGFDIYMDELEQGDRDSCSVREGMAFEDVYEVDTGTLKSDLHFLLDFN
TVSPMLVDSSLLSQSEDISSLGTDVINVTEYAEEIYQYLREAEIRHRPKAHYMKKQPDIT
EGMRTILVDWLVEVGEEYKLRAETLYLAVNFLDRFLSCMSVLRGKLQLVGTAAMLLASKY
EEIYPPEVDEFVYITDDTYTKRQLLKMEHLLLKVLAFDLTVPTTNQFLLQYLRRQGVCVR
TENLAKYVAELSLLEADPFLKYLPSLIAAAAFCLANYTVNKHFWPETLAAFTGYSLSEIV
PCLSELHKAYLDIPHRPQQAIREKYKASKYLCVSLMEPPAVLLLQ
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Component 3
Name:Cyclin-dependent kinase 2
Synonyms:CDK2 | CDK2-Kinase | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | p33 protein kinase
Type:Enzyme Subunit
Mol. Mass.:33938.17
Organism:Homo sapiens (Human)
Description:P24941
Residue:298
Sequence:
MENFQKVEKIGEGTYGVVYKARNKLTGEVVALKKIRLDTETEGVPSTAIREISLLKELNH
PNIVKLLDVIHTENKLYLVFEFLHQDLKKFMDASALTGIPLPLIKSYLFQLLQGLAFCHS
HRVLHRDLKPQNLLINTEGAIKLADFGLARAFGVPVRTYTHEVVTLWYRAPEILLGCKYY
STAVDIWSLGCIFAEMVTRRALFPGDSEIDQLFRIFRTLGTPDEVVWPGVTSMPDYKPSF
PKWARQDFSKVVPPLDEDGRSLLSQMLHYDPNKRISAKAALAHPFFQDVTKPVPHLRL
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Component 4
Name:Cyclin-A2
Synonyms:CCN1 | CCNA | CCNA1 | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:n/a
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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BDBM50307507
n/a
NameBDBM50307507
Synonyms:CHEMBL597754 | N-1-Dimethyl-8-{[1-(methylsulfonyl)piperidin-4-yl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
TypeSmall organic molecule
Emp. Form.C24H34N8O4S
Mol. Mass.530.643
SMILESCNC(=O)c1nn(C)c-2c1CCc1cnc(NC3CCN(CC3)C(=O)C3CCN(CC3)S(C)(=O)=O)nc-21
Structure
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