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TargetCyclin-A1/Cyclin-A2/Cyclin-dependent kinase 2
LigandBDBM2579
Substrate/Competitorn/a
Meas. Tech.ChEMBL_936300 (CHEMBL2320998)
Ki 4±n/a nM
Citation Hole, AJBaumli, SShao, HShi, SHuang, SPepper, CFischer, PMWang, SEndicott, JANoble, ME Comparative structural and functional studies of 4-(thiazol-5-yl)-2-(phenylamino)pyrimidine-5-carbonitrile CDK9 inhibitors suggest the basis for isotype selectivity. J Med Chem56:660-70 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cyclin-A1/Cyclin-A2/Cyclin-dependent kinase 2
Name:Cyclin-A1/Cyclin-A2/Cyclin-dependent kinase 2
Synonyms:CDK2/Cyclin A/Cyclin A1 | 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 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:P20248
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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Component 2
Name:Cyclin-A1
Synonyms:CCNA1 | CCNA1_HUMAN | CDK2/Cyclin A1 | Cyclin-A1 | Cyclin-A1/Cyclin-dependent kinase 4
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 | CDK2_HUMAN | CDKN2 | Cell division protein kinase 2 | Cyclin-dependent kinase 2 (CDK2) | Protein cereblon/Cyclin-dependent kinase 2 | 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 | CCNA2 | CCNA2_HUMAN | Cyclin A | Cyclin-A
Type:Enzyme Subunit
Mol. Mass.:48550.19
Organism:Homo sapiens (Human)
Description:P20248
Residue:432
Sequence:
MLGNSAPGPATREAGSALLALQQTALQEDQENINPEKAAPVQQPRTRAALAVLKSGNPRG
LAQQQRPKTRRVAPLKDLPVNDEHVTVPPWKANSKQPAFTIHVDEAEKEAQKKPAESQKI
EREDALAFNSAISLPGPRKPLVPLDYPMDGSFESPHTMDMSIILEDEKPVSVNEVPDYHE
DIHTYLREMEVKCKPKVGYMKKQPDITNSMRAILVDWLVEVGEEYKLQNETLHLAVNYID
RFLSSMSVLRGKLQLVGTAAMLLASKFEEIYPPEVAEFVYITDDTYTKKQVLRMEHLVLK
VLTFDLAAPTVNQFLTQYFLHQQPANCKVESLAMFLGELSLIDADPYLKYLPSVIAGAAF
HLALYTVTGQSWPESLIRKTGYTLESLKPCLMDLHQTYLKAPQHAQQSIREKYKNSKYHG
VSLLNPPETLNL
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  Blast E-value cutoff:
BDBM2579
n/a
NameBDBM2579
Synonyms:(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one | CHEMBL388978 | Staurosporin, 4 | Staurosporine | Staurosporine, 8 | US20240002365, Compound staurosporine | US9206188, Staurosporine | US9226923, Staurosporine
TypeSmall organic molecule
Emp. Form.C28H26N4O3
Mol. Mass.466.531
SMILESCN[C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)n1c3ccccc3c3c4CNC(=O)c4c4c5ccccc5n2c4c13 |r|
Structure
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