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TargetCyclin-Dependent Kinase 5 (CDK5)
LigandBDBM31545
Substrate/CompetitorHistone H1
Meas. Tech.Kinase SPA Assay
pH7.4±n/a
Temperature296.15±n/a K
IC50 265±n/a nM
Citation Brasca, MGAmboldi, NBallinari, DCameron, ACasale, ECervi, GColombo, MColotta, FCroci, VD'Alessio, RFiorentini, FIsacchi, AMercurio, CMoretti, WPanzeri, APastori, WPevarello, PQuartieri, FRoletto, FTraquandi, GVianello, PVulpetti, ACiomei, M Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. J Med Chem52:5152-63 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Cyclin-Dependent Kinase 5 (CDK5)
Name:Cyclin-Dependent Kinase 5 (CDK5)
Synonyms:CDK5/p35 | Cyclin-dependent kinase 5 regulatory subunit 1 | Cyclin-dependent kinase 5/CDK5 activator 1
Type:Protein Complex
Mol. Mass.:n/a
Description:n/a
Components:This complex has 2 components.
Component 1
Name:Cyclin-T1/Cyclin-dependent-like kinase 5
Synonyms:CDK5 | Cyclin-dependent kinase 5 (CDK5/ p25) | Cyclin-dependent kinase 5 (CDK5/p35) | Cyclin-dependent-like kinase 5 (CDK5)
Type:Enzyme Subunit
Mol. Mass.:33308.61
Organism:Homo sapiens (human)
Description:n/a
Residue:292
Sequence:
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKH
KNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSR
NVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYS
TSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYP
MYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
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Component 2
Name:Cyclin-dependent kinase 5 regulatory subunit 1
Synonyms:Cyclin-Dependent Kinase 5 Activator 1, p35 | Cyclin-dependent kinase 5 (CDK5/p25) | TPKII regulatory subunit | p35
Type:Enzyme Subunit
Mol. Mass.:34077.43
Organism:Homo sapiens (human)
Description:n/a
Residue:307
Sequence:
MGTVLSLSPSYRKATLFEDGAATVGHYTAVQNSKNAKDKNLKRHSIISVLPWKRIVAVSA
KKKNSKKVQPNSSYQNNITHLNNENLKKSLSCANLSTFAQPPPAQPPAPPASQLSGSQTG
GSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRS
VDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNE
ISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKR
LLLGLDR
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  Blast E-value cutoff:
BDBM31545
Histone H1
Name:Histone H1
Synonyms:n/a
Type:Other Protein Type
Mol. Mass.:358.43
Organism:Bos taurus (bovine)
Description:n/a
Residue:3
Sequence:
n/a