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Target
Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM7497
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
4200±n/a nM
Citation
 Kunick, C; Lauenroth, K; Leost, M; Meijer, L; Lemcke, T 1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. Bioorg Med Chem Lett 14:413-6 (2004) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 5 activator 1 [99-307]
Synonyms:
CDK5/p25 | Cyclin-Dependent Kinase 5 (CDK5)
Type:
Protein Complex
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Cyclin-dependent kinase 5
Synonyms:
CDK5 | CDK5_HUMAN | CDKN5 | Cell division protein kinase 5 | Cyclin-dependent kinase 5 (CDK5/ p25) | Cyclin-dependent kinase 5 (CDK5/p35) | Cyclin-dependent-like kinase 5 | Cyclin-dependent-like kinase 5 (CDK5) | PSSALRE | Serine/threonine-protein kinase PSSALRE | Tau protein kinase II catalytic subunit
Type:
Enzyme Subunit
Mol. Mass.:
33308.61
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
292
Sequence:
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKHKNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSRNVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYSTSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYPMYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
  
Component 2
Name:
Cyclin-dependent kinase 5 activator 1 [99-307]
Synonyms:
CD5R1_HUMAN | CDK5R | CDK5R1 | Cyclin-Dependent Kinase 5 Activator | Cyclin-dependent kinase 5 activator 1, p25 | NCK5A | TPKII regulatory subunit | p25
Type:
Enzyme Subunit
Mol. Mass.:
23250.56
Organism:
Homo sapiens (Human)
Description:
Q15078 aa 99-307
Residue:
209
Sequence:
AQPPPAQPPAPPASQLSGSQTGGSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRSVDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNEISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKRLLLGLDR
  
Inhibitor
Name:
BDBM7497
Synonyms:
1-Azakenpaullone | 14-bromo-3,8,18-triazatetracyclo[9.7.0.0^{2,7}.0^{12,17}]octadeca-1(11),2,4,6,12(17),13,15-heptaen-9-one | US11759530, Compound Table1.11
Type:
Small organic molecule
Emp. Form.:
C15H10BrN3O
Mol. Mass.:
328.163
SMILES:
Brc1ccc2[nH]c-3c(CC(=O)Nc4cccnc-34)c2c1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA