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Target
Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM7377
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
Temperature
303.15±n/a K
IC50
200±n/a nM
Comments
extracted
Citation
 Mettey, Y; Gompel, M; Thomas, V; Garnier, M; Leost, M; Ceballos-Picot, I; Noble, M; Endicott, J; Vierfond, JM; Meijer, L Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem 46:222-36 (2003) [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:
BDBM7377
Synonyms:
4-{7-butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl}phenol | 6-phenyl[5H]pyrrolo[2,3-b]pyrazine (aloisine) 39 | 7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine | CHEMBL75680 | aloisine A
Type:
Small organic molecule
Emp. Form.:
C16H17N3O
Mol. Mass.:
267.3257
SMILES:
CCCCc1c([nH]c2nccnc12)-c1ccc(O)cc1
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