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Target
Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM27218
Substrate
Histone H1
Meas. Tech.
CDK Inhibition Assay
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
60±n/a nM
Citation
 Popowycz, F; Fournet, G; Schneider, C; Bettayeb, K; Ferandin, Y; Lamigeon, C; Tirado, OM; Mateo-Lozano, S; Notario, V; Colas, P; Bernard, P; Meijer, L; Joseph, B Pyrazolo[1,5-a]-1,3,5-triazine as a purine bioisostere: access to potent cyclin-dependent kinase inhibitor (R)-roscovitine analogue. J Med Chem 52:655-63 (2009) [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:
BDBM27218
Synonyms:
(2R)-2-({4-[(3-chlorophenyl)amino]-8-(propan-2-yl)pyrazolo[1,5-a][1,3,5]triazin-2-yl}amino)-3-methylbutan-1-ol | pyrazolo[1,5-a]-1,3,5-triazine, 7c
Type:
Small organic molecule
Emp. Form.:
C19H25ClN6O
Mol. Mass.:
388.894
SMILES:
CC(C)[C@H](CO)Nc1nc(Nc2cccc(Cl)c2)n2ncc(C(C)C)c2n1 |r|
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