Target
Cyclin-dependent kinase 5 activator 1
Ligand
BDBM50415034
Substrate
n/a
Meas. Tech.
ChEMBL_598630 (CHEMBL1048133)
IC50
1090±n/a nM
Citation
 Helal, CJKang, ZLucas, JCGant, TAhlijanian, MKSchachter, JBRichter, KECook, JMMenniti, FSKelly, KMente, SPandit, JHosea, N Potent and cellularly active 4-aminoimidazole inhibitors of cyclin-dependent kinase 5/p25 for the treatment of Alzheimer's disease. Bioorg Med Chem Lett 19:5703-7 (2009) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 5 activator 1
Synonyms:
CDK5/p35 | Cyclin-Dependent Kinase 5 (CDK5) | 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-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
Synonyms:
CD5R1_HUMAN | CDK5R | CDK5R1 | Cyclin-Dependent Kinase 5 Activator 1, p35 | Cyclin-dependent kinase 5 (CDK5/p25) | Cyclin-dependent kinase 5 regulatory subunit 1 | NCK5A | TPKII regulatory subunit | p35
Type:
Enzyme Subunit
Mol. Mass.:
34077.43
Organism:
Homo sapiens (Human)
Description:
Q15078
Residue:
307
Sequence:
MGTVLSLSPSYRKATLFEDGAATVGHYTAVQNSKNAKDKNLKRHSIISVLPWKRIVAVSAKKKNSKKVQPNSSYQNNITHLNNENLKKSLSCANLSTFAQPPPAQPPAPPASQLSGSQTGGSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRSVDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNEISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKRLLLGLDR
  
Inhibitor
Name:
BDBM50415034
Synonyms:
CHEMBL571523
Type:
Small organic molecule
Emp. Form.:
C16H19N3O3
Mol. Mass.:
301.3404
SMILES:
COc1ccc(CC(=O)Nc2cn(cn2)[C@H]2C[C@H](O)C2)cc1 |r,wU:15.15,wD:17.18,(29.97,-7.31,;31.3,-6.54,;31.31,-5,;29.98,-4.23,;29.98,-2.69,;31.32,-1.93,;31.33,-.39,;30,.39,;28.66,-.38,;30,1.93,;28.67,2.7,;27.43,1.79,;26.18,2.68,;26.64,4.15,;28.18,4.16,;24.72,2.19,;24.02,.81,;22.65,1.49,;21.19,1,;23.33,2.87,;32.65,-2.69,;32.65,-4.23,)|
Structure:
Search PDB for entries with ligand similarity: