Target
Cyclin-dependent kinase 5 activator 1
Ligand
BDBM50415035
Substrate
n/a
Meas. Tech.
ChEMBL_598630 (CHEMBL1048133)
IC50
145±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:
BDBM50415035
Synonyms:
CHEMBL576126
Type:
Small organic molecule
Emp. Form.:
C18H21N3O4
Mol. Mass.:
343.377
SMILES:
COC(=O)[C@H]1C[C@H](C1)n1cnc(NC(=O)Cc2ccc(OC)cc2)c1 |r,wU:6.8,4.3,(-9.08,-15.29,;-7.72,-14.56,;-7.67,-13.02,;-8.98,-12.21,;-6.32,-12.29,;-5.63,-10.91,;-4.24,-11.59,;-4.94,-12.98,;-2.78,-11.1,;-2.32,-9.63,;-.78,-9.62,;-.29,-11.08,;1.04,-11.85,;1.04,-13.39,;-.3,-14.16,;2.37,-14.17,;2.36,-15.71,;1.02,-16.47,;1.02,-18.01,;2.35,-18.79,;2.34,-20.33,;1.01,-21.09,;3.69,-18.01,;3.69,-16.48,;-1.53,-12,)|
Structure:
Search PDB for entries with ligand similarity: