Target
Cyclin-dependent kinase 5 activator 1
Ligand
BDBM50415044
Substrate
n/a
Meas. Tech.
ChEMBL_598630 (CHEMBL1048133)
IC50
14±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:
BDBM50415044
Synonyms:
CHEMBL569587
Type:
Small organic molecule
Emp. Form.:
C25H23N5O2
Mol. Mass.:
425.4824
SMILES:
O=C(Cc1cccc2ccccc12)Nc1cn(cn1)[C@@H]1C[C@@H](C1)NC(=O)c1ccccn1 |r,wU:21.26,19.21,(28.29,2.47,;29.63,3.24,;30.96,2.46,;30.96,.92,;32.28,.16,;32.28,-1.38,;30.94,-2.15,;29.61,-1.38,;28.29,-2.14,;26.96,-1.38,;26.96,.16,;28.29,.93,;29.62,.16,;29.63,4.78,;28.3,5.55,;27.07,4.63,;25.81,5.53,;26.27,7,;27.81,7.01,;24.35,5.04,;22.96,5.72,;22.28,4.34,;23.66,3.66,;20.95,3.56,;19.61,4.32,;19.6,5.86,;18.29,3.53,;16.95,4.29,;15.63,3.51,;15.64,1.97,;16.99,1.21,;18.31,2,)|
Structure:
Search PDB for entries with ligand similarity: