Target
Cyclin-dependent kinase 5 activator 1
Ligand
BDBM50415043
Substrate
n/a
Meas. Tech.
ChEMBL_598630 (CHEMBL1048133)
IC50
46±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:
BDBM50415043
Synonyms:
CHEMBL569586
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)c1cccnc1 |r,wU:21.26,19.21,(3.14,2.57,;4.48,3.33,;5.81,2.56,;5.8,1.02,;7.13,.25,;7.13,-1.29,;5.79,-2.06,;4.46,-1.28,;3.13,-2.05,;1.81,-1.28,;1.81,.26,;3.14,1.02,;4.46,.25,;4.48,4.87,;3.15,5.65,;1.91,4.73,;.66,5.62,;1.12,7.09,;2.66,7.11,;-.8,5.13,;-2.19,5.82,;-2.88,4.44,;-1.5,3.75,;-4.2,3.65,;-5.54,4.41,;-5.56,5.95,;-6.87,3.63,;-8.2,4.39,;-9.53,3.61,;-9.51,2.07,;-8.16,1.31,;-6.84,2.09,)|
Structure:
Search PDB for entries with ligand similarity: