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Target
Cyclin-dependent kinase 5 activator 1
Ligand
BDBM50585749
Substrate
n/a
Meas. Tech.
ChEMBL_2163801 (CHEMBL5048662)
IC50
16±n/a nM
Citation
 Daniels, MH; Malojcic, G; Clugston, SL; Williams, B; Coeffet-Le Gal, M; Pan-Zhou, XR; Venkatachalan, S; Harmange, JC; Ledeboer, M Discovery and Optimization of Highly Selective Inhibitors of CDK5. J Med Chem 65:3575-3596 (2022) [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:
Cyclin-dependent-like kinase 5 (CDK5) | Cell division protein kinase 5 | Serine/threonine-protein kinase PSSALRE | Tau protein kinase II catalytic subunit | Cyclin-dependent-like kinase 5 | CDK5_HUMAN | CDK5 | CDKN5 | PSSALRE
Type:
Enzyme Subunit
Mol. Mass.:
33308.61
Organism:
Human
Description:
Residue:
292
Sequence:
MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKHKNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSRNVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYSTSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYPMYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
  
Component 2
Name:
Cyclin-dependent kinase 5 activator 1
Synonyms:
TPKII regulatory subunit | Cyclin-dependent kinase 5 regulatory subunit 1 | CD5R1_HUMAN | CDK5R1 | CDK5R | NCK5A
Type:
Enzyme Subunit
Mol. Mass.:
34077.43
Organism:
Human
Description:
Q15078
Residue:
307
Sequence:
MGTVLSLSPSYRKATLFEDGAATVGHYTAVQNSKNAKDKNLKRHSIISVLPWKRIVAVSAKKKNSKKVQPNSSYQNNITHLNNENLKKSLSCANLSTFAQPPPAQPPAPPASQLSGSQTGGSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRSVDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNEISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKRLLLGLDR
  
Inhibitor
Name:
BDBM50585749
Synonyms:
CHEMBL5088480
Type:
Small organic molecule
Emp. Form.:
C23H23FN6O2
Mol. Mass.:
434.48
SMILES:
OCc1ccn(n1)-c1ccc(Nc2cc3nc(OC4CCNCC4)ccc3cn2)c(F)c1
Structure:
Search PDB for entries with ligand similarity: