Reaction Details Report a problem with these data
Target
Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM10649
Substrate
Histone H1
Meas. Tech.
Kinase Inhibition Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
4900±n/a nM
Citation
 Vandromme, L; Piguel, S; Lozach, O; Meijer, L; Legraverend, M; Grierson, DS Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors. Bioorg Med Chem Lett 16:3144-6 (2006) [PubMed]  Article 
Target
Name:
Cyclin-dependent kinase 5 activator 1 [99-307]
Synonyms:
CDK5/p25 | Cyclin-Dependent Kinase 5 (CDK5)
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 [99-307]
Synonyms:
CD5R1_HUMAN | CDK5R | CDK5R1 | Cyclin-Dependent Kinase 5 Activator | Cyclin-dependent kinase 5 activator 1, p25 | NCK5A | TPKII regulatory subunit | p25
Type:
Enzyme Subunit
Mol. Mass.:
23250.56
Organism:
Homo sapiens (Human)
Description:
Q15078 aa 99-307
Residue:
209
Sequence:
AQPPPAQPPAPPASQLSGSQTGGSSSVKKAPHPAVTSAGTPKRVIVQASTSELLRCLGEFLCRRCYRLKHLSPTDPVLWLRSVDRSLLLQGWQDQGFITPANVVFLYMLCRDVISSEVGSDHELQAVLLTCLYLSYSYMGNEISYPLKPFLVESCKEAFWDRCLSVINLMSSKMLQINADPHYFTQVFSDLKNESGQEDKKRLLLGLDR
  
Inhibitor
Name:
BDBM10649
Synonyms:
1-(5-{6-[(2-methoxyethyl)amino]-9-(propan-2-yl)-9H-purin-2-yl}thiophen-2-yl)ethan-1-one | 2-purine deriv. 14
Type:
Small organic molecule
Emp. Form.:
C17H21N5O2S
Mol. Mass.:
359.446
SMILES:
COCCNc1nc(nc2n(cnc12)C(C)C)-c1ccc(s1)C(C)=O
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Histone H1
Synonyms:
n/a
Type:
Other Protein Type
Mol. Mass.:
358.43
Organism:
Bos taurus (bovine)
Description:
n/a
Residue:
3
Sequence:
NA