Reaction Details 
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Cyclin-dependent kinase 5 activator 1 [99-307]
Ligand
BDBM7108
Substrate
Histone H1
Meas. Tech.
Kinase SPA Assay
IC50
114±n/a nM
Citation
Pevarello, P; Brasca, MG; Amici, R; Orsini, P; Traquandi, G; Corti, L; Piutti, C; Sansonna, P; Villa, M; Pierce, BS; Pulici, M; Giordano, P; Martina, K; Fritzen, EL; Nugent, RA; Casale, E; Cameron, A; Ciomei, M; Roletto, F; Isacchi, A; Fogliatto, G; Pesenti, E; Pastori, W; Marsiglio, A; Leach, KL; Clare, PM; Fiorentini, F; Varasi, M; Vulpetti, A; Warpehoski, MA 3-Aminopyrazole inhibitors of CDK2/cyclin A as antitumor agents. 1. Lead finding. J Med Chem 47:3367-80 (2004) [PubMed] ArticleMore Info.:
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:
BDBM7108
Synonyms:
(N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(2-naphthyl)acetamide | N-(5-cyclopropyl-1H-pyrazol-3-yl)-2-(naphthalen-2-yl)acetamide | PNU-292137
Type:
Small organic molecule
Emp. Form.:
C18H17N3O
Mol. Mass.:
291.3471
SMILES:
O=C(Cc1ccc2ccccc2c1)Nc1cc(n[nH]1)C1CC1
Structure:
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