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TargetProtein kinase C alpha type
LigandBDBM50045370
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1459005 (CHEMBL3369598)
IC50>30000±n/a nM
Citation Xiao, DZhu, XSofolarides, MDegrado, SShao, NRao, AChen, XAslanian, RFossetta, JTian, FTrivedi, PLundell, DPalani, A Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres. Bioorg Med Chem Lett24:3609-13 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Protein kinase C alpha type
Name:Protein kinase C alpha type
Synonyms:KPCA_HUMAN | PKC alpha | PKC alpha and beta-2 | PKC-A | PKC-alpha | PKCA | PRKACA | PRKCA | Protein Kinase C- alpha | Protein kinase C alpha | Protein kinase C alpha (PKCa) | Protein kinase C alpha type (PKC-A) | Protein kinase C alpha type (PRKCA) | Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase
Type:Enzyme
Mol. Mass.:76755.65
Organism:Homo sapiens (Human)
Description:The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:672
Sequence:
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50045370
n/a
NameBDBM50045370
Synonyms:CHEMBL3314140
TypeSmall organic molecule
Emp. Form.C23H21ClN4O
Mol. Mass.404.892
SMILESClc1ccc(cc1)-c1ccc(o1)-c1nccn1-c1ccc(cc1)N1CCNCC1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: