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TargetProtein kinase C gamma type
LigandBDBM50049439
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1455517 (CHEMBL3364570)
IC50 13000±n/a nM
Citation George, DMBreinlinger, ECFriedman, MZhang, YWang, JArgiriadi, MBansal-Pakala, PBarth, MDuignan, DBHonore, PLang, QMittelstadt, SPotin, DRundell, LEdmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Protein kinase C gamma type
Name:Protein kinase C gamma type
Synonyms:KPCG_HUMAN | PKC gamma | PKC-gamma | PKCG | PRKCG | Protein kinase C gamma | Protein kinase C gamma type | Protein kinase C, PKC; classical/novel | Protein kinase C, gamma
Type:Enzyme
Mol. Mass.:78458.05
Organism:Homo sapiens (Human)
Description:The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:697
Sequence:
MAGLGPGVGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIG
KQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSL
LYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTADEIHVTVGEA
RNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTRTVKATLNPVWNETFVFNLKPGDVERRL
SVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQ
KFEACNYPLELYERVRMGPSSSPIPSPSPSPTDPKRCFFGASPGRLHISDFSFLMVLGKG
SFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQL
HSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRD
LKLDNVMLDAEGHIKITDFGMCKENVFPGTTTRTFCGTPDYIAPEIIAYQPYGKSVDWWS
FGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGS
GPDGEPTIRAHGFFRWIDWERLERLEIPPPFRPRPCGRSGENFDKFFTRAAPALTPPDRL
VLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50049439
n/a
NameBDBM50049439
Synonyms:CHEMBL3356472
TypeSmall organic molecule
Emp. Form.C20H21N5O2
Mol. Mass.363.413
SMILESC[C@H]1N2C(COc3cc(c(NC4CNC4)cc23)-c2ccccc2)=NNC1=O |r,c:26|
Structure
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