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Target
Protein kinase C gamma type
Ligand
BDBM50049437
Substrate
n/a
Meas. Tech.
ChEMBL_1455517 (CHEMBL3364570)
IC50
7800±n/a nM
Citation
 George, DM; Breinlinger, EC; Friedman, M; Zhang, Y; Wang, J; Argiriadi, M; Bansal-Pakala, P; Barth, M; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Potin, D; Rundell, L; Edmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem 58:222-36 (2015) [PubMed]  Article 
Target
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:
MAGLGPGVGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIGKQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSLLYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTADEIHVTVGEARNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTRTVKATLNPVWNETFVFNLKPGDVERRLSVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQKFEACNYPLELYERVRMGPSSSPIPSPSPSPTDPKRCFFGASPGRLHISDFSFLMVLGKGSFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQLHSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRDLKLDNVMLDAEGHIKITDFGMCKENVFPGTTTRTFCGTPDYIAPEIIAYQPYGKSVDWWSFGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGSGPDGEPTIRAHGFFRWIDWERLERLEIPPPFRPRPCGRSGENFDKFFTRAAPALTPPDRLVLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM
  
Inhibitor
Name:
BDBM50049437
Synonyms:
CHEMBL3356474
Type:
Small organic molecule
Emp. Form.:
C15H16F3N5O2
Mol. Mass.:
355.315
SMILES:
C[C@H]1N2C(COc3cc(c(NC4CNC4)cc23)C(F)(F)F)=NNC1=O |r,c:23|
Structure:
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