Target
Protein kinase C zeta type
Ligand
BDBM50049439
Substrate
n/a
Meas. Tech.
ChEMBL_1455519 (CHEMBL3364572)
IC50
8500±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 Chem 58:222-36 (2015) [PubMed]  Article 
Target
Name:
Protein kinase C zeta type
Synonyms:
KPCZ_HUMAN | PKC2 | PRKCZ | Protein Kinase C, zeta | Protein kinase C (PKC) | Protein kinase C iota type/zeta type | Protein kinase C zeta | Protein kinase C zeta (PKCζ) | Protein kinase C zeta type | Protein kinase C zeta type (PKC zeta) | Protein kinase C zeta type (PKCzeta) | nPKC-zeta
Type:
Enzyme
Mol. Mass.:
67649.13
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
592
Sequence:
MPSRTGPKMEGSGGRVRLKAHYGGDIFITSVDAATTFEELCEEVRDMCRLHQQHPLTLKWVDSEGDPCTVSSQMELEEAFRLARQCRDEGLIIHVFPSTPEQPGLPCPGEDKSIYRRGARRWRKLYRANGHLFQAKRFNRRAYCGQCSERIWGLARQGYRCINCKLLVHKRCHGLVPLTCRKHMDSVMPSQEPPVDDKNEDADLPSEETDGIAYISSSRKHDSIKDDSEDLKPVIDGMDGIKISQGLGLQDFDLIRVIGRGSYAKVLLVRLKKNDQIYAMKVVKKELVHDDEDIDWVQTEKHVFEQASSNPFLVGLHSCFQTTSRLFLVIEYVNGGDLMFHMQRQRKLPEEHARFYAAEICIALNFLHERGIIYRDLKLDNVLLDADGHIKLTDYGMCKEGLGPGDTTSTFCGTPNYIAPEILRGEEYGFSVDWWALGVLMFEMMAGRSPFDIITDNPDMNTEDYLFQVILEKPIRIPRFLSVKASHVLKGFLNKDPKERLGCRPQTGFSDIKSHAFFRSIDWDLLEKKQALPPFQPQITDDYGLDNFDTQFTSEPVQLTPDDEDAIKRIDQSEFEGFEYINPLLLSTEESV
  
Inhibitor
Name:
BDBM50049439
Synonyms:
CHEMBL3356472
Type:
Small organic molecule
Emp. Form.:
C20H21N5O2
Mol. Mass.:
363.413
SMILES:
C[C@H]1N2C(COc3cc(c(NC4CNC4)cc23)-c2ccccc2)=NNC1=O |r,c:26|
Structure:
Search PDB for entries with ligand similarity: