Target
Protein kinase C epsilon type
Ligand
BDBM50393231
Substrate
n/a
Meas. Tech.
ChEMBL_850745 (CHEMBL2156014)
IC50
>316±n/a nM
Citation
 Wagner, Jvon Matt, PFaller, BCooke, NGAlbert, RSedrani, RWiegand, HJean, CBeerli, CWeckbecker, GEvenou, JPZenke, GCottens, S Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis. J Med Chem 54:6028-39 (2011) [PubMed]  Article 
Target
Name:
Protein kinase C epsilon type
Synonyms:
KPCE_HUMAN | PKC epsilon | PKCE | PRKCE | Protein kinase C epsilon | Protein kinase C epsilon type | Protein kinase C, PKC; classical/novel | Protein kinase C, epsilon | nPKC-epsilon
Type:
Enzyme
Mol. Mass.:
83680.45
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
737
Sequence:
MVVFNGLLKIKICEAVSLKPTAWSLRHAVGPRPQTFLLDPYIALNVDDSRIGQTATKQKTNSPAWHDEFVTDVCNGRKIELAVFHDAPIGYDDFVANCTIQFEELLQNGSRHFEDWIDLEPEGRVYVIIDLSGSSGEAPKDNEERVFRERMRPRKRQGAVRRRVHQVNGHKFMATYLRQPTYCSHCRDFIWGVIGKQGYQCQVCTCVVHKRCHELIITKCAGLKKQETPDQVGSQRFSVNMPHKFGIHNYKVPTFCDHCGSLLWGLLRQGLQCKVCKMNVHRRCETNVAPNCGVDARGIAKVLADLGVTPDKITNSGQRRKKLIAGAESPQPASGSSPSEEDRSKSAPTSPCDQEIKELENNIRKALSFDNRGEEHRAASSPDGQLMSPGENGEVRQGQAKRLGLDEFNFIKVLGKGSFGKVMLAELKGKDEVYAVKVLKKDVILQDDDVDCTMTEKRILALARKHPYLTQLYCCFQTKDRLFFVMEYVNGGDLMFQIQRSRKFDEPRSRFYAAEVTSALMFLHQHGVIYRDLKLDNILLDAEGHCKLADFGMCKEGILNGVTTTTFCGTPDYIAPEILQELEYGPSVDWWALGVLMYEMMAGQPPFEADNEDDLFESILHDDVLYPVWLSKEAVSILKAFMTKNPHKRLGCVASQNGEDAIKQHPFFKEIDWVLLEQKKIKPPFKPRIKTKRDVNNFDQDFTREEPVLTLVDEAIVKQINQEEFKGFSYFGEDLMP
  
Inhibitor
Name:
BDBM50393231
Synonyms:
CHEMBL2153753
Type:
Small organic molecule
Emp. Form.:
C28H28N6O2
Mol. Mass.:
480.5609
SMILES:
CC(C)c1ccc2nc(nc(C3=C(C(=O)NC3=O)c3c[nH]c4ccccc34)c2c1)N1CCN(C)CC1 |t:11|
Structure:
Search PDB for entries with ligand similarity: