Target
Protein kinase C epsilon type
Ligand
BDBM50012948
Substrate
n/a
Meas. Tech.
ChEMBL_1352186 (CHEMBL3268159)
IC50
1020±n/a nM
Citation
 Rechfeld, FGruber, PKirchmair, JBoehler, MHauser, NHechenberger, GGarczarczyk, DLapa, GBPreobrazhenskaya, MNGoekjian, PLanger, THofmann, J Thienoquinolines as novel disruptors of the PKCe/RACK2 protein-protein interaction. J Med Chem 57:3235-46 (2014) [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:
BDBM50012948
Synonyms:
CHEMBL3261358
Type:
Small organic molecule
Emp. Form.:
C37H65N9O13
Mol. Mass.:
843.9645
SMILES:
CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](N)CCC(O)=O)C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(O)=O |r|
Structure:
Search PDB for entries with ligand similarity: