Target
Protein kinase C epsilon type
Ligand
BDBM50241856
Substrate
n/a
Meas. Tech.
ChEMBL_1670920 (CHEMBL4020949)
Ki
131±n/a nM
Citation
 Elhalem, EDonadío, LGZhou, XLewin, NEGarcia, LCLai, CCKelley, JAPeach, MLBlumberg, PMComin, MJ Exploring the influence of indololactone structure on selectivity for binding to the C1 domains of PKC?, PKC?, and RasGRP. Bioorg Med Chem 25:2971-2980 (2017) [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:
BDBM50241856
Synonyms:
CHEMBL4097154
Type:
Small organic molecule
Emp. Form.:
C32H27NO5
Mol. Mass.:
505.5605
SMILES:
Cc1ccc(cc1)C#Cc1ccc(C=C2CC(CO)(COC(=O)c3cn(C)c4ccccc34)OC2=O)cc1
Structure:
Search PDB for entries with ligand similarity: