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Target
Protein kinase C epsilon type
Ligand
BDBM14027
Substrate
n/a
Meas. Tech.
ChEMBL_634589 (CHEMBL1117930)
IC50
3000±n/a nM
Citation
 Wu, F; Büttner, FH; Chen, R; Hickey, E; Jakes, S; Kaplita, P; Kashem, MA; Kerr, S; Kugler, S; Paw, Z; Prokopowicz, A; Shih, CK; Snow, R; Young, E; Cywin, CL Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account. Bioorg Med Chem Lett 20:3235-9 (2010) [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:
BDBM14027
Synonyms:
5-(1,4-diazepan-1-ylsulfonyl)isoquinoline | 5-(1,4-diazepane-1-sulfonyl)isoquinoline | AT877 | CHEMBL38380 | CHEMBL541388 | Fasudil (HA-1077) | HA-1077 | US9687483, Fasudil | cid_163751
Type:
Small organic molecule
Emp. Form.:
C14H17N3O2S
Mol. Mass.:
291.369
SMILES:
O=S(=O)(N1CCCNCC1)c1cccc2cnccc12
Structure:
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