Reaction Details |
| Report a problem with these data |
Target | Protein kinase C epsilon type |
---|
Ligand | BDBM50049439 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1454736 (CHEMBL3362928) |
---|
IC50 | 460±n/a nM |
---|
Citation | George, DM; Breinlinger, EC; Friedman, M; Zhang, Y; Wang, J; Argiriadi, M; Bansal-Pakala, P; Barth, M; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Potin, D; Rundell, L; Edmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (2015) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Protein kinase C epsilon type |
---|
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: | MVVFNGLLKIKICEAVSLKPTAWSLRHAVGPRPQTFLLDPYIALNVDDSRIGQTATKQKT
NSPAWHDEFVTDVCNGRKIELAVFHDAPIGYDDFVANCTIQFEELLQNGSRHFEDWIDLE
PEGRVYVIIDLSGSSGEAPKDNEERVFRERMRPRKRQGAVRRRVHQVNGHKFMATYLRQP
TYCSHCRDFIWGVIGKQGYQCQVCTCVVHKRCHELIITKCAGLKKQETPDQVGSQRFSVN
MPHKFGIHNYKVPTFCDHCGSLLWGLLRQGLQCKVCKMNVHRRCETNVAPNCGVDARGIA
KVLADLGVTPDKITNSGQRRKKLIAGAESPQPASGSSPSEEDRSKSAPTSPCDQEIKELE
NNIRKALSFDNRGEEHRAASSPDGQLMSPGENGEVRQGQAKRLGLDEFNFIKVLGKGSFG
KVMLAELKGKDEVYAVKVLKKDVILQDDDVDCTMTEKRILALARKHPYLTQLYCCFQTKD
RLFFVMEYVNGGDLMFQIQRSRKFDEPRSRFYAAEVTSALMFLHQHGVIYRDLKLDNILL
DAEGHCKLADFGMCKEGILNGVTTTTFCGTPDYIAPEILQELEYGPSVDWWALGVLMYEM
MAGQPPFEADNEDDLFESILHDDVLYPVWLSKEAVSILKAFMTKNPHKRLGCVASQNGED
AIKQHPFFKEIDWVLLEQKKIKPPFKPRIKTKRDVNNFDQDFTREEPVLTLVDEAIVKQI
NQEEFKGFSYFGEDLMP
|
|
|
BDBM50049439 |
---|
n/a |
---|
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 |
|