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Target
Protein kinase C eta type
Ligand
BDBM50393222
Substrate
n/a
Meas. Tech.
ChEMBL_850746 (CHEMBL2156015)
IC50
9.1±n/a nM
Citation
 Wagner, J; von Matt, P; Faller, B; Cooke, NG; Albert, R; Sedrani, R; Wiegand, H; Jean, C; Beerli, C; Weckbecker, G; Evenou, JP; Zenke, G; Cottens, 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 eta type
Synonyms:
KPCL_HUMAN | PKC-L | PKCL | PRKCH | PRKCL | Protein Kinase C, eta | Protein kinase C, PKC; classical/novel | nPKC-eta
Type:
Enzyme
Mol. Mass.:
77844.26
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
683
Sequence:
MSSGTMKFNGYLRVRIGEAVGLQPTRWSLRHSLFKKGHQLLDPYLTVSVDQVRVGQTSTKQKTNKPTYNEEFCANVTDGGHLELAVFHETPLGYDHFVANCTLQFQELLRTTGASDTFEGWVDLEPEGKVFVVITLTGSFTEATLQRDRIFKHFTRKRQRAMRRRVHQINGHKFMATYLRQPTYCSHCREFIWGVFGKQGYQCQVCTCVVHKRCHHLIVTACTCQNNINKVDSKIAEQRFGINIPHKFSIHNYKVPTFCDHCGSLLWGIMRQGLQCKICKMNVHIRCQANVAPNCGVNAVELAKTLAGMGLQPGNISPTSKLVSRSTLRRQGKESSKEGNGIGVNSSNRLGIDNFEFIRVLGKGSFGKVMLARVKETGDLYAVKVLKKDVILQDDDVECTMTEKRILSLARNHPFLTQLFCCFQTPDRLFFVMEFVNGGDLMFHIQKSRRFDEARARFYAAEIISALMFLHDKGIIYRDLKLDNVLLDHEGHCKLADFGMCKEGICNGVTTATFCGTPDYIAPEILQEMLYGPAVDWWAMGVLLYEMLCGHAPFEAENEDDLFEAILNDEVVYPTWLHEDATGILKSFMTKNPTMRLGSLTQGGEHAILRHPFFKEIDWAQLNHRQIEPPFRPRIKSREDVSNFDPDFIKEEPVLTPIDEGHLPMINQDEFRNFSYVSPELQP
  
Inhibitor
Name:
BDBM50393222
Synonyms:
CHEMBL2151408
Type:
Small organic molecule
Emp. Form.:
C25H21ClN6O2
Mol. Mass.:
472.926
SMILES:
CN1CCN(CC1)c1nc(C2=C(C(=O)NC2=O)c2c[nH]c3ccc(Cl)cc23)c2ccccc2n1 |t:11|
Structure:
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