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Target
Protein kinase C eta type
Ligand
BDBM50302042
Substrate
n/a
Meas. Tech.
ChEMBL_599140 (CHEMBL1047195)
IC50
33±n/a nM
Citation
 Prashad, AS; Wang, D; Subrath, J; Wu, B; Lin, M; Zhang, MY; Kagan, N; Lee, J; Yang, X; Brennan, A; Chaudhary, D; Xu, X; Leung, L; Wang, J; Boschelli, DH C-5 substituted heteroaryl-3-pyridinecarbonitriles as PKCtheta inhibitors: part II. Bioorg Med Chem Lett 19:5799-802 (2009) [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:
BDBM50302042
Synonyms:
4-(4-methyl-1H-indol-5-ylamino)-5-(5-((4-methylpiperazin-1-yl)methyl)benzofuran-2-yl)nicotinonitrile | CHEMBL571581
Type:
Small organic molecule
Emp. Form.:
C29H28N6O
Mol. Mass.:
476.5722
SMILES:
CN1CCN(Cc2ccc3oc(cc3c2)-c2cncc(C#N)c2Nc2ccc3[nH]ccc3c2C)CC1
Structure:
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