Target
Protein kinase C eta type
Ligand
BDBM50301686
Substrate
n/a
Meas. Tech.
ChEMBL_600776 (CHEMBL1037488)
IC50
140±n/a nM
Citation
 Subrath, JWang, DWu, BNiu, CBoschelli, DHLee, JYang, XBrennan, AChaudhary, D C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I. Bioorg Med Chem Lett 19:5423-5 (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:
BDBM50301686
Synonyms:
1-((5-(3-ethynyl-2-((4-methyl-1H-inden-5-yl)methyl)phenyl)furan-2-yl)methyl)-4-methylpiperazine | CHEMBL570865
Type:
Small organic molecule
Emp. Form.:
C29H30N2O
Mol. Mass.:
422.5613
SMILES:
CN1CCN(Cc2ccc(o2)-c2cccc(C#C)c2Cc2ccc3CC=Cc3c2C)CC1 |c:27|
Structure:
Search PDB for entries with ligand similarity: