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Target
Protein kinase C eta type
Ligand
BDBM3162
Substrate
Lysine-rich histone
Meas. Tech.
PKC assay
IC50
310±n/a nM
Citation
 Mendoza, JS; Jagdmann , GE; Gosnell, PA SYNTHESIS AND BIOLOGICAL EVALUATION OF CONFORMATIONALLY CONSTRAINED BICYCLIC AND TRICYCLIC BALANOL ANALOGUES AS INHIBITORS OF PROTEIN KINASE C. Bioorg Med Chem Lett 5:2211-6 (1995)    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:
BDBM3162
Synonyms:
2-({2,6-dihydroxy-4-[({3-[(4-hydroxybenzene)amido]-1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl}oxy)carbonyl]phenyl}carbonyl)-3-hydroxybenzoic acid | Balanol analog 28
Type:
Small organic molecule
Emp. Form.:
C32H31NO10
Mol. Mass.:
589.5892
SMILES:
CC1(C)C2CCC1(C)C(OC(=O)c1cc(O)c(C(=O)c3c(O)cccc3C(O)=O)c(O)c1)C2NC(=O)c1ccc(O)cc1 |TLB:9:8:5.4:1,33:32:5.4:1|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Lysine-rich histone
Synonyms:
ING Peptide | Lys-rich histone | histone type IIIS
Type:
Peptide
Mol. Mass.:
10508.21
Organism:
Bos taurus (bovine)
Description:
Purified as a lysine rich fraction of histone H1 from calf thymus.
Residue:
105
Sequence:
SETAPAAPAAAPPAEKTPVKKKAAKKPAGARRKASGPPVSELITKAVAASKERSGVSLAALKKALAAAGYDVEKNNSRIKLGLKSLVSKGTLVQTKGTGASGSFK