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Target
Protein kinase C alpha type
Ligand
BDBM50122938
Substrate
n/a
Meas. Tech.
ChEMBL_160297 (CHEMBL769625)
Ki
7.8±n/a nM
Citation
 Kozikowski, AP; Nowak, I; Petukhov, PA; Etcheberrigaray, R; Mohamed, A; Tan, M; Lewin, N; Hennings, H; Pearce, LL; Blumberg, PM New amide-bearing benzolactam-based protein kinase C modulators induce enhanced secretion of the amyloid precursor protein metabolite sAPPalpha. J Med Chem 46:364-73 (2003) [PubMed]  Article 
Target
Name:
Protein kinase C alpha type
Synonyms:
KPCA_HUMAN | PKC alpha | PKC alpha and beta-2 | PKC-A | PKC-alpha | PKCA | PRKACA | PRKCA | Protein Kinase C- alpha | Protein kinase C alpha | Protein kinase C alpha (PKCa) | Protein kinase C alpha type (PKC-A) | Protein kinase C alpha type (PRKCA) | Proto-oncogene c-RAF | RAF proto-oncogene serine/threonine-protein kinase
Type:
Enzyme
Mol. Mass.:
76755.65
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
672
Sequence:
MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGSLLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDAKNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRLSVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNMELRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKGTEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYVNGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIADFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDGEDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRIDWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVNPQFVHPILQSAV
  
Inhibitor
Name:
BDBM50122938
Synonyms:
5-(3,5-Bis-trifluoromethyl-phenyl)-pentanoic acid (5-hydroxymethyl-2-isopropyl-1-methyl-3-oxo-1,2,3,4,5,6-hexahydro-benzo[e][1,4]diazocin-8-yl)-amide | CHEMBL333323
Type:
Small organic molecule
Emp. Form.:
C28H33F6N3O3
Mol. Mass.:
573.5703
SMILES:
CC(C)[C@@H]1N(C)c2ccc(NC(=O)CCCCc3cc(cc(c3)C(F)(F)F)C(F)(F)F)cc2C[C@@H](CO)NC1=O
Structure:
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