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Target
Protein kinase C alpha type
Ligand
BDBM50455592
Substrate
n/a
Meas. Tech.
ChEMBL_1754792 (CHEMBL4189552)
IC50
140±n/a nM
Citation
 Kwiatkowski, J; Liu, B; Tee, DHY; Chen, G; Ahmad, NHB; Wong, YX; Poh, ZY; Ang, SH; Tan, ESW; Ong, EH; Nurul Dinie, na; Poulsen, A; Pendharkar, V; Sangthongpitag, K; Lee, MA; Sepramaniam, S; Ho, SY; Cherian, J; Hill, J; Keller, TH; Hung, AW Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors. J Med Chem 61:4386-4396 (2018) [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:
BDBM50455592
Synonyms:
CHEMBL4206065
Type:
Small organic molecule
Emp. Form.:
C24H21N5O
Mol. Mass.:
395.4564
SMILES:
COc1cc2CN(C)Cc2cc1-c1cnn2ccc(cc12)-c1ccnc2[nH]ccc12
Structure:
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