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Target
Protein kinase C alpha type
Ligand
BDBM50162992
Substrate
n/a
Meas. Tech.
ChEMBL_305791 (CHEMBL827979)
IC50
290±n/a nM
Citation
 Zhang, HC; Derian, CK; McComsey, DF; White, KB; Ye, H; Hecker, LR; Li, J; Addo, MF; Croll, D; Eckardt, AJ; Smith, CE; Li, Q; Cheung, WM; Conway, BR; Emanuel, S; Demarest, KT; Andrade-Gordon, P; Damiano, BP; Maryanoff, BE Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. J Med Chem 48:1725-8 (2005) [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:
BDBM50162992
Synonyms:
3-[1-(3-Dimethylamino-propyl)-1H-indazol-3-yl]-4-(1-isoquinolin-4-yl-1H-indol-3-yl)-pyrrole-2,5-dione | CHEMBL359808
Type:
Small organic molecule
Emp. Form.:
C33H28N6O2
Mol. Mass.:
540.6144
SMILES:
CN(C)CCCn1nc(C2=C(C(=O)NC2=O)c2cn(-c3cncc4ccccc34)c3ccccc23)c2ccccc12 |t:9|
Structure:
Search PDB for entries with ligand similarity: