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Target
Protein kinase C alpha type
Ligand
BDBM50149481
Substrate
n/a
Meas. Tech.
ChEMBL_306262 (CHEMBL828395)
IC50
2539±n/a nM
Citation
 Sharma, V; Tepe, JJ Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine. Bioorg Med Chem Lett 14:4319-21 (2004) [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:
BDBM50149481
Synonyms:
5-[2-Amino-5-oxo-1,5-dihydro-imidazol-(4Z)-ylidene]-3,4,5,10-tetrahydro-2H-azepino[3,4-b]indol-1-one | 5-[2-Amino-5-oxo-3,5-dihydro-imidazol-(4Z)-ylidene]-3,4,5,10-tetrahydro-2H-azepino[3,4-b]indol-1-one | CHEMBL332551
Type:
Small organic molecule
Emp. Form.:
C15H13N5O2
Mol. Mass.:
295.296
SMILES:
Nc1nc(O)c([nH]1)C1=C2C(=Nc3ccccc23)C(=O)NCC1 |c:10,t:8|
Structure:
Search PDB for entries with ligand similarity: