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Target
Protein kinase C alpha type
Ligand
BDBM50317750
Substrate
n/a
Meas. Tech.
ChEMBL_629477 (CHEMBL1120766)
IC50
>50000±n/a nM
Citation
 Williams, DK; Chen, XT; Tarby, C; Kaltenbach, R; Cai, ZW; Tokarski, JS; An, Y; Sack, JS; Wautlet, B; Gullo-Brown, J; Henley, BJ; Jeyaseelan, R; Kellar, K; Manne, V; Trainor, GL; Lombardo, LJ; Fargnoli, J; Borzilleri, RM Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors. Bioorg Med Chem Lett 20:2998-3002 (2010) [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:
BDBM50317750
Synonyms:
2-(4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenylamino)-N-(2,4-difluorophenyl)nicotinamide | CHEMBL1095873
Type:
Small organic molecule
Emp. Form.:
C25H16F3N5O2
Mol. Mass.:
475.422
SMILES:
Fc1ccc(NC(=O)c2cccnc2Nc2ccc(Oc3ccnc4[nH]ccc34)c(F)c2)c(F)c1
Structure:
Search PDB for entries with ligand similarity: