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Target
Protein kinase C alpha type
Ligand
BDBM50331629
Substrate
n/a
Meas. Tech.
ChEMBL_687503 (CHEMBL1292179)
IC50
>40000±n/a nM
Citation
 Das, J; Moquin, RV; Dyckman, AJ; Li, T; Pitt, S; Zhang, R; Shen, DR; McIntyre, KW; Gillooly, K; Doweyko, AM; Newitt, JA; Sack, JS; Zhang, H; Kiefer, SE; Kish, K; McKinnon, M; Barrish, JC; Dodd, JH; Schieven, GL; Leftheris, K 5-amino-pyrazoles as potent and selective p38a inhibitors. Bioorg Med Chem Lett 20:6886-9 (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:
BDBM50331629
Synonyms:
5-amino-1-(2-fluorophenyl)-N-(5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl)-1H-pyrazole-4-carboxamide | CHEMBL1290746
Type:
Small organic molecule
Emp. Form.:
C21H17FN6O3
Mol. Mass.:
420.3965
SMILES:
Cc1ccc(cc1NC(=O)c1cnn(c1N)-c1ccccc1F)C(=O)Nc1ccon1
Structure:
Search PDB for entries with ligand similarity: