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Target
Protein kinase C alpha type
Ligand
BDBM16316
Substrate
n/a
Meas. Tech.
ChEMBL_429708 (CHEMBL904282)
IC50
>10000±n/a nM
Citation
 Leftheris, K; Ahmed, G; Chan, R; Dyckman, AJ; Hussain, Z; Ho, K; Hynes, J; Letourneau, J; Li, W; Lin, S; Metzger, A; Moriarty, KJ; Riviello, C; Shimshock, Y; Wen, J; Wityak, J; Wrobleski, ST; Wu, H; Wu, J; Desai, M; Gillooly, KM; Lin, TH; Loo, D; McIntyre, KW; Pitt, S; Shen, DR; Shuster, DJ; Zhang, R; Diller, D; Doweyko, A; Sack, J; Baldwin, J; Barrish, J; Dodd, J; Henderson, I; Kanner, S; Schieven, GL; Webb, M The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase. J Med Chem 47:6283-91 (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:
BDBM16316
Synonyms:
3-({4-[(2,2-dimethylpropyl)(methyl)amino]-6-(4-methyl-1,4-diazepan-1-yl)-1,3,5-triazin-2-yl}amino)-N-methoxy-4-methylbenzamide | CHEMBL225088 | triaminotriazine aniline amide inhibitor, 1
Type:
Small organic molecule
Emp. Form.:
C24H38N8O2
Mol. Mass.:
470.6109
SMILES:
CONC(=O)c1ccc(C)c(Nc2nc(nc(n2)N2CCCN(C)CC2)N(C)CC(C)(C)C)c1
Structure:
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