Reaction Details |
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Target | Protein kinase C alpha type |
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Ligand | BDBM16316 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_429708 (CHEMBL904282) |
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IC50 | >10000±n/a nM |
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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 Chem47:6283-91 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C alpha type |
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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: | MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
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BDBM16316 |
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n/a |
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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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