| Reaction Details |
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 | Report a problem with these data |
| Target | Protein kinase C alpha type |
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| Ligand | BDBM50049440 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1454726 (CHEMBL3362645) |
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| IC50 | 3000±n/a nM |
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| Citation |  George, DM; Breinlinger, EC; Friedman, M; Zhang, Y; Wang, J; Argiriadi, M; Bansal-Pakala, P; Barth, M; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Potin, D; Rundell, L; Edmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (2015) [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 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 76755.65 |
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| Organism: | Homo sapiens (Human) |
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| Description: | The recombinant human PKC enzymes were
produced using a baculovirus expression system in SF9 cells |
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| Residue: | 672 |
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| Sequence: | MADVFPGNDSTASQDVANRFARKGALRQKNVHEVKDHKFIARFFKQPTFCSHCTDFIWGF
GKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPDTDDPRSKHKFKIHTYGSPTFCDHCGS
LLYGLIHQGMKCDTCDMNVHKQCVINVPSLCGMDHTEKRGRIYLKAEVADEKLHVTVRDA
KNLIPMDPNGLSDPYVKLKLIPDPKNESKQKTKTIRSTLNPQWNESFTFKLKPSDKDRRL
SVEIWDWDRTTRNDFMGSLSFGVSELMKMPASGWYKLLNQEEGEYYNVPIPEGDEEGNME
LRQKFEKAKLGPAGNKVISPSEDRKQPSNNLDRVKLTDFNFLMVLGKGSFGKVMLADRKG
TEELYAIKILKKDVVIQDDDVECTMVEKRVLALLDKPPFLTQLHSCFQTVDRLYFVMEYV
NGGDLMYHIQQVGKFKEPQAVFYAAEISIGLFFLHKRGIIYRDLKLDNVMLDSEGHIKIA
DFGMCKEHMMDGVTTRTFCGTPDYIAPEIIAYQPYGKSVDWWAYGVLLYEMLAGQPPFDG
EDEDELFQSIMEHNVSYPKSLSKEAVSVCKGLMTKHPAKRLGCGPEGERDVREHAFFRRI
DWEKLENREIQPPFKPKVCGKGAENFDKFFTRGQPVLTPPDQLVIANIDQSDFEGFSYVN
PQFVHPILQSAV
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| BDBM50049440 |
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| n/a |
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| Name | BDBM50049440 |
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| Synonyms: | CHEMBL3356471 |
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| Type | Small organic molecule |
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| Emp. Form. | C15H19N5O2 |
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| Mol. Mass. | 301.3437 |
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| SMILES | C[C@@H]1N2C(COc3cc(C)c(NC4CNC4)cc23)=NNC1=O |r,c:20| |
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| Structure | 
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