| Reaction Details |
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 | Report a problem with these data |
| Target | Protein kinase C alpha type |
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| Ligand | BDBM50329198 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_701549 (CHEMBL1656188) |
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| IC50 | >100±n/a nM |
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| Citation |  Kerekes, AD; Esposite, SJ; Tagat, JR; Xiao, Y; Terracina, GA Aurora kinase inhibitors based on the imidazo[1,2-a]pyrazine core: fluorine and deuterium incorporation improve oral absorption and exposure. J Med Chem54:201-10 (2011) [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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| BDBM50329198 |
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| n/a |
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| Name | BDBM50329198 |
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| Synonyms: | 2-(ethyl((5-(6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-ylamino)isothiazol-3-yl)methyl)amino)-2-methylpropan-1-ol | 2-{ethyl[(5-{[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino}isothiazol-3-yl)methyl]amino}-2-methylpropan-1-ol | CHEMBL1232515 | CHEMBL1650533 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H26N8OS |
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| Mol. Mass. | 426.538 |
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| SMILES | CCN(Cc1cc(Nc2nc(C)cn3c(cnc23)-c2cn[nH]c2)sn1)C(C)(C)CO |
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| Structure | 
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