| Reaction Details |
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 | Report a problem with these data |
| Target | Protein kinase C alpha type |
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| Ligand | BDBM50257409 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEBML_1689806 |
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| IC50 | 7200±n/a nM |
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| Citation |  Okawa, T; Aramaki, Y; Yamamoto, M; Kobayashi, T; Fukumoto, S; Toyoda, Y; Henta, T; Hata, A; Ikeda, S; Kaneko, M; Hoffman, ID; Sang, BC; Zou, H; Kawamoto, T Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem60:6942-6990 (2017) [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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| BDBM50257409 |
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| n/a |
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| Name | BDBM50257409 |
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| Synonyms: | CHEMBL4087117 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H21N5O |
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| Mol. Mass. | 383.4457 |
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| SMILES | O=C(NCc1ccccc1)c1cccc(NCc2cc(n[nH]2)-c2ccncc2)c1 |
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| Structure | 
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