Reaction Details |
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Target | Protein kinase C eta type |
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Ligand | BDBM50313569 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_614206 (CHEMBL1105156) |
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IC50 | 120±n/a nM |
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Citation | Boschelli, DH; Subrath, J; Niu, C; Wu, B; Wang, Y; Lee, J; Brennan, A; Ho, M; Deng, B; Yang, X; Xu, X; Leung, L; Wang, J; Atherton, J; Chaudhary, D Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors. Bioorg Med Chem Lett20:1965-8 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C eta type |
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Name: | Protein kinase C eta type |
Synonyms: | KPCL_HUMAN | PKC-L | PKCL | PRKCH | PRKCL | Protein Kinase C, eta | Protein kinase C, PKC; classical/novel | nPKC-eta |
Type: | Enzyme |
Mol. Mass.: | 77844.26 |
Organism: | Homo sapiens (Human) |
Description: | The recombinant human PKC enzymes were
produced using a baculovirus expression system in SF9 cells |
Residue: | 683 |
Sequence: | MSSGTMKFNGYLRVRIGEAVGLQPTRWSLRHSLFKKGHQLLDPYLTVSVDQVRVGQTSTK
QKTNKPTYNEEFCANVTDGGHLELAVFHETPLGYDHFVANCTLQFQELLRTTGASDTFEG
WVDLEPEGKVFVVITLTGSFTEATLQRDRIFKHFTRKRQRAMRRRVHQINGHKFMATYLR
QPTYCSHCREFIWGVFGKQGYQCQVCTCVVHKRCHHLIVTACTCQNNINKVDSKIAEQRF
GINIPHKFSIHNYKVPTFCDHCGSLLWGIMRQGLQCKICKMNVHIRCQANVAPNCGVNAV
ELAKTLAGMGLQPGNISPTSKLVSRSTLRRQGKESSKEGNGIGVNSSNRLGIDNFEFIRV
LGKGSFGKVMLARVKETGDLYAVKVLKKDVILQDDDVECTMTEKRILSLARNHPFLTQLF
CCFQTPDRLFFVMEFVNGGDLMFHIQKSRRFDEARARFYAAEIISALMFLHDKGIIYRDL
KLDNVLLDHEGHCKLADFGMCKEGICNGVTTATFCGTPDYIAPEILQEMLYGPAVDWWAM
GVLLYEMLCGHAPFEAENEDDLFEAILNDEVVYPTWLHEDATGILKSFMTKNPTMRLGSL
TQGGEHAILRHPFFKEIDWAQLNHRQIEPPFRPRIKSREDVSNFDPDFIKEEPVLTPIDE
GHLPMINQDEFRNFSYVSPELQP
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BDBM50313569 |
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n/a |
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Name | BDBM50313569 |
Synonyms: | (E)-4-(4-methyl-1H-indol-5-ylamino)-5-(2-(6-((4-methylpiperazin-1-yl)methyl)pyridin-2-yl)vinyl)nicotinonitrile | CHEMBL1084411 |
Type | Small organic molecule |
Emp. Form. | C28H29N7 |
Mol. Mass. | 463.5768 |
SMILES | CN1CCN(Cc2cccc(\C=C\c3cncc(C#N)c3Nc3ccc4[nH]ccc4c3C)n2)CC1 |
Structure |
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