Reaction Details |
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Target | Protein kinase C alpha type |
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Ligand | BDBM3033 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_650126 (CHEMBL1219824) |
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IC50 | 3.7±n/a nM |
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Citation | Meredith, EL; Ardayfio, O; Beattie, K; Dobler, MR; Enyedy, I; Gaul, C; Hosagrahara, V; Jewell, C; Koch, K; Lee, W; Lehmann, H; McKinsey, TA; Miranda, K; Pagratis, N; Pancost, M; Patnaik, A; Phan, D; Plato, C; Qian, M; Rajaraman, V; Rao, C; Rozhitskaya, O; Ruppen, T; Shi, J; Siska, SJ; Springer, C; van Eis, M; Vega, RB; von Matt, A; Yang, L; Yoon, T; Zhang, JH; Zhu, N; Monovich, LG Identification of orally available naphthyridine protein kinase D inhibitors. J Med Chem53:5400-21 (2010) [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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BDBM3033 |
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n/a |
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Name | BDBM3033 |
Synonyms: | 3-{23-methyl-14-oxo-3,13,23-triazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17,19,21-nonaen-3-yl}propanenitrile | CHEMBL302449 | Go 6976 | Indolocarbazole deriv. |
Type | Small organic molecule |
Emp. Form. | C24H18N4O |
Mol. Mass. | 378.4259 |
SMILES | Cn1c2ccccc2c2c3C(=O)NCc3c3c4ccccc4n(CCC#N)c3c12 |
Structure |
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