| Reaction Details |
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 | Report a problem with these data |
| Target | Protein kinase C alpha type |
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| Ligand | BDBM50168392 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_304719 (CHEMBL827159) |
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| IC50 | >50000±n/a nM |
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| Citation |  Borzilleri, RM; Zheng, X; Qian, L; Ellis, C; Cai, ZW; Wautlet, BS; Mortillo, S; Jeyaseelan, R; Kukral, DW; Fura, A; Kamath, A; Vyas, V; Tokarski, JS; Barrish, JC; Hunt, JT; Lombardo, LJ; Fargnoli, J; Bhide, RS Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors. J Med Chem48:3991-4008 (2005) [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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| BDBM50168392 |
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| n/a |
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| Name | BDBM50168392 |
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| Synonyms: | CHEMBL370266 | [4-(2,4-Difluoro-5-methoxycarbamoyl-phenylamino)-5-isopropyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid tetrahydro-furan-2-ylmethyl ester |
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| Type | Small organic molecule |
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| Emp. Form. | C23H26F2N6O5 |
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| Mol. Mass. | 504.4865 |
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| SMILES | CONC(=O)c1cc(Nc2ncnn3cc(NC(=O)OCC4CCCO4)c(C(C)C)c23)c(F)cc1F |
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| Structure | 
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