Reaction Details |
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Target | Protein kinase C alpha type |
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Ligand | BDBM50377357 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_479565 (CHEMBL929429) |
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IC50 | >50000±n/a nM |
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Citation | Ruel, R; Thibeault, C; L'Heureux, A; Martel, A; Cai, ZW; Wei, D; Qian, L; Barrish, JC; Mathur, A; D'Arienzo, C; Hunt, JT; Kamath, A; Marathe, P; Zhang, Y; Derbin, G; Wautlet, B; Mortillo, S; Jeyaseelan, R; Henley, B; Tejwani, R; Bhide, RS; Trainor, GL; Fargnoli, J; Lombardo, LJ Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor. Bioorg Med Chem Lett18:2985-9 (2008) [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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BDBM50377357 |
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n/a |
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Name | BDBM50377357 |
Synonyms: | CHEMBL258694 |
Type | Small organic molecule |
Emp. Form. | C19H18N8O |
Mol. Mass. | 374.3992 |
SMILES | CC(C)c1c(cn2ncnc(Nc3cnc4[nH]ccc4c3)c12)-c1nnc(C)o1 |
Structure |
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