Reaction Details |
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Target | Protein kinase C alpha type |
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Ligand | BDBM17055 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_162574 (CHEMBL768516) |
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IC50 | 360±n/a nM |
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Citation | Jirousek, MR; Gillig, JR; Gonzalez, CM; Heath, WF; McDonald, JH; Neel, DA; Rito, CJ; Singh, U; Stramm, LE; Melikian-Badalian, A; Baevsky, M; Ballas, LM; Hall, SE; Winneroski, LL; Faul, MM (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J Med Chem39:2664-71 (1996) [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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BDBM17055 |
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n/a |
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Name | BDBM17055 |
Synonyms: | (18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.1^{7,14}.0^{2,6}.0^{8,13}.0^{22,27}]nonacosa-1(28),2(6),7(29),8(13),9,11,22(27),23,25-nonaene-3,5-dione | (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-di(metheno)dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione | K00587a | LY 333531 | LY-333531 | LY333531 | Ruboxistaurin | cid_153999 |
Type | Small organic molecule |
Emp. Form. | C28H28N4O3 |
Mol. Mass. | 468.5469 |
SMILES | CN(C)C[C@@H]1CCn2cc(C3=C(C(=O)NC3=O)c3cn(CCO1)c1ccccc31)c1ccccc21 |r,t:10| |
Structure |
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