Reaction Details |
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Target | Protein kinase C gamma type |
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Ligand | BDBM50049439 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1455517 (CHEMBL3364570) |
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IC50 | 13000±n/a nM |
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Citation | George, DM; Breinlinger, EC; Friedman, M; Zhang, Y; Wang, J; Argiriadi, M; Bansal-Pakala, P; Barth, M; Duignan, DB; Honore, P; Lang, Q; Mittelstadt, S; Potin, D; Rundell, L; Edmunds, JJ Discovery of selective and orally bioavailable protein kinase C¿ (PKC¿) inhibitors from a fragment hit. J Med Chem58:222-36 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein kinase C gamma type |
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Name: | Protein kinase C gamma type |
Synonyms: | KPCG_HUMAN | PKC gamma | PKC-gamma | PKCG | PRKCG | Protein kinase C gamma | Protein kinase C gamma type | Protein kinase C, PKC; classical/novel | Protein kinase C, gamma |
Type: | Enzyme |
Mol. Mass.: | 78458.05 |
Organism: | Homo sapiens (Human) |
Description: | The recombinant human PKC enzymes were
produced using a baculovirus expression system in SF9 cells
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Residue: | 697 |
Sequence: | MAGLGPGVGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIG
KQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSL
LYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTADEIHVTVGEA
RNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTRTVKATLNPVWNETFVFNLKPGDVERRL
SVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQ
KFEACNYPLELYERVRMGPSSSPIPSPSPSPTDPKRCFFGASPGRLHISDFSFLMVLGKG
SFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQL
HSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRD
LKLDNVMLDAEGHIKITDFGMCKENVFPGTTTRTFCGTPDYIAPEIIAYQPYGKSVDWWS
FGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGS
GPDGEPTIRAHGFFRWIDWERLERLEIPPPFRPRPCGRSGENFDKFFTRAAPALTPPDRL
VLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM
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BDBM50049439 |
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n/a |
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Name | BDBM50049439 |
Synonyms: | CHEMBL3356472 |
Type | Small organic molecule |
Emp. Form. | C20H21N5O2 |
Mol. Mass. | 363.413 |
SMILES | C[C@H]1N2C(COc3cc(c(NC4CNC4)cc23)-c2ccccc2)=NNC1=O |r,c:26| |
Structure |
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