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Target
Protein kinase C gamma type
Ligand
BDBM50133065
Substrate
n/a
Meas. Tech.
ChEMBL_161149 (CHEMBL767417)
IC50
5170±n/a nM
Citation
Kuo, GH; Prouty, C; DeAngelis, A; Shen, L; O'Neill, DJ; Shah, C; Connolly, PJ; Murray, WV; Conway, BR; Cheung, P; Westover, L; Xu, JZ; Look, RA; Demarest, KT; Emanuel, S; Middleton, SA; Jolliffe, L; Beavers, MP; Chen, X Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors. J Med Chem 46:4021-31 (2003) [PubMed] Article
More Info.:
Target
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
Residue:
697
Sequence:
MAGLGPGVGDSEGGPRPLFCRKGALRQKVVHEVKSHKFTARFFKQPTFCSHCTDFIWGIGKQGLQCQVCSFVVHRRCHEFVTFECPGAGKGPQTDDPRNKHKFRLHSYSSPTFCDHCGSLLYGLVHQGMKCSCCEMNVHRRCVRSVPSLCGVDHTERRGRLQLEIRAPTADEIHVTVGEARNLIPMDPNGLSDPYVKLKLIPDPRNLTKQKTRTVKATLNPVWNETFVFNLKPGDVERRLSVEVWDWDRTSRNDFMGAMSFGVSELLKAPVDGWYKLLNQEEGEYYNVPVADADNCSLLQKFEACNYPLELYERVRMGPSSSPIPSPSPSPTDPKRCFFGASPGRLHISDFSFLMVLGKGSFGKVMLAERRGSDELYAIKILKKDVIVQDDDVDCTLVEKRVLALGGRGPGGRPHFLTQLHSTFQTPDRLYFVMEYVTGGDLMYHIQQLGKFKEPHAAFYAAEIAIGLFFLHNQGIIYRDLKLDNVMLDAEGHIKITDFGMCKENVFPGTTTRTFCGTPDYIAPEIIAYQPYGKSVDWWSFGVLLYEMLAGQPPFDGEDEEELFQAIMEQTVTYPKSLSREAVAICKGFLTKHPGKRLGSGPDGEPTIRAHGFFRWIDWERLERLEIPPPFRPRPCGRSGENFDKFFTRAAPALTPPDRLVLASIDQADFQGFTYVNPDFVHPDARSPTSPVPVPVM
Inhibitor
Name:
BDBM50133065
Synonyms:
17,20,23,26,29-pentaoxa-4,14,32-triazahexacyclo[30.6.1.17,14.02,6.08,13.033,38]tetraconta-1(39),2(6),7(40),8,10,12,33,35,37-nonaene-3,5-dione | CHEMBL130774
Type:
Small organic molecule
Emp. Form.:
C32H35N3O7
Mol. Mass.:
573.6362
SMILES:
O=C1NC(=O)C2=C1c1cn(CCOCCOCCOCCOCCOCCn3cc2c2ccccc32)c2ccccc12 |c:5|