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Target
Protein kinase C beta type
Ligand
BDBM50150698
Substrate
n/a
Meas. Tech.
ChEMBL_304975 (CHEMBL829308)
IC50
1100±n/a nM
Citation
 Engler, TA; Henry, JR; Malhotra, S; Cunningham, B; Furness, K; Brozinick, J; Burkholder, TP; Clay, MP; Clayton, J; Diefenbacher, C; Hawkins, E; Iversen, PW; Li, Y; Lindstrom, TD; Marquart, AL; McLean, J; Mendel, D; Misener, E; Briere, D; O'Toole, JC; Porter, WJ; Queener, S; Reel, JK; Owens, RA; Brier, RA; Eessalu, TE; Wagner, JR; Campbell, RM; Vaughn, R Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3. J Med Chem 47:3934-7 (2004) [PubMed]  Article 
Target
Name:
Protein kinase C beta type
Synonyms:
KPCB_HUMAN | PKC alpha and beta-2 | PKC beta | PKC beta isoform 2 | PKCB | PRKCB | PRKCB1 | Protein Kinase C, beta II | Protein kinase C beta type | Protein kinase C beta type II (PRKCB2)
Type:
Enzyme
Mol. Mass.:
76873.67
Organism:
Homo sapiens (Human)
Description:
The recombinant human PKC enzymes were produced using a baculovirus expression system in SF9 cells
Residue:
671
Sequence:
MADPAAGPPPSEGEESTVRFARKGALRQKNVHEVKNHKFTARFFKQPTFCSHCTDFIWGFGKQGFQCQVCCFVVHKRCHEFVTFSCPGADKGPASDDPRSKHKFKIHTYSSPTFCDHCGSLLYGLIHQGMKCDTCMMNVHKRCVMNVPSLCGTDHTERRGRIYIQAHIDRDVLIVLVRDAKNLVPMDPNGLSDPYVKLKLIPDPKSESKQKTKTIKCSLNPEWNETFRFQLKESDKDRRLSVEIWDWDLTSRNDFMGSLSFGISELQKASVDGWFKLLSQEEGEYFNVPVPPEGSEANEELRQKFERAKISQGTKVPEEKTTNTVSKFDNNGNRDRMKLTDFNFLMVLGKGSFGKVMLSERKGTDELYAVKILKKDVVIQDDDVECTMVEKRVLALPGKPPFLTQLHSCFQTMDRLYFVMEYVNGGDLMYHIQQVGRFKEPHAVFYAAEIAIGLFFLQSKGIIYRDLKLDNVMLDSEGHIKIADFGMCKENIWDGVTTKTFCGTPDYIAPEIIAYQPYGKSVDWWAFGVLLYEMLAGQAPFEGEDEDELFQSIMEHNVAYPKSMSKEAVAICKGLMTKHPGKRLGCGPEGERDIKEHAFFRYIDWEKLERKEIQPPYKPKARDKRDTSNFDKEFTRQPVELTPTDKLFIMNLDQNEFAGFSYTNPEFVINV
  
Inhibitor
Name:
BDBM50150698
Synonyms:
3-(imidazo[1,2-a]pyridin-3-yl)-4-(2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-1H-pyrrole-2,5-dione | 3-Imidazo[1,2-a]pyridin-3-yl-4-[2-(morpholine-4-carbonyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl]-pyrrole-2,5-dione | CHEMBL178737
Type:
Small organic molecule
Emp. Form.:
C27H24N6O4
Mol. Mass.:
496.5173
SMILES:
O=C(N1CCOCC1)N1CCn2cc(C3=C(C(=O)NC3=O)c3cnc4ccccn34)c3cccc(C1)c23 |t:15|
Structure:
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