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Target
Protein kinase C beta type
Ligand
BDBM50163000
Substrate
n/a
Meas. Tech.
ChEMBL_305828 (CHEMBL829570)
IC50
62±n/a nM
Citation
Zhang, HC; Derian, CK; McComsey, DF; White, KB; Ye, H; Hecker, LR; Li, J; Addo, MF; Croll, D; Eckardt, AJ; Smith, CE; Li, Q; Cheung, WM; Conway, BR; Emanuel, S; Demarest, KT; Andrade-Gordon, P; Damiano, BP; Maryanoff, BE Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety. J Med Chem 48:1725-8 (2005) [PubMed] Article
More Info.:
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:
BDBM50163000
Synonyms:
3-(1-Piperazin-1-yl-1H-indazol-3-yl)-4-[1-(1,4,4a,8a-tetrahydro-naphthalen-2-yl)-1H-indol-3-yl]-pyrrole-2,5-dione | CHEMBL175845
Type:
Small organic molecule
Emp. Form.:
C37H34N6O2
Mol. Mass.:
594.7049
SMILES:
CN1CCN(CCCn2nc(C3=C(C(=O)NC3=O)c3cn(-c4ccc5ccccc5c4)c4ccccc34)c3ccccc23)CC1 |t:11|