Target
Protein kinase C beta type
Ligand
BDBM50343559
Substrate
n/a
Meas. Tech.
ChEMBL_745937 (CHEMBL1776307)
IC50
>10000±n/a nM
Citation
 Beria, IBossi, RTBrasca, MGCaruso, MCeccarelli, WFachin, GFasolini, MForte, BFiorentini, FPesenti, EPezzetta, DPosteri, HScolaro, ARe Depaolini, SValsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett 21:2969-74 (2011) [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:
BDBM50343559
Synonyms:
1-(2-HYDROXYETHYL)-8-[[5-(4-METHYLPIPERAZIN-1-YL)-2-(TRIFLUOROMETHOXY)PHENYL]AMINO]-4,5-DIHYDROPYRIMIDO[5,4-G]INDAZOLE-3-CARBOXAMIDE | 1-(2-hydroxyethyl)-8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1738758
Type:
Small organic molecule
Emp. Form.:
C24H27F3N8O3
Mol. Mass.:
532.5182
SMILES:
CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCO)c4-c3n2)C(N)=O)c1
Structure:
Search PDB for entries with ligand similarity: