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Target
Protein kinase C gamma type
Ligand
BDBM50204693
Substrate
n/a
Meas. Tech.
ChEMBL_442108 (CHEMBL891246)
IC50
4900±n/a nM
Citation
 Tong, Y; Claiborne, A; Stewart, KD; Park, C; Kovar, P; Chen, Z; Credo, RB; Gu, WZ; Gwaltney, SL; Judge, RA; Zhang, H; Rosenberg, SH; Sham, HL; Sowin, TJ; Lin, NH Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem 15:2759-67 (2007) [PubMed]  Article 
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:
BDBM50204693
Synonyms:
3-(4'-hydroxy-biphenyl-4-yl)-1,4-dihydro-indeno[1,2-c]pyrazole-6-carboxylic acid (pyridin-4-ylmethyl)-amide | CHEMBL242753
Type:
Small organic molecule
Emp. Form.:
C29H22N4O2
Mol. Mass.:
458.5106
SMILES:
Oc1ccc(cc1)-c1ccc(cc1)-c1n[nH]c-2c1Cc1cc(ccc-21)C(=O)NCc1ccncc1
Structure:
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