Reaction Details Report a problem with these data
Target
Protein kinase C gamma type
Ligand
BDBM50249959
Substrate
n/a
Meas. Tech.
ChEMBL_498040 (CHEMBL1000243)
Ki
16±n/a nM
Citation
Comin, MJ; Czifra, G; Kedei, N; Telek, A; Lewin, NE; Kolusheva, S; Velasquez, JF; Kobylarz, R; Jelinek, R; Blumberg, PM; Marquez, VE Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths. J Med Chem 52:3274-83 (2009) [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:
BDBM50249959
Synonyms:
CHEMBL522428 | [2-(Hydroxymethyl)-4-(methylethylidene)-5-oxo-2-2,3-dihydrofuryl]methyl 4-[2-(4-Methylphenyl)ethynyl]benzoate
Type:
Small organic molecule
Emp. Form.:
C25H24O5
Mol. Mass.:
404.4551
SMILES:
[#6]\[#6](-[#6])=[#6]-1/[#6]C([#6]-[#8])([#6]-[#8]-[#6](=O)-c2ccc(cc2)C#Cc2ccc(-[#6])cc2)[#8]-[#6]-1=O