Target
Protein-glutamine gamma-glutamyltransferase 2
Ligand
BDBM185155
Substrate
n/a
Meas. Tech.
TG Activity Assays
IC50
1.4e+3± 5e+2 nM
Citation
 Badarau, EWang, ZRathbone, DLCostanzi, AThibault, TMurdoch, CEEl Alaoui, SBartkeviciute, MGriffin, M Development of Potent and Selective Tissue Transglutaminase Inhibitors: Their Effect on TG2 Function and Application in Pathological Conditions. Chem Biol 22:1347-61 (2015) [PubMed]  Article 
Target
Name:
Protein-glutamine gamma-glutamyltransferase 2
Synonyms:
Protein-glutamine gamma-glutamyltransferase | Protein-glutamine gamma-glutamyltransferase 2 (TG2) | TGM2 | TGM2_HUMAN | Tissue transglutaminase | Tissue transglutaminase (TG2) | Transglutaminase 2 (TGM2) | Transglutaminase C | Transglutaminase-2
Type:
Protein
Mol. Mass.:
77309.30
Organism:
Homo sapiens (Human)
Description:
P21980
Residue:
687
Sequence:
MAEELVLERCDLELETNGRDHHTADLCREKLVVRRGQPFWLTLHFEGRNYEASVDSLTFSVVTGPAPSQEAGTKARFPLRDAVEEGDWTATVVDQQDCTLSLQLTTPANAPIGLYRLSLEASTGYQGSSFVLGHFILLFNAWCPADAVYLDSEEERQEYVLTQQGFIYQGSAKFIKNIPWNFGQFEDGILDICLILLDVNPKFLKNAGRDCSRRSSPVYVGRVVSGMVNCNDDQGVLLGRWDNNYGDGVSPMSWIGSVDILRRWKNHGCQRVKYGQCWVFAAVACTVLRCLGIPTRVVTNYNSAHDQNSNLLIEYFRNEFGEIQGDKSEMIWNFHCWVESWMTRPDLQPGYEGWQALDPTPQEKSEGTYCCGPVPVRAIKEGDLSTKYDAPFVFAEVNADVVDWIQQDDGSVHKSINRSLIVGLKISTKSVGRDEREDITHTYKYPEGSSEEREAFTRANHLNKLAEKEETGMAMRIRVGQSMNMGSDFDVFAHITNNTAEEYVCRLLLCARTVSYNGILGPECGTKYLLNLNLEPFSEKSVPLCILYEKYRDCLTESNLIKVRALLVEPVINSYLLAERDLYLENPEIKIRILGEPKQKRKLVAEVSLQNPLPVALEGCTFTVEGAGLTEEQKTVEIPDPVEAGEEVKVRMDLLPLHMGLHKLVVNFESDKLKAVKGFRNVIIGPA
  
Inhibitor
Name:
BDBM185155
Synonyms:
[2-[[2-(4-Benzyloxycarbonylpiperazin-1-yl)-2-oxo-ethyl]amino]-2-oxo-ethyl]-dimethylsulfonium bromide (1a)
Type:
Small organic molecule
Emp. Form.:
C18H26N3O4S
Mol. Mass.:
380.481
SMILES:
C[S+](C)CC(=O)NCC(=O)N1CCN(CC1)C(=O)OCc1ccccc1
Structure:
Search PDB for entries with ligand similarity: