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Target
Protein-glutamine gamma-glutamyltransferase 2
Ligand
BDBM50342597
Substrate
n/a
Meas. Tech.
ChEMBL_744966 (CHEMBL1771981)
IC50
1200±n/a nM
Citation
 Klöck, C; Jin, X; Choi, K; Khosla, C; Madrid, PB; Spencer, A; Raimundo, BC; Boardman, P; Lanza, G; Griffin, JH Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2. Bioorg Med Chem Lett 21:2692-6 (2011) [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:
BDBM50342597
Synonyms:
(E)-methyl 4-((4-chloro-2-oxo-3-(2-oxo-2-(pyridin-3-yl)ethylidene)indolin-1-yl)methyl)benzoate | CHEMBL1770537
Type:
Small organic molecule
Emp. Form.:
C24H17ClN2O4
Mol. Mass.:
432.856
SMILES:
COC(=O)c1ccc(CN2C(=O)\C(=C\C(=O)c3cccnc3)c3c2cccc3Cl)cc1
Structure:
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