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Literature summary for 1.13.11.52 extracted from

  • Serafini, M.; Torre, E.; Aprile, S.; Grosso, E.D.; Gesu, A.; Griglio, A.; Colombo, G.; Travelli, C.; Paiella, S.; Adamo, A.; Orecchini, E.; Coletti, A.; Pallotta, M.T.; Ugel, S.; Massarotti, A.; Pirali, T.; Fallarini, S.
    Discovery of highly potent benzimidazole derivatives as indoleamine 2,3-dioxygenase-1 (IDO1) inhibitors from structure-based virtual screening to in vivo pharmacodynamic activity (2020), J. Med. Chem., 63, 3047-3065 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
-
Mus musculus
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide selective inhibitor of IDO1 against L-Trp dioxygenase (TDO) at 0.001 mM, yet when the concentration is increased up to 0.010 mM, an inhibition of TDO is observed to some extent Mus musculus
N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
-
Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus P28776
-
-

Synonyms

Synonyms Comment Organism
IDO1
-
Mus musculus
indoleamine 2,3-dioxygenase-1
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000546
-
pH and temperature not specified in the publication, in cell line P1.TDO Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
0.0000093
-
pH and temperature not specified in the publication, in cell line P1.IDO1 Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
0.0000127
-
pH and temperature not specified in the publication, in cell line P1.IDO1 Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-bromo-1H-pyrrole-2-carboxamide
0.0000132
-
pH and temperature not specified in the publication, in cell line P1.TDO Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-1H-indole-2-carboxamide
0.0000323
-
pH and temperature not specified in the publication, in cell line P1.TDO Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide
0.000112
-
pH and temperature not specified in the publication, in cell line P1.IDO1 Mus musculus N-(3-((1H-benzo[d]imidazol-1-yl)methyl)benzyl)-4-cyanobenzamide