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Literature summary extracted from

  • Murafuji, H.; Muto, T.; Goto, M.; Imajo, S.; Sugawara, H.; Oyama, Y.; Minamitsuji, Y.; Miyazaki, S.; Murai, K.; Fujioka, H.
    Discovery and structure-activity relationship of imidazolinylindole derivatives as kallikrein 7 inhibitors (2019), Bioorg. Med. Chem. Lett., 29, 334-338 .
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
3.4.21.117 in complex with inhibitor 1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole. 2-Chlorobenzene inserts into the S1 pocket, the methyl group on the imidazoline ring is located at the S2 site composed of side chains of His99, Asp102, His57, and Ser214 Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.117 1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
-
 Homo sapiens
3.4.21.117 1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
-
 Mus musculus
3.4.21.117 1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
-
 Homo sapiens
3.4.21.117 1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.117 Homo sapiens P49862
-
-
3.4.21.117 Mus musculus Q91VE3
-
-

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.117 0.00039
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
3.4.21.117 0.0004
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus 1-(2-bromobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
3.4.21.117 0.0012
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole
3.4.21.117 0.0015
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus 1-(2-chlorobenzene-1-sulfonyl)-5-methyl-3-(2-methyl-4,5-dihydro-1H-imidazol-4-yl)-1H-indole