Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.59 extracted from

  • Costanzo, M.J.; Yabut, S.C.; Zhang, H.C.; White, K.B.; de Garavilla, L.; Wang, Y.; Minor, L.K.; Tounge, B.A.; Barnakov, A.N.; Lewandowski, F.; Milligan, C.; Spurlino, J.C.; Abraham, W.M.; Boswell-Smith, V.; Page, C.P.; Maryanoff, B.E.
    Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives (2008), Bioorg. Med. Chem. Lett., 18, 2114-2121.
    View publication on PubMed
Search for more literature for 3.4.21.59

Inhibitors

Inhibitors Comment Organism Structure
4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboxamide
-
 Homo sapiens
4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboximidamide
-
 Homo sapiens
JNJ-27390467
-
 Homo sapiens
additional information synthesis and inhibitory potency of spirocyclic piperidine amide derivatives as enzyme inhibitors, overview Homo sapiens
RWJ-56423
-
 Homo sapiens
RWJ-58643
-
 Homo sapiens
[1'-(acetyloxy)-5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[5'-(aminomethyl)-1'-[(methylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[5'-(aminomethyl)-1'-[(phenylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl](5-benzylfuran-2-yl)methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(2-phenylethyl)furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylsulfanyl)furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-chlorophenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-fluorophenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methoxyphenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methylphenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-hydroxyphenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-methylphenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-tert-butylphenyl)ethynyl]furan-2-yl]methanone
-
 Homo sapiens
[5-[(1E)-1-aminoprop-1-en-1-yl]spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens
[6'-(aminomethyl)-2',3'-dihydrospiro[cyclohexane-1,1'-inden]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation from lung Homo sapiens
-
lung commercial preparation Homo sapiens
-
mast cell
-
 Homo sapiens
-

Subunits

Subunits Comment Organism
tetramer
-
 Homo sapiens

Synonyms

Synonyms Comment Organism
beta-tryptase
-
 Homo sapiens
Mast cell tryptase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000012
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methylphenyl)ethynyl]furan-2-yl]methanone
0.0000018
-
 pH 7.4, 37°C Homo sapiens [5'-(aminomethyl)-1'-[(methylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
0.0000031
-
 pH 7.4, 37°C Homo sapiens [6'-(aminomethyl)-2',3'-dihydrospiro[cyclohexane-1,1'-inden]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
0.0000036
-
 pH 7.4, 37°C Homo sapiens JNJ-27390467
0.0000043
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-fluorophenyl)ethynyl]furan-2-yl]methanone
0.0000045
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
0.0000052
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-chlorophenyl)ethynyl]furan-2-yl]methanone
0.0000057
-
 pH 7.4, 37°C Homo sapiens [5'-(aminomethyl)-1'-[(phenylsulfinyl)oxy]-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
0.0000083
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-methylphenyl)ethynyl]furan-2-yl]methanone
0.000013
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(2-methoxyphenyl)ethynyl]furan-2-yl]methanone
0.000015
-
 pH 7.4, 37°C Homo sapiens [1'-(acetyloxy)-5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
0.000023
-
 pH 7.4, 37°C Homo sapiens [5'-(aminomethyl)-1',2'-dihydrospiro[cyclohexane-1,3'-indol]-4-yl][5-(phenylethynyl)furan-2-yl]methanone
0.000028
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl](5-benzylfuran-2-yl)methanone
0.000059
-
 pH 7.4, 37°C Homo sapiens [5-[(1E)-1-aminoprop-1-en-1-yl]spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylethynyl)furan-2-yl]methanone
0.000082
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(2-phenylethyl)furan-2-yl]methanone
0.00009
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-(phenylsulfanyl)furan-2-yl]methanone
0.0007
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-tert-butylphenyl)ethynyl]furan-2-yl]methanone
0.00078
-
 pH 7.4, 37°C Homo sapiens 4'-[[5-(phenylethynyl)furan-2-yl]carbonyl]spiro[1-benzofuran-3,1'-cyclohexane]-5-carboximidamide
0.0032
-
 pH 7.4, 37°C Homo sapiens [5-(aminomethyl)spiro[1-benzofuran-3,1'-cyclohexan]-4'-yl][5-[(4-hydroxyphenyl)ethynyl]furan-2-yl]methanone