Application | Comment | Organism |
---|---|---|
drug development | extensive clinical use, high bioavailability and relatively low toxicity of dicoumarols suggests that the dicoumarol structure will be a good starting point for development of drug-like inhibitors of furin and other proprotein convertases that can act both intracellularly and at the cell surface | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
plasmid pEFGRAPfurin expressed in CHO cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(E)-N-((E)-5-(2-chloro-5-nitrobenzylidene)-4-oxothiazolidin-2-ylidene)-4-methylbenzenesulfonamide | competitive inhibitor | Homo sapiens | |
(N'Z,N''Z)-4,4'-oxybis(N'-(2-hydroxybenzylidene)benzenesulfonohydrazide) | competitive inhibitor | Homo sapiens | |
2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid | noncompetitive inhibitor | Homo sapiens | |
3'-oxo-6a,14a-dihydro-3'H-spiro[dibenzo[c,h]xanthene-7,1'-isobenzofuran]-3,11-diyl diacetate | - |
Homo sapiens | |
3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-((2-bromophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-((2-chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-((3,4,5-trimethoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-((4-isopropoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-(benzo[d][1,3]dioxol-5-ylmethylene)bis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3,3'-methylenebis(4-hydroxy-2H-chromen-2-one) | noncompetitive inhibitor | Homo sapiens | |
3-(alpha-acetonyl-benzyl)-4-(hydroxycoumarin) | - |
Homo sapiens | |
3-allyl-1-methyl-1,2,3,4-tetrahydroisoquinoline | competitive inhibitor | Homo sapiens | |
3-hydroxy-5-(4-methoxyphenyl)-2-(4-phenoxy-3-sulfophenyl)-3H-pyrazol-2-ium | competitive inhibitor | Homo sapiens | |
4-hydroxy-3-oxo-1-phenylbutylcoumarin | - |
Homo sapiens | |
4-Hydroxycoumarin | - |
Homo sapiens | |
6-oxo-6H-benzo[c]chromen-3-yl 2-chlorobenzoate | - |
Homo sapiens | |
methyl 4-(bis(4-hydroxy-2-oxo-2H-chromen-3-yl)methyl)benzoate | noncompetitive inhibitor | Homo sapiens | |
N''-[(1E)-[2-[(4-chlorobenzyl)oxy]phenyl]methylidene]carbonohydrazonic diamide | competitive inhibitor | Homo sapiens | |
N-(benzo[d][1,3]dioxol-5-yl)-1,2,3,4-tetrahydroacridin-9-amine | competitive inhibitor | Homo sapiens | |
N-(thiazol-2-yl)-4-(5-((2,4,6-trioxotetrahydropyrimidin-5(6H)-ylidene)methyl)furan-2-yl)benzenesulfonamide | competitive inhibitor | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0123 | - |
Ac-Arg-Val-Arg-Arg-4-nitroanilide | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cell surface | - |
Homo sapiens | 9986 | - |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Ac-Arg-Val-Arg-Arg-4-nitroanilide + H2O | - |
Homo sapiens | Ac-Arg-Val-Arg-Arg + 4-nitroaniline | - |
? | |
anthrax protective antigen precursor + H2O | - |
Homo sapiens | ? | - |
? | |
CPA95 + H2O | - |
Homo sapiens | ? | - |
? | |
membrane-type 1-matrix metalloproteinase + H2O | - |
Homo sapiens | ? | - |
? | |
N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-4-methylcoumarin 7-amide + H2O | - |
Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
Proprotein convertase | - |
Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00104 | - |
3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one) | with CPA95 as substrate | Homo sapiens | |
0.0033 | - |
3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one) | with CPA95 as substrate | Homo sapiens | |
0.00605 | - |
3,3'-(benzo[d][1,3]dioxol-5-ylmethylene)bis(4-hydroxy-2H-chromen-2-one) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.0118 | - |
N''-[(1E)-[2-[(4-chlorobenzyl)oxy]phenyl]methylidene]carbonohydrazonic diamide | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.012 | - |
2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid | with CPA95 as substrate/with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | |
0.0188 | - |
3,3'-methylenebis(4-hydroxy-2H-chromen-2-one) | with CPA95 as substrate | Homo sapiens | |
0.0208 | - |
3,3'-((4-isopropoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.022 | - |
3,3'-((3,4,5-trimethoxyphenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.0783 | - |
3,3'-((2-chlorophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.1452 | - |
methyl 4-(bis(4-hydroxy-2-oxo-2H-chromen-3-yl)methyl)benzoate | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
0.1851 | - |
3,3'-((2-bromophenyl)methylene)bis(4-hydroxy-2H-chromen-2-one) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
1.3 | - |
4-hydroxy-3-oxo-1-phenylbutylcoumarin | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
2 | - |
3-(alpha-acetonyl-benzyl)-4-(hydroxycoumarin) | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens | |
7.3 | - |
4-Hydroxycoumarin | with Ac-Arg-Val-Arg-Arg-4-nitroanilide as substrate | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.004 | - |
with CPA95 as substrate | Homo sapiens | 3,3'-((2,3-dihydro-1H-inden-5-yl)methylene)bis(4-hydroxy-2H-chromen-2-one) | |
0.007 | - |
with CPA95 as substrate/with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | 2-(11-hydroxy-3-oxo-3H-dibenzo[c,h]xanthen-7-yl)benzoic acid | |
0.011 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | N-(thiazol-2-yl)-4-(5-((2,4,6-trioxotetrahydropyrimidin-5(6H)-ylidene)methyl)furan-2-yl)benzenesulfonamide | |
0.02 | - |
with CPA95 as substrate | Homo sapiens | 3,3'-methylenebis(4-hydroxy-2H-chromen-2-one) | |
0.025 | - |
with CPA95 as substrate | Homo sapiens | 3'-oxo-6a,14a-dihydro-3'H-spiro[dibenzo[c,h]xanthene-7,1'-isobenzofuran]-3,11-diyl diacetate | |
0.028 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | 6-oxo-6H-benzo[c]chromen-3-yl 2-chlorobenzoate | |
0.051 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | 3-allyl-1-methyl-1,2,3,4-tetrahydroisoquinoline | |
0.055 | - |
with CPA95 as substrate | Homo sapiens | 3,3',3'',3'''-(1,4-phenylenebis(methanetriyl))tetrakis(4-hydroxy-2H-chromen-2-one) | |
0.084 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | (N'Z,N''Z)-4,4'-oxybis(N'-(2-hydroxybenzylidene)benzenesulfonohydrazide) | |
0.102 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | (E)-N-((E)-5-(2-chloro-5-nitrobenzylidene)-4-oxothiazolidin-2-ylidene)-4-methylbenzenesulfonamide | |
0.137 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | 3-hydroxy-5-(4-methoxyphenyl)-2-(4-phenoxy-3-sulfophenyl)-3H-pyrazol-2-ium | |
0.159 | - |
with N-tert-butoxycarbonyl-Arg-Val-Arg-Arg-methylcoumarin amide as substrate | Homo sapiens | N-(benzo[d][1,3]dioxol-5-yl)-1,2,3,4-tetrahydroacridin-9-amine |