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Literature summary extracted from
- Selective irreversible inhibitors of the Wnt-deacylating enzyme NOTUM developed by activity-based protein profiling (2018), ACS Med. Chem. Lett., 9, 563-568 .
Application
| EC Number | Application | Comment | Organism |
|---|---|---|---|
| 3.1.1.98 | drug development | NOTUM inhibitors have potential for treating degenerative diseases | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.1.1.98 | 2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]-7-[(6-phenoxypyridin-3-yl)methyl]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens |  |
| 3.1.1.98 | 7-(4-chlorobenzoyl)-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens | |
| 3.1.1.98 | 7-(4-chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl 2,3-dihydro-4Hbenzo[b][1,4]oxazine-4-carboxylate | i.e. ABC99, selective irreversible inhibitor. The optimized -hydroxyhydantoin carbamate inhibitor preserves Wnt-mediated cell signaling in the presence of NOTUM and is also converted into an ABPP probe for visualizing NOTUM in native biological systems | Homo sapiens | |
| 3.1.1.98 | 7-[(2-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens | |
| 3.1.1.98 | 7-[(3-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens | |
| 3.1.1.98 | 7-[(4-bromophenyl)methyl]-2-[[4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens | |
| 3.1.1.98 | 7-[(4-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | - |
Homo sapiens | |
| 3.1.1.98 | 7-[(4-chlorophenyl)methyl]-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | the optimized N-hydroxyhydantoin carbamate inhibitor preserves Wnt-mediated cell signaling in the presence of NOTUM and is also converted into an activity-based protein profiling (ABPP) probe for visualizing NOTUM in native biological systems. NOTUM inhibitors have potential for treating degenerative diseases | Homo sapiens | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 3.1.1.98 | 54000 | - |
calculated from sequence | Homo sapiens |
Natural Substrates/ Products (Substrates)
| EC Number | Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.1.98 | [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O | Homo sapiens | the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase | [Wnt]-L-serine + (9Z)-hexadec-9-enoate | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.1.1.98 | Homo sapiens | - |
- |
- |
| 3.1.1.98 | Homo sapiens | Q6P988 | - |
- |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.1.1.98 | SW-620 cell | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.1.1.98 | [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O | - |
Homo sapiens | [Wnt]-L-serine + (9Z)-hexadec-9-enoate | - |
? | |
| 3.1.1.98 | [Wnt]-O-(9Z)-hexadec-9-enoyl-L-serine + H2O | the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase | Homo sapiens | [Wnt]-L-serine + (9Z)-hexadec-9-enoate | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.1.1.98 | Notum | - |
Homo sapiens |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.1.1.98 | 0.000013 | - |
pH and temperature not specified in the publication | Homo sapiens | 7-(4-chlorobenzyl)-1,3-dioxohexahydroimidazo[1,5-a]pyrazin-2(3H)-yl 2,3-dihydro-4Hbenzo[b][1,4]oxazine-4-carboxylate | |
| 3.1.1.98 | 0.000013 | - |
IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-[(4-chlorophenyl)methyl]-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.0002 | - |
IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-[(2-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.00029 | - |
IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-[(4-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.000677 | - |
IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-[(4-bromophenyl)methyl]-2-[[4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.001506 | - |
IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]-7-[(6-phenoxypyridin-3-yl)methyl]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.01 | - |
above 0.01 mM, IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-[(3-chlorophenyl)methyl]-2-([4-(4-methoxyphenyl)piperazine-1-carbonyl]oxy)tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
| 3.1.1.98 | 0.01 | - |
above 0.01 mM, IC50 value is determined by competitive gel-based activity-based protein profiling, pH and temperature not specified in the publication | Homo sapiens | 7-(4-chlorobenzoyl)-2-[(2,3-dihydro-4H-1,4-benzoxazine-4-carbonyl)oxy]tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-dione | |
General Information
| EC Number | General Information | Comment | Organism |
|---|---|---|---|
| 3.1.1.98 | metabolism | the enzyme removes the palmitoleate modification that is introduced to specific L-serine residues in Wnt proteins by [Wnt protein]-O-palmitoleoyl transferase | Homo sapiens |
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