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Literature summary for 2.3.1.22 extracted from
- Monoacylglycerol acyltransferase 2 (MGAT2) inhibitors for the treatment of metabolic diseases and nonalcoholic steatohepatitis (NASH) (2018), J. Med. Chem., 61, 9879-9888 .
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| (1S)-4'-(2-cyclopropyl-3H-pyrrol-4-yl)-5'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-5-(4,4,4-trifluorobutoxy)-2,3-dihydro-1'H-spiro[indene-1,2'-pyridin]-6'(3'H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens |  |
| (3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| (3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Mus musculus | |
| (6S)-4-(4-methylphenyl)-2-oxo-N-[4-(1H-tetrazol-5-yl)phenyl]-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| (6S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| (6S)-4-(5-cyclopropylthiophen-2-yl)-3-(2,5-dihydro-1H-tetrazol-5-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| (6S)-4-[4-(difluoromethyl)phenyl]-6-[2-fluoro-4-[(6,6,6-trifluorohexyl)oxy]phenyl]-N-(methanesulfonyl)-2-oxo-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 1-[5-[(4-methoxyanilino)sulfanyl]-2-methylphenyl]-3-phenoxypropan-2-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-(cyclobutylsulfanyl)-3-phenyl-6-[([5-[4-(trifluoromethyl)phenoxy]pentyl]amino)acetyl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1H-inden-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Mus musculus | |
| 2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Mus musculus | |
| 3-(2,5-dihydro-1H-tetrazol-5-yl)-4-(5-ethylthiophen-2-yl)-6-[4-[(6,6,6-trifluorohexyl)oxy]-2-(trifluoromethyl)phenyl]pyridin-2(1H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Mus musculus | |
| 3-phenyl-2-[[(pyridin-3-yl)methyl]sulfanyl]-6-[5-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-benzimidazol-2-yl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 7-(4,6-di-tert-butylpyrimidin-2-yl)-3-[4-(trifluoromethoxy)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| 9-chloro-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| ethyl 3-[4-([3-[2-(cyclohexylsulfanyl)-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carbonyl]azetidin-1-yl]methyl)phenyl]propanoate | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-(2,4-dichlorophenyl)-2-[[(4-methoxyphenyl)methyl]amino]-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carboxamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-(4-chloro-2,6-difluorophenyl)-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]pyrimidin-2-yl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-[(1R)-1-(4-[[(2S)-2-(4-fluorophenyl)morpholin-4-yl]methyl]phenyl)ethyl]methanesulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-[(1S)-1-[4-[(4-tert-butylpiperidin-1-yl)methyl]phenyl]-2,2,2-trifluoroethyl]methanesulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-[(1S)-1-[4-[([[(3S)-2,3-dihydro[1,4]dioxino[2,3-b]pyridin-3-yl]methyl]amino)methyl]phenyl]2,2,2-trifluoroethyl]methanesulfonamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydro-1H-indol-7-yl]acetamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
| N-[[(6'S)-5-(2-hydroxypropan-2-yl)-2'-oxo-6'-[4-(4,4,4-trifluorobutoxy)phenyl]-6'-(trifluoromethyl)-1',2',5',6'-tetrahydro[2,4'-bipyridin]-3'-yl]methyl]-2-(methanesulfonyl)acetamide | MGAT2 inhibitor for the treatment of metabolic diseases and nonalcoholic steatohepatitis | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q3SYC2 | - |
- |
| Mus musculus | Q80W94 | - |
- |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Mgat2 | - |
Homo sapiens |
| Mgat2 | - |
Mus musculus |
| MOGAT2 | - |
Homo sapiens |
| MOGAT2 | - |
Mus musculus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0000002 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (6S)-4-(5-cyclopropylthiophen-2-yl)-3-(2,5-dihydro-1H-tetrazol-5-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one | |
| 0.0000003 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-(2,5-dihydro-1H-tetrazol-5-yl)-4-(5-ethylthiophen-2-yl)-6-[4-[(6,6,6-trifluorohexyl)oxy]-2-(trifluoromethyl)phenyl]pyridin-2(1H)-one | |
| 0.00000038 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1H-inden-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | |
| 0.00000064 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(cyclobutylsulfanyl)-3-phenyl-6-[([5-[4-(trifluoromethyl)phenoxy]pentyl]amino)acetyl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | |
| 0.00000073 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[[(6'S)-5-(2-hydroxypropan-2-yl)-2'-oxo-6'-[4-(4,4,4-trifluorobutoxy)phenyl]-6'-(trifluoromethyl)-1',2',5',6'-tetrahydro[2,4'-bipyridin]-3'-yl]methyl]-2-(methanesulfonyl)acetamide | |
| 0.000001 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (1S)-4'-(2-cyclopropyl-3H-pyrrol-4-yl)-5'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-5-(4,4,4-trifluorobutoxy)-2,3-dihydro-1'H-spiro[indene-1,2'-pyridin]-6'(3'H)-one | |
| 0.000001 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (6S)-4-[4-(difluoromethyl)phenyl]-6-[2-fluoro-4-[(6,6,6-trifluorohexyl)oxy]phenyl]-N-(methanesulfonyl)-2-oxo-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide | |
| 0.000001 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[5-[(2,4-difluorophenyl)sulfamoyl]-1-(2-phenylethyl)-2,3-dihydro-1H-indol-7-yl]acetamide | |
| 0.0000011 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-(cyclobutylsulfanyl)-6-(3-[[(2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amino]propanoyl)-3-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | |
| 0.0000016 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-[(1R)-1-(3,5-difluorophenyl)ethyl]-N-[3-(pyrrolidine-1-carbonyl)-1,2,4-oxadiazol-5-yl]-1,2,3,4-tetrahydroisoquinoline-7-sulfonamide | |
| 0.000002 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (6S)-4-(5-cyclopropyl-1,3-thiazol-2-yl)-6-[2-fluoro-4-(4,4,4-trifluorobutoxy)phenyl]-3-(5-oxo-4,5-dihydro-1H-tetrazol-1-yl)-6-(trifluoromethyl)-5,6-dihydropyridin-2(1H)-one | |
| 0.0000034 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 5-[(2,4-difluorophenyl)sulfamoyl]-7-(2-oxopyrrolidin-1-yl)-N-[4-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-1-carboxamide | |
| 0.0000038 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[(1S)-1-[4-[([[(3S)-2,3-dihydro[1,4]dioxino[2,3-b]pyridin-3-yl]methyl]amino)methyl]phenyl]2,2,2-trifluoroethyl]methanesulfonamide | |
| 0.000004 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | |
| 0.000004 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | ethyl 3-[4-([3-[2-(cyclohexylsulfanyl)-4-oxo-3-phenyl-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidine-6(4H)-carbonyl]azetidin-1-yl]methyl)phenyl]propanoate | |
| 0.0000063 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | |
| 0.000007 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | (6S)-4-(4-methylphenyl)-2-oxo-N-[4-(1H-tetrazol-5-yl)phenyl]-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1,2,5,6-tetrahydropyridine-3-carboxamide | |
| 0.0000078 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(4-chloro-2,6-difluorophenyl)-1-[5-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]pyrimidin-2-yl]-7-(2-oxopyrrolidin-1-yl)-2,3-dihydro-1H-indole-5-sulfonamide | |
| 0.000009 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 9-chloro-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | |
| 0.000019 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 7-(4,6-di-tert-butylpyrimidin-2-yl)-3-[4-(trifluoromethoxy)phenyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine | |
| 0.000028 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-[2-(4-tert-butylphenyl)ethyl]-N-[4-(3-cyclopentylpropyl)-2-fluorophenyl]-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | |
| 0.00005 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | (3R)-N-(2,4-difluorophenyl)-3-ethyl-3-methyl-2,5-dioxo-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | |
| 0.000056 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-phenyl-2-[[(pyridin-3-yl)methyl]sulfanyl]-6-[5-(trifluoromethyl)-3a,4,5,6,7,7a-hexahydro-1H-benzimidazol-2-yl]-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one | |
| 0.000058 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[(1S)-1-[4-[(4-tert-butylpiperidin-1-yl)methyl]phenyl]-2,2,2-trifluoroethyl]methanesulfonamide | |
| 0.00013 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 1-[5-[(4-methoxyanilino)sulfanyl]-2-methylphenyl]-3-phenoxypropan-2-one | |
| 0.000274 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-[(1R)-1-(4-[[(2S)-2-(4-fluorophenyl)morpholin-4-yl]methyl]phenyl)ethyl]methanesulfonamide | |
| 0.000398 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | |
| 0.00117 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | |
| 0.001522 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 2-[2-(4-tert-butylphenyl)ethyl]-N-(4-fluorophenyl)-1,2,3,4-tetrahydroisoquinoline-6-sulfonamide | |
| 0.002511 | - |
pH not specified in the publication, temperature not specified in the publication | Mus musculus | 3-ethyl-3-methyl-2,5-dioxo-N-phenyl-2,3,4,5-tetrahydro-1H-1,4-benzodiazepine-7-sulfonamide | |
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