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Literature summary for 3.4.21.37 extracted from

  • Weale, C.A.; Bernstein, P.R.; Bryant, C.; Ceccarelli, C.; Damewood, J.R.; Earlay, R.; Feeney, S.W.; Gomes, B.; Kosmider, B.J.; Steelman, G.B.; Thomas, R.M.; Vacek, E.P.; Williams, J.C.; Wolanin, D.J.; Woolson, S.
    Nonpeptidic inhibitors of human leukocyte elastase. 5. Design, synthesis, and X-ray crystallography of a series of orally active 5-aminopyrimidin-6-one-containing trifluoromethyl ketones (1995), J. Med. Chem., 38, 98-108.
    View publication on PubMed
Search for more literature for 3.4.21.37

Inhibitors

Inhibitors Comment Organism Structure
(2-(3,5-bis-trifluoromethyl-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-(4-amino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-(4-chloro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-(4-methoxy-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-(4-nitro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-cyclohexyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(2-isopropyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(6-oxo-2-(4-fluorophenyl)-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(6-oxo-2-phenyl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(6-oxo-2-pyridin-3-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(6-oxo-2-thiophen-2-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
(6-oxo-2-[4-(2,2,2-trifluoro-acetylamino)-phenyl]-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 2-(4-aminophenyl)-5-[(methylsulfonyl)amino]-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 2-(4-fluorophenyl)-5-(methylamino)-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 5-(ethylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 5-(formylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 5-amino-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 5-amino-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-2-(2-thienyl)-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
 Homo sapiens
1(6H)-Pyrimidineacetamide, 6-oxo-2-phenyl-5-[(trifluoroacetyl)amino]-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
2-(5-amino-6-oxo-2-thien-2-ylpyrimidin-1(6H)-yl)-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
2-[2-(4-fluorophenyl)-6-oxo-5-[(cyclohexylsulfamoyl)-amino]-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
2-[5-amino-2-(3,5-difluorophenyl)-6-oxopyrimidin-1(6H)-yl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
2-[5-amino-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide
-
 Homo sapiens
2-[5-[(benzyloxycarbonyl)amino]-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
5-aminopyridin-6-one-containing trifluoromethyl ketones
-
 Homo sapiens
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 1-methylethyl ester
-
 Homo sapiens
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
 Homo sapiens
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, methyl ester
-
 Homo sapiens
Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
 Homo sapiens
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-1-[2-[[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]amino]-2-oxoethyl]-6-oxo-5-pyrimidinyl]-, (3,5-dimethyl-4-pyridinyl)methyl ester
-
 Homo sapiens
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 2-pyridinylmethyl ester
-
 Homo sapiens
Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 4-pyridinylmethyl ester
-
 Homo sapiens
Carbamothioic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, S-methyl ester
-
 Homo sapiens
Carbamothioic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, S-methyl ester
-
 Homo sapiens
L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
 Homo sapiens
[6-Oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-2-(4-trifluoromethyl-phenyl)-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
leukocyte
-
 Homo sapiens
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000096
-
 Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-1-[2-[[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]amino]-2-oxoethyl]-6-oxo-5-pyrimidinyl]-, (3,5-dimethyl-4-pyridinyl)methyl ester
-
 Homo sapiens
0.0000016
-
 1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
 Homo sapiens
0.0000016
-
 L-Prolinamide, N-[(phenylmethoxy)carbonyl]-L-valyl-N-[(1S)-3,3-difluoro-1-(1-methylethyl)-2-oxo-4-[(phenylmethyl)amino]butyl]-
-
 Homo sapiens
0.0000016
-
 2-[2-(4-fluorophenyl)-6-oxo-5-[(cyclohexylsulfamoyl)-amino]-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide pH 7.4 Homo sapiens
0.0000036
-
 (2-(4-amino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.0000049
-
 1(6H)-Pyrimidineacetamide, 5-amino-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-2-(2-thienyl)-
-
 Homo sapiens
0.0000062
-
 2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide pH 7.4 Homo sapiens
0.0000066
-
 (6-oxo-2-phenyl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.0000077
-
 1(6H)-Pyrimidineacetamide, 5-[[(cyclohexylamino)sulfonyl]amino]-2-(4-fluorophenyl)-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]-6-oxo-
-
 Homo sapiens
0.0000081
-
 (2-(4-methoxy-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.0000082
-
 (6-oxo-2-(4-fluorophenyl)-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000009
-
 (2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000011
-
 2-[5-[(benzyloxycarbonyl)amino]-6-oxo-2-(2-thienyl)-1,6-dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide pH 7.4 Homo sapiens
0.000015
-
 1(6H)-Pyrimidineacetamide, 2-(4-aminophenyl)-5-[(methylsulfonyl)amino]-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
0.000016
-
 Carbamothioic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, S-methyl ester
-
 Homo sapiens
0.000017
-
 (2-(4-nitro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000018
-
 (2-(4-chloro-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000022
-
 Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 2-pyridinylmethyl ester
-
 Homo sapiens
0.000023
-
 Carbamothioic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, S-methyl ester
-
 Homo sapiens
0.000023
-
 Carbamic acid, [2-(4-fluorophenyl)-1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-5-pyrimidinyl]-, 4-pyridinylmethyl ester
-
 Homo sapiens
0.000026
-
 1(6H)-Pyrimidineacetamide, 5-(ethylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
0.000027
-
 Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 1-methylethyl ester
-
 Homo sapiens
0.000033
-
 (6-oxo-2-pyridin-3-yl-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.00004
-
 Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-phenyl-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
 Homo sapiens
0.000042
-
 [6-Oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-2-(4-trifluoromethyl-phenyl)-1,6-dihydro-pyrimidin-5-yl]-carbamic acid benzyl ester
-
 Homo sapiens
0.000042
-
 Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, methyl ester
-
 Homo sapiens
0.000043
-
 Carbamic acid, [1,6-dihydro-6-oxo-1-[2-oxo-2-[[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]amino]ethyl]-2-(2-thienyl)-5-pyrimidinyl]-, 2,2,2-trifluoroethyl ester
-
 Homo sapiens
0.000043
-
 (6-oxo-2-[4-(2,2,2-trifluoro-acetylamino)-phenyl]-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000046
-
 1(6H)-Pyrimidineacetamide, 2-(4-fluorophenyl)-5-(methylamino)-6-oxo-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
0.000052
-
 2-[5-amino-6-oxo-2-(4-fluorophenyl)-1,6-dihydro-1-pyrimidinyl]-N-[2-methyl-1-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)propyl]acetamide pH 7.4 Homo sapiens
0.000057
-
 (2-cyclohexyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000072
-
 (2-(3,5-bis-trifluoromethyl-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.000094
-
 1(6H)-Pyrimidineacetamide, 6-oxo-2-phenyl-5-[(trifluoroacetyl)amino]-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
0.0001
-
 1(6H)-Pyrimidineacetamide, 5-(formylamino)-6-oxo-2-(2-thienyl)-N-[3,3,3-trifluoro-1-(1-methylethyl)-2-oxopropyl]-
-
 Homo sapiens
0.000101
-
 (2-(4-formylamino-phenyl)-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.00017
-
 (2-isopropyl-6-oxo-1-[(3,3,3-trifluoro-1-isopropyl-2-oxo-propylcarbamoyl)-methyl]-1,6-dihydro-pyrimidin-5-yl)-carbamic acid benzyl ester
-
 Homo sapiens
0.00027
-
 2-[5-amino-2-(3,5-difluorophenyl)-6-oxopyrimidin-1(6H)-yl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens
0.00052
-
 2-(5-amino-6-oxo-2-thien-2-ylpyrimidin-1(6H)-yl)-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide
-
 Homo sapiens