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Literature summary for 2.3.1.180 extracted from

  • Yang, Y.S.; Zhang, F.; Gao, C.; Zhang, Y.B.; Wang, X.L.; Tang, J.F.; Sun, J.; Gong, H.B.; Zhu, H.L.
    Discovery and modification of sulfur-containing heterocyclic pyrazoline derivatives as potential novel class of beta-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors (2012), Bioorg. Med. Chem. Lett., 22, 4619-4624.
    View publication on PubMed
Search for more literature for 2.3.1.180

Cloned(Commentary)

Cloned (Comment) Organism
overexpressed in Escherichia coli DH10B cells using the pET30 vector, selenomethionine-substituted protein expressed in Escherichia coli BL21(DE3) Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
2-[3-(4-bromophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(4-methoxyphenyl)-1,3-thiazole
-
 Escherichia coli
2-[3-(4-bromophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli
2-[3-(4-bromophenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
-
 Escherichia coli
2-[3-(4-bromophenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli
2-[3-(4-fluorophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
-
 Escherichia coli
2-[3-(4-fluorophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli
2-[3-(4-methoxyphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
-
 Escherichia coli
2-[3-(4-methoxyphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli
2-[3-(4-methylphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
-
 Escherichia coli
2-[3-(4-methylphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli
2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
-
 Escherichia coli
2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(4-methoxyphenyl)-1,3-thiazole
-
 Escherichia coli
2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
-
 Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
-
-

Purification (Commentary)

Purification (Comment) Organism
to homogeneity in three chromatographic steps (Q-Sepharose, MonoQ, and hydroxyapatite), immobilized metal ion affinity chromatography (Ni2+) Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
malonyl-ACP + acetyl-CoA
-
 Escherichia coli CO2 + CoA + acetoacetyl-ACP
-
 ?

Synonyms

Synonyms Comment Organism
beta-ketoacyl-acyl carrier protein synthase III
-
 Escherichia coli
FabH
-
 Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0046
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0084
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-fluorophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
0.0097
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-bromophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0109
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-methylphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0136
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-methylphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
0.0157
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(4-methoxyphenyl)-1,3-thiazole
0.0184
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
0.0197
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-bromophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-(4-methoxyphenyl)-1,3-thiazole
0.0223
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-fluorophenyl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0233
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-bromophenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0271
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-bromophenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one
0.0306
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-methoxyphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-4-phenyl-1,3-thiazole
0.0899
-
 pH 7.0, temperature not specified in the publication Escherichia coli 2-[3-(4-methoxyphenyl)-5-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one