Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(10Z)-hexadecenoic acid | - |
Homo sapiens | |
(5Z,8Z,11Z,14Z)-eicosatetraenoic acid | - |
Homo sapiens | |
(6Z,9Z,12Z)-octadecatrienoic acid | - |
Homo sapiens | |
(9Z)-octadecenoic acid | - |
Homo sapiens | |
(9Z)-tetradecenoic acid | - |
Homo sapiens | |
(9Z,12Z)-octadecadienoic acid | - |
Homo sapiens | |
11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid | - |
Homo sapiens | |
14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid | - |
Homo sapiens | |
15-deoxy-DELTA12,14-prostaglandin J2 | - |
Homo sapiens | |
22(R)-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
24(S),25-epoxycholesterol | inhibits only CES1, not CES2 | Homo sapiens | |
24(S)-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
25-hydroxycholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
27-Hydroxycholesterol | partially noncompetitive inhibitor of recombinant CES1, impaires intracellular CES1 activity following treatment of intact THP1 cells. No inhibition of CES2 | Homo sapiens | |
7-oxocholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
arachidonic acid | most potent fatty acid inhibitor of recombinant CES1 acting by a noncompetitive mechanism, overview. The inhibition is reversible by bovine serum albumin | Homo sapiens | |
benzil | inhibition of CES1 in THP-1 cells | Homo sapiens | |
bioresmethrin | a pyrethroid insecticide | Homo sapiens | |
cholesterol | slight inhibition of CES1, not CES2 | Homo sapiens | |
hexadecanoic acid | - |
Homo sapiens | |
additional information | unsaturated fatty acids are better inhibitors of CES1 activity than saturated fatty acids, CES2 activity is unaffected by any fatty acid | Homo sapiens | |
octadecanoic acid | - |
Homo sapiens | |
paraoxon | inhibition of CES1 in THP-1 cells | Homo sapiens | |
prostaglandin E2 | - |
Homo sapiens | |
prostaglandin F2alpha | - |
Homo sapiens | |
tetradecanoic acid | - |
Homo sapiens | |
trans-permethrin | a pyrethroid insecticide | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | xenobiotic substrates are pyrethroid insecticides | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isozymes CES1 and CES2 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | CES1 and CES2, S9 fraction, HL1220 and HL1274 | Homo sapiens | - |
macrophage | CES1, no expression of CES2 | Homo sapiens | - |
monocyte | CES1, no expression of CES2 | Homo sapiens | - |
THP-1 cell | CES1, no expression of CES2 | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
4-nitrophenyl valerate + H2O | - |
Homo sapiens | 4-nitrophenol + valerate | - |
? | |
additional information | xenobiotic substrates are pyrethroid insecticides | Homo sapiens | ? | - |
? |
Synonyms | Comment | Organism |
---|---|---|
carboxylesterase 1 | - |
Homo sapiens |
CES1 | - |
Homo sapiens |
CES2 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
0.00001 | - |
27-Hydroxycholesterol | pH 7.4, 37°C, recombinant CES1 | Homo sapiens | |
0.0018 | - |
arachidonic acid | pH 7.4, 37°C, recombinant CES1 | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.000033 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 27-Hydroxycholesterol | |
0.002 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (5Z,8Z,11Z,14Z)-eicosatetraenoic acid | |
0.007 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z)-octadecenoic acid | |
0.007 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (10Z)-hexadecenoic acid | |
0.0081 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 24(S),25-epoxycholesterol | |
0.009 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | tetradecanoic acid | |
0.009 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z,12Z)-octadecadienoic acid | |
0.012 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (9Z)-tetradecenoic acid | |
0.013 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 15-deoxy-DELTA12,14-prostaglandin J2 | |
0.019 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | (6Z,9Z,12Z)-octadecatrienoic acid | |
0.025 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | hexadecanoic acid | |
0.027 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 11,12-epoxy-(5Z,8Z,14Z)-eicosatrienoic acid | |
0.038 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | 14,15-epoxy-(5Z,8Z,11Z)-eicosatrienoic acid | |
0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | prostaglandin E2 | |
0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | prostaglandin F2alpha | |
0.1 | - |
pH 7.4, 37°C, recombinant CES1 | Homo sapiens | octadecanoic acid |