General Information of the Protein
Protein ID
PT04078
Protein Name
Acyl-CoA (8-3)-desaturase
Secondarily
Protein Name
Delta(5) fatty acid desaturase
Fatty acid desaturase 1
Gene Name
FADS1
Secondarily
Gene Name
FADSD5
Sequence
MAPDPVAAETAAQGPTPRYFTWDEVAQRSGCEERWLVIDRKVYNISEFTRRHPGGSRVISHYAGQDATDPFVAFHINKGLVKKYMNSLLIGELSPEQPSFEPTKNKELTDEFRELRATVERMGLMKANHVFFLLYLLHILLLDGAAWLTLWVFGTSFLPFLLCAVLLSAVQAQAGWLQHDFGHLSVFSTSKWNHLLHHFVIGHLKGAPASWWNHMHFQHHAKPNCFRKDPDINMHPFFFALGKILSVELGKQKKKYMPYNHQHKYFFLIGPPALLPLYFQWYIFYFVIQRKKWVDLAWMITFYVRFFLTYVPLLGLKAFLGLFFIVRFLESNWFVWVTQMNHIPMHIDHDRNMDWVSTQLQATCNVHKSAFNDWFSGHLNFQIEHHLFPTMPRHNYHKVAPLVQSLCAKHGIEYQSKPLLSAFADIIHSLKESGQLWLDAYLHQ
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Acts as a front-end fatty acyl-coenzyme A (CoA) desaturase that introduces a cis double bond at carbon 5 located between a preexisting double bond and the carboxyl end of the fatty acyl chain. Involved in biosynthesis of highly unsaturated fatty acids (HUFA) from the essential polyunsaturated fatty acids (PUFA) linoleic acid (LA) (18:2n-6) and alpha-linolenic acid (ALA) (18:3n-3) precursors. Specifically, desaturates dihomo-gamma-linoleoate (DGLA) (20:3n-6) and eicosatetraenoate (ETA) (20:4n-3) to generate arachidonate (AA) (20:4n-6) and eicosapentaenoate (EPA) (20:5n-3), respectively (PubMed:10601301, PubMed:10769175). As a rate limiting enzyme for DGLA (20:3n-6) and AA (20:4n-6)-derived eicosanoid biosynthesis, controls the metabolism of inflammatory lipids like prostaglandin E2, critical for efficient acute inflammatory response and maintenance of epithelium homeostasis. Contributes to membrane phospholipid biosynthesis by providing AA (20:4n-6) as a major acyl chain esterified into phospholipids. In particular, regulates phosphatidylinositol-4,5-bisphosphate levels, modulating inflammatory cytokine production in T-cells (By similarity). Also desaturates (11E)-octadecenoate (trans-vaccenoate)(18:1n-9), a metabolite in the biohydrogenation pathway of LA (18:2n-6) (By similarity).
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Uniprot ID
Primary ID:
O60427

Secondarily ID:
A8K0I7
B2RAI0
Q53GM5
Q8N3A6
Q8NCC7
Q8NCG0
Q96I39
Q96SV3
Q96T10
Q9NRP8
Q9NYX1
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Ensembl ID
ENSG00000149485
HGNC ID
HGNC:3574
Subcellular Location
Endoplasmic reticulum membrane
Mitochondrion
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000063 , Hep-G2
Compound ID Compound Name Compound Formula
CP0457853
3-chloro-5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzonitrile
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C17H12ClFN2O2
 1
1
IC50 = 0.52 nM
   TI
   LI
   LO
   TS
CP0184306
5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzene-1,3-dicarbonitrile
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C18H12FN3O2
 1
1
IC50 = 1.5 nM
   TI
   LI
   LO
   TS
CP0508436
3-fluoro-5-[(4S,5S)-5-(4-fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzonitrile
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C17H12F2N2O2
 1
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0547069
5-(4-fluorophenyl)-3-(3-methoxyphenyl)-1,3-oxazolidin-2-one
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C16H14FNO3
 1
1
IC50 = 4.1 nM
   TI
   LI
   LO
   TS
CP0457857
3-(2,5-dimethoxyphenyl)-5-(4-fluorophenyl)-1,3-oxazolidin-2-one
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C17H16FNO4
 1
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
CP0565125
3-(3-chlorophenyl)-5-(4-fluorophenyl)-1,3-oxazolidin-2-one
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C15H11ClFNO2
 1
1
IC50 = 55 nM
   TI
   LI
   LO
   TS
CP0548769
3-[(5S)-5-(4-fluorophenyl)-2-oxo-1,3-oxazolidin-3-yl]benzonitrile
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C16H11FN2O2
 1
1
IC50 = 60 nM
   TI
   LI
   LO
   TS
CP0547070
3-[(2,4-dichlorophenyl)methyl]-5-(4-fluorophenyl)-1,3-oxazolidin-2-one
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C16H12Cl2FNO2
 1
1
IC50 = 150 nM
   TI
   LI
   LO
   TS
CP0520916
3-[5-(4-fluorophenyl)-2-oxo-1,3-oxazolidin-3-yl]benzonitrile
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C16H11FN2O2
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0538803
3-(3-fluorophenyl)-5-(4-fluorophenyl)-1,3-oxazolidin-2-one
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C15H11F2NO2
 1
1
IC50 = 170 nM
   TI
   LI
   LO
   TS
CP0520917
5-(4-fluorophenyl)-3-phenyl-1,3-oxazolidin-2-one
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C15H12FNO2
 1
1
IC50 = 190 nM
   TI
   LI
   LO
   TS
CP0557814
3-[(2,4-dichloro-5-hydroxyphenyl)methyl]-5-phenyl-1,3-oxazolidin-2-one
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C16H13Cl2NO3
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0200792
2-[5-[3-[3-(2-bromo-5-fluorophenoxy)propoxy]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
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C15H13BrFN5O5
 1
1
IC50 > 20000 nM
   TI
   LI
   LO
   TS
CP0096178
2-[5-[3-[2-(2-chloro-5-fluorophenyl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-1,2-oxazol-5-yl]tetrazol-2-yl]acetic acid
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C18H17ClFN7O3
 1
1
IC50 > 80000 nM
   TI
   LI
   LO
   TS
CP0382800
5-methyl-3-(2-(4-(2-(trifluoromethyl)phenoxy)piperidin-1-yl)thiazol-5-yl)-1,2,4-oxadiazole
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C18H17F3N4O2S
 1
1
IC50 > 2000 nM
   TI
   LI
   LO
   TS