General Information of the Protein
Protein ID
PT03114
Protein Name
Sphingosine-1-phosphate lyase 1
Secondarily
Protein Name
Sphingosine-1-phosphate aldolase
Gene Name
SGPL1
Secondarily
Gene Name
KIAA1252
Sequence
MPSTDLLMLKAFEPYLEILEVYSTKAKNYVNGHCTKYEPWQLIAWSVVWTLLIVWGYEFVFQPESLWSRFKKKCFKLTRKMPIIGRKIQDKLNKTKDDISKNMSFLKVDKEYVKALPSQGLSSSAVLEKLKEYSSMDAFWQEGRASGTVYSGEEKLTELLVKAYGDFAWSNPLHPDIFPGLRKIEAEIVRIACSLFNGGPDSCGCVTSGGTESILMACKAYRDLAFEKGIKTPEIVAPQSAHAAFNKAASYFGMKIVRVPLTKMMEVDVRAMRRAISRNTAMLVCSTPQFPHGVIDPVPEVAKLAVKYKIPLHVDACLGGFLIVFMEKAGYPLEHPFDFRVKGVTSISADTHKYGYAPKGSSLVLYSDKKYRNYQFFVDTDWQGGIYASPTIAGSRPGGISAACWAALMHFGENGYVEATKQIIKTARFLKSELENIKGIFVFGNPQLSVIALGSRDFDIYRLSNLMTAKGWNLNQLQFPPSIHFCITLLHARKRVAIQFLKDIRESVTQIMKNPKAKTTGMGAIYGMAQTTVDRNMVAELSSVFLDSLYSTDTVTQGSQMNGSPKPH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Lyase
Function
Cleaves phosphorylated sphingoid bases (PSBs), such as sphingosine-1-phosphate, into fatty aldehydes and phosphoethanolamine. Elevates stress-induced ceramide production and apoptosis (PubMed:11018465, PubMed:14570870, PubMed:24809814, PubMed:28165339). Required for global lipid homeostasis in liver and cholesterol homeostasis in fibroblasts. Involved in the regulation of pro-inflammatory response and neutrophil trafficking. Modulates neuronal autophagy via phosphoethanolamine production which regulates accumulation of aggregate-prone proteins such as APP (By similarity). Seems to play a role in establishing neuronal contact sites and axonal maintenance (By similarity).
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Uniprot ID
Primary ID:
O95470

Secondarily ID:
B2RBD4
Q7Z732
Q9ULG8
Q9UN89
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Ensembl ID
ENSG00000166224
HGNC ID
HGNC:10817
Subcellular Location
Endoplasmic reticulum membrane
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: CL000198 , HEK293-H
Compound ID Compound Name Compound Formula
CP0259082
N-[2-[(4-butoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C26H33N3O3
 1
1
IC50 = 230 nM
   TI
   LI
   LO
   TS
CP0096034
N-[2-[[2,5-dimethyl-4-(2,2,2-trifluoroethoxy)phenyl]methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C24H26F3N3O3
 1
1
IC50 = 240 nM
   TI
   LI
   LO
   TS
CP0204724
N-[2-[(4-ethoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C24H29N3O3
 1
1
IC50 = 930 nM
   TI
   LI
   LO
   TS
CP0391152
N-[(1S)-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H27N3O3
 1
1
IC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0112585
N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H27N3O3
 1
1
IC50 = 1800 nM
   TI
   LI
   LO
   TS
CP0250713
N-[2-[[4-methoxy-2-methyl-5-(trifluoromethyl)phenyl]methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H24F3N3O3
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0391151
N-[1-[4-(3-hydroxyprop-1-ynyl)phenyl]-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C26H29N3O4
 1
1
IC50 = 3700 nM
   TI
   LI
   LO
   TS
CP0259083
N-[1-[4-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C27H34N4O4
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0409630
5-cyclopropyl-N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
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C25H29N3O3
 1
1
IC50 = 5500 nM
   TI
   LI
   LO
   TS
CP0140507
N-[1-(4-fluorophenyl)-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H26FN3O3
 1
1
IC50 = 7200 nM
   TI
   LI
   LO
   TS
CP0140508
N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-pyridin-4-ylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C22H26N4O3
 1
1
IC50 = 25000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0096086
1-benzyl-4-[(3R)-4-(5-cyanopyridin-2-yl)-3-methylpiperazin-1-yl]phthalazine-6-carbonitrile
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C27H23N7
 1
1 IC50 = 93.5 nM
CP0259082
N-[2-[(4-butoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C26H33N3O3
 1
1 IC50 = 117 nM
CP0259083
N-[1-[4-(4-amino-4-oxobutyl)phenyl]-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C27H34N4O4
 1
1 IC50 = 150 nM
CP0391151
N-[1-[4-(3-hydroxyprop-1-ynyl)phenyl]-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C26H29N3O4
 1
1 IC50 = 150 nM
CP0204724
N-[2-[(4-ethoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C24H29N3O3
 1
1 IC50 = 260 nM
CP0391152
N-[(1S)-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H27N3O3
 1
1 IC50 = 485 nM
CP0096034
N-[2-[[2,5-dimethyl-4-(2,2,2-trifluoroethoxy)phenyl]methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C24H26F3N3O3
 1
1 IC50 = 590 nM
CP0140507
N-[1-(4-fluorophenyl)-2-[(4-methoxy-2,5-dimethylphenyl)methylamino]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H26FN3O3
 1
1 IC50 = 720 nM
CP0409630
5-cyclopropyl-N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-1,2-oxazole-3-carboxamide
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C25H29N3O3
 1
1 IC50 = 730 nM
CP0140508
N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-pyridin-4-ylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C22H26N4O3
 1
1 IC50 = 850 nM
CP0112585
N-[2-[(4-methoxy-2,5-dimethylphenyl)methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H27N3O3
 1
1 IC50 = 1000 nM
CP0250713
N-[2-[[4-methoxy-2-methyl-5-(trifluoromethyl)phenyl]methylamino]-1-phenylethyl]-5-methyl-1,2-oxazole-3-carboxamide
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C23H24F3N3O3
 1
1 IC50 = 1200 nM
CP0084726
2-(4-octylphenethyl)-2-aminopropane-1,3-diol
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C19H33NO2
 1
1 IC50 = 52000 nM
Clinical Information about the Protein
Target 1 ( Sphingosine-1-phosphate lyase 1 (SGPL1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Rheumatoid arthritis [ICD-11: FA20]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 LX2931 Phase 2
Rheumatoid arthritis