General Information of the Protein
Protein ID
PT01786
Protein Name
Ectonucleotide pyrophosphatase/phosphodiesterase family member 2
Secondarily
Protein Name
Autotaxin
Extracellular lysophospholipase D
Gene Name
ENPP2
Secondarily
Gene Name
ATX
PDNP2
Sequence
MARRSSFQSCQIISLFTFAVGVNICLGFTAHRIKRAEGWEEGPPTVLSDSPWTNISGSCKGRCFELQEAGPPDCRCDNLCKSYTSCCHDFDELCLKTARGWECTKDRCGEVRNEENACHCSEDCLARGDCCTNYQVVCKGESHWVDDDCEEIKAAECPAGFVRPPLIIFSVDGFRASYMKKGSKVMPNIEKLRSCGTHSPYMRPVYPTKTFPNLYTLATGLYPESHGIVGNSMYDPVFDATFHLRGREKFNHRWWGGQPLWITATKQGVKAGTFFWSVVIPHERRILTILQWLTLPDHERPSVYAFYSEQPDFSGHKYGPFGPEMTNPLREIDKIVGQLMDGLKQLKLHRCVNVIFVGDHGMEDVTCDRTEFLSNYLTNVDDITLVPGTLGRIRSKFSNNAKYDPKAIIANLTCKKPDQHFKPYLKQHLPKRLHYANNRRIEDIHLLVERRWHVARKPLDVYKKPSGKCFFQGDHGFDNKVNSMQTVFVGYGSTFKYKTKVPPFENIELYNVMCDLLGLKPAPNNGTHGSLNHLLRTNTFRPTMPEEVTRPNYPGIMYLQSDFDLGCTCDDKVEPKNKLDELNKRLHTKGSTEERHLLYGRPAVLYRTRYDILYHTDFESGYSEIFLMPLWTSYTVSKQAEVSSVPDHLTSCVRPDVRVSPSFSQNCLAYKNDKQMSYGFLFPPYLSSSPEAKYDAFLVTNMVPMYPAFKRVWNYFQRVLVKKYASERNGVNVISGPIFDYDYDGLHDTEDKIKQYVEGSSIPVPTHYYSIITSCLDFTQPADKCDGPLSVSSFILPHRPDNEESCNSSEDESKWVEELMKMHTARVRDIEHLTSLDFFRKTSRSYPEILTLKTYLHTYESEI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Hydrolyzes lysophospholipids to produce the signaling molecule lysophosphatidic acid (LPA) in extracellular fluids (PubMed:15769751, PubMed:26371182, PubMed:27754931, PubMed:14500380, PubMed:12354767). Major substrate is lysophosphatidylcholine (PubMed:12176993, PubMed:27754931, PubMed:14500380). Can also act on sphingosylphosphorylcholine producing sphingosine-1-phosphate, a modulator of cell motility (PubMed:14500380). Can hydrolyze, in vitro, bis-pNPP, to some extent pNP-TMP, and barely ATP (PubMed:15769751, PubMed:12176993). Involved in several motility-related processes such as angiogenesis and neurite outgrowth. Acts as an angiogenic factor by stimulating migration of smooth muscle cells and microtubule formation (PubMed:11559573). Stimulates migration of melanoma cells, probably via a pertussis toxin-sensitive G protein (PubMed:1733949). May have a role in induction of parturition (PubMed:12176993). Possible involvement in cell proliferation and adipose tissue development (Probable). Tumor cell motility-stimulating factor (PubMed:1733949, PubMed:11559573). Required for LPA production in activated platelets, cleaves the sn-1 lysophospholipids to generate sn-1 lysophosphatidic acids containing predominantly 18:2 and 20:4 fatty acids (PubMed:21393252). Shows a preference for the sn-1 to the sn-2 isomer of 1-O-alkyl-sn-glycero-3-phosphocholine (lyso-PAF) (PubMed:21393252).
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Uniprot ID
Primary ID:
Q13822

Secondarily ID:
A8UHA1
E9PHP7
Q13827
Q14555
Q15117
Q9UCQ8
Q9UCR0
Q9UCR1
Q9UCR2
Q9UCR3
Q9UCR4
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Ensembl ID
ENSG00000136960
HGNC ID
HGNC:3357
Subcellular Location
Secreted
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: CL000098 , A2058
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0082479
 Compound Info 
2,4-dichloro-5-morpholin-4-ylsulfonyl-N-(3,4,5-trifluorophenyl)benzenecarbothioamide
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C17H13Cl2F3N2O3S2
  1
1
IC50 = 403 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0526186
 Compound Info 
2,4-dichloro-N-(3,4-difluorophenyl)-5-morpholin-4-ylsulfonylbenzamide
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C17H14Cl2F2N2O4S
  1
1
IC50 = 528 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0248462
 Compound Info 
2,4-dichloro-N-(4-chloro-3,5-difluorophenyl)-5-morpholin-4-ylsulfonylbenzamide
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C17H13Cl3F2N2O4S
  1
1
IC50 = 740.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0260174
 Compound Info 
2,4-dichloro-5-morpholin-4-ylsulfonyl-N-(3,4,5-trifluorophenyl)benzamide
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C17H13Cl2F3N2O4S
  1
1
IC50 = 1478 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000088 , Flp-In-293
 Cell Line Info 
Cell Line ID: CL000742 , FreeStyle 293-F
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000065 , HEK293-EBNA
 Cell Line Info 
Cell Line ID: CL000111 , MDA-MB-231
 Cell Line Info 
Cell Line ID: CL000112 , MDA-MB-435
 Cell Line Info 
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0181524
 Compound Info 
2-[[2-ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]-methylamino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile
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C30H33FN8O2S
  10
1 IC50 = 0.01 nM
2 IC50 = 1.3 nM
3 IC50 = 2.9 nM
4 IC50 = 3.1 nM
5 IC50 = 3.9 nM
6 IC50 = 100 nM
7 IC50 = 131 nM
8 IC50 = 242 nM
9 IC50 > 100 nM
10 Ki = 15 nM
CP0089180
 Compound Info 
N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[3-[[4-(trifluoromethoxy)phenyl]methyl]imidazo[4,5-b]pyridin-2-yl]propanamide
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C25H22ClF3N4O2
  1
1 IC50 = 1 nM
CP0224657
 Compound Info 
(3,5-dichlorophenyl)methyl 4-[3-oxo-3-(2-oxo-3H-1,3-benzoxazol-6-yl)propyl]piperazine-1-carboxylate
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C22H21Cl2N3O5
  6
1 IC50 = 1.1 nM
2 IC50 = 2.7 nM
3 IC50 = 2.8 nM
4 IC50 = 3 nM
5 IC50 = 3.7 nM
6 IC50 = 101 nM
CP0410967
 Compound Info 
[4-[[1-[(3,5-dichlorophenyl)methoxycarbonyl]piperidine-4-carbonyl]amino]phenyl]methylphosphonic acid
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C21H23Cl2N2O6P
  3
1 IC50 = 1.23 nM
2 IC50 = 2.18 nM
3 IC50 = 136 nM
CP0123400
 Compound Info 
US9409895, 17
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C19H23Cl2N5O3
  3
1 IC50 = 2 nM
2 IC50 = 3.1 nM
3 IC50 = 9 nM
CP0160898
 Compound Info 
3-(6-chloro-2-methyl-1-phenylindol-3-yl)sulfanylbenzoic acid
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C22H16ClNO2S
  1
1 IC50 = 5 nM
CP0169882
 Compound Info 
6-[6-chloro-2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]sulfanylpyridine-2-carboxylic acid
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C19H15ClN4O2S
  1
1 IC50 = 22 nM
CP0181525
 Compound Info 
2,4-dichloro-N-(3-fluorophenyl)-5-morpholin-4-ylsulfonylbenzamide
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C17H15Cl2FN2O4S
  2
1 IC50 = 31.4 nM
2 IC50 = 116 nM
CP0516045
 Compound Info 
3-[[6-chloro-2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]methyl]benzoic acid
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C21H18ClN3O2
  1
1 IC50 = 33 nM
CP0320335
 Compound Info 
6-[6-methoxy-2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]sulfanylpyridine-2-carboxylic acid
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C20H18N4O3S
  1
1 IC50 = 75 nM
CP0196587
 Compound Info 
6-[2,6-dimethyl-1-(1-methylpyrazol-4-yl)indol-3-yl]sulfanylpyridine-2-carboxylic acid
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C20H18N4O2S
  1
1 IC50 = 85 nM
CP0181435
 Compound Info 
6-[[6-chloro-2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]methyl]pyridine-2-carboxylic acid
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C20H17ClN4O2
  1
1 IC50 = 89 nM
CP0324028
 Compound Info 
3-(6-chloro-1,2-dimethylindol-3-yl)sulfanylbenzoic acid
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C17H14ClNO2S
  2
1 IC50 = 100 nM
2 IC50 > 1000 nM
CP0160900
 Compound Info 
3-[6-chloro-2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]oxybenzoic acid
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C20H16ClN3O3
  1
1 IC50 = 204 nM
CP0169877
 Compound Info 
3-[(6-chloro-2-methyl-1H-indol-3-yl)sulfanyl]benzoic acid
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C16H12ClNO2S
  1
1 IC50 = 290 nM
CP0160899
 Compound Info 
6-[(6-chloro-2-methyl-1H-indol-3-yl)sulfanyl]pyridine-2-carboxylic acid
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C15H11ClN2O2S
  1
1 IC50 = 604 nM
CP0169880
 Compound Info 
6-[6-fluoro-2-methyl-1-(1-methylpyrazol-3-yl)indol-3-yl]sulfanylpyridine-2-carboxylic acid
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C19H15FN4O2S
  1
1 IC50 = 816 nM
CP0181431
 Compound Info 
6-(6-chloro-1-cyclopentyl-2-methylindol-3-yl)sulfanylpyridine-2-carboxylic acid
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C20H19ClN2O2S
  1
1 IC50 = 2000 nM
CP0181433
 Compound Info 
6-[2-methyl-1-(1-methylpyrazol-4-yl)indol-3-yl]sulfanylpyridine-2-carboxylic acid
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C19H16N4O2S
  1
1 IC50 = 5700 nM
CP0160896
 Compound Info 
6-(6-chloro-1,2-dimethylindol-3-yl)sulfanylpyridine-2-carboxylic acid
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C16H13ClN2O2S
  1
1 IC50 > 4000 nM
CP0324027
 Compound Info 
3-(6-chloro-1-cyclopentyl-2-methylindol-3-yl)sulfanylbenzoic acid
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C21H20ClNO2S
  1
1 IC50 > 4000 nM
CP0169883
 Compound Info 
3-(2-methyl-1-phenylindol-3-yl)sulfanylbenzoic acid
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C22H17NO2S
  1
1 IC50 > 30000 nM
CP0304384
 Compound Info 
[(2R,3S)-3-(hexadecanoylamino)-2-hydroxy-4-[4-[(4-methoxy-3,5-dimethylpyridin-2-yl)methoxy]phenyl]butyl]phosphonic acid
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C35H57N2O7P
  1
1 Ki = 1000 nM
CP0227783
 Compound Info 
2-(4-((3,5-dichlorophenyl)carbamothioyl)piperazin-1-yl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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C21H20Cl2N6O3S
  2
1 Ki = 1900 nM
2 Ki = 6500 nM
CP0281260
 Compound Info 
2-(4-((9H-xanthene-9-carbonyl)carbamothioyl)piperazin-1-yl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic acid
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C29H26N6O5S
  2
1 Ki = 2700 nM
2 Ki = 19800 nM
CP0265597
 Compound Info 
4,4'-(5,5'-carbonylbis(1,3-dioxoisoindoline-5,2-diyl))bis(methylene)dibenzoic acid
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C33H20N2O9
  1
1 Ki = 5000 nM
CP0301794
 Compound Info 
4-(4-(2-(naphthalen-1-yl)-1,3-dioxoisoindoline-5-carbonyl)phenoxy)benzoic acid
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C32H19NO6
  2
1 Ki = 5800 nM
2 Ki = 32300 nM
CP0281261
 Compound Info 
4-(2-(3-ethyl-4-oxo-3,4,6,7,8,9-hexahydropyrimido[4,5-b]quinolin-2-ylthio)acetamido)benzoic acid
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C22H22N4O4S
  2
1 Ki = 6500 nM
2 Ki = 9300 nM
CP0265598
 Compound Info 
3-(1,3-dioxo-2-(4-(phenyldiazenyl)phenyl)isoindoline-5-carboxamido)benzoic acid
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C28H18N4O5
  2
1 Ki = 15100 nM
2 Ki = 40300 nM
CP0162606
 Compound Info 
(3S)-1-bromo-3-hydroxy-4-(stearoyloxy)butylphosphonic acid
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C22H44BrO6P
  1
1 Ki = 40100 nM
Clinical Information about the Protein
Target 1 ( Extracellular lysophospholipase D (E-NPP2) )
Target Type Clinical trial Target
Disease 4 Target-related Diseases  4
1 Idiopathic pulmonary fibrosis [ICD-11: CB03.4]
2 Inflammation [ICD-11: 1A00-CA43.1]
3 Fibrosis [ICD-11: GA14-GC01]
4 Pain [ICD-11: MG30-MG3Z]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Cudetaxestat
 Drug Info 
Phase 2
Idiopathic pulmonary fibrosis
Patented Agent(s) 3 Patented Agents  3
1 Complex heterocyclic compound 1
 Drug Info 
Patented
Inflammation
2 Pyridine and pyrimidine derivative 1
 Drug Info 
Patented
Fibrosis
3 Pyrido/pyrrolo-fused pyrimidine derivative 1
 Drug Info 
Patented
Pain