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Literature summary extracted from

  • Albers, H.M.; Dong, A.; van Meeteren, L.A.; Egan, D.A.; Sunkara, M.; van Tilburg, E.W.; Schuurman, K.; van Tellingen, O.; Morris, A.J.; Smyth, S.S.; Moolenaar, W.H.; Ovaa, H.
    Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation (2010), Proc. Natl. Acad. Sci. USA, 107, 7257-7262.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.39 (5Z)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
-
 Mus musculus
3.1.4.39 3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
-
 Mus musculus
3.1.4.39 3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-3-methoxyphenoxy)methyl]benzoic acid competitive inhibition, 35% residual ATX activity at 0.005 mM Mus musculus
3.1.4.39 3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid competitive inhibition, 7% residual ATX activity at 0.005 mM Mus musculus
3.1.4.39 [3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]phenyl]boronic acid mixed-type inhibition, complete inhibition at 0.005 mM Mus musculus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.39 0.094
-
 lysophosphatidylcholine
-
 Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.39 Mus musculus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.39 bis(4-nitrophenyl)phosphate + H2O
-
 Mus musculus ?
-
 ?
3.1.4.39 lysophosphatidylcholine + H2O
-
 Mus musculus lysophosphatidic acid + choline
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.39 ATX
-
 Mus musculus
3.1.4.39 ATX/lysoPLD
-
 Mus musculus
3.1.4.39 autotaxin
-
 Mus musculus
3.1.4.39 NPP2
-
 Mus musculus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.39 0.000028
-
 in Tris-HCl buffer (pH 7.4) at 37°C Mus musculus [3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]phenyl]boronic acid
3.1.4.39 0.00011
-
 in Tris-HCl buffer (pH 7.4) at 37°C Mus musculus (5Z)-3-benzyl-5-[(1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
3.1.4.39 0.000161
-
 in Tris-HCl buffer (pH 7.4) at 37°C Mus musculus 3-([4-[(Z)-(3-benzyl-2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]-3-ethoxyphenoxy]methyl)benzoic acid
3.1.4.39 0.0017
-
 in Tris-HCl buffer (pH 7.4) at 37°C Mus musculus 3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
3.1.4.39 0.0025
-
 in Tris-HCl buffer (pH 7.4) at 37°C Mus musculus 3-[(4-[(Z)-[3-(4-fluorobenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]-3-methoxyphenoxy)methyl]benzoic acid