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Literature summary extracted from

  • Hoeglund, A.B.; Howard, A.L.; Wanjala, I.W.; Pham, T.C.; Parrill, A.L.; Baker, D.L.
    Characterization of non-lipid autotaxin inhibitors (2010), Bioorg. Med. Chem., 18, 769-776.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.39 2,2'-methylenebis(4-chlorophenol)
-
 Homo sapiens
3.1.4.39 bithionol
-
 Homo sapiens
3.1.4.39 eosin Y
-
 Homo sapiens
3.1.4.39 H2L 5210574 mixed-mode inhibition against ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 H2L 5564949 mixed-mode inhibition against ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 H2L 5761473 competitive ATX inhibitor Homo sapiens
3.1.4.39 H2L 7839888 mixed-mode inhibition against ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 H2L 7905958 competitive inhibition with respect to ATX-mediated FS-3 hydrolysis and non-competitive inhibition with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis Homo sapiens
3.1.4.39 H2L 7921385 non-competitive inhibitor Homo sapiens
3.1.4.39 Hexachlorophene
-
 Homo sapiens
3.1.4.39 L-histidine
-
 Homo sapiens
3.1.4.39 lysophosphatidic acid efficacious inhibitor of ATX activity Homo sapiens
3.1.4.39 merbromin
-
 Homo sapiens
3.1.4.39 NSC10881
-
 Homo sapiens
3.1.4.39 NSC13792
-
 Homo sapiens
3.1.4.39 NSC48300
-
 Homo sapiens
3.1.4.39 NSC60016
-
 Homo sapiens
3.1.4.39 NSC78785
-
 Homo sapiens
3.1.4.39 NSC86629
-
 Homo sapiens
3.1.4.39 RJC 03297
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.1.4.39 0.0037
-
 FS-3
-
 Homo sapiens
3.1.4.39 5.6
-
 4-nitrophenyl-TMP
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.39 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.39 4-nitrophenyl-TMP + H2O
-
 Homo sapiens ?
-
 ?
3.1.4.39 FS-3 + H2O fluorogenic lysoPLD substrate Homo sapiens 2-(6-hydroxy-3-oxo-9a,10a-dihydro-3H-xanthen-9-yl)-5-[(18-hydroxy-15-oxo-3,6,9,12-tetraoxa-16-azaoctadec-1-yl)carbamoyl]benzoic acid + (2R)-2-hydroxy-3-(phosphonooxy)propyl 6-[(4-[(E)-[4-(dimethylamino)phenyl]diazenyl]benzoyl)amino]hexanoate
-
 ?
3.1.4.39 lysophosphatidylcholine + H2O
-
 Homo sapiens lysophosphatidic acid + choline
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.39 ATX
-
 Homo sapiens
3.1.4.39 autotaxin
-
 Homo sapiens
3.1.4.39 NPP2
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.4.39 0.0019
-
 H2L 7905958 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 0.002
-
 H2L 5761473 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 0.0027
-
 H2L 7839888 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 0.0065
-
 H2L 7905958 with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis Homo sapiens
3.1.4.39 0.0093
-
 H2L 7921385 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens
3.1.4.39 0.0151
-
 H2L 5564949 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.39 0.0012
-
 with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis Homo sapiens H2L 7905958
3.1.4.39 0.0015
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 7839888
3.1.4.39 0.0016
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 7905958
3.1.4.39 0.0016
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 7921385
3.1.4.39 0.0017
-
 with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis Homo sapiens H2L 7839888
3.1.4.39 0.0068
-
 with respect to ATX-mediated 4-nitrophenyl-TMP hydrolysis Homo sapiens H2L 5210574
3.1.4.39 0.0068
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 5210574
3.1.4.39 0.0128
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 5761473
3.1.4.39 0.0128
-
 with respect to ATX-mediated FS-3 hydrolysis Homo sapiens H2L 5564949