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Literature summary for 3.1.3.1 extracted from

  • Ardecky, R.J.; Bobkova, E.V.; Kiffer-Moreira, T.; Brown, B.; Ganji, S.; Zou, J.; Pass, I.; Narisawa, S.; Iano, F.G.; Rosenstein, C.; Cheltsov, A.; Rascon, J.; Hedrick, M.; Gasior, C.; Forster, A.; Shi, S.; Dahl, R.; Vasile, S.; Su, Y.; Sergienko, E.; Chung, T.D.; Kaunitz, J.; Hoylaerts, M.F.; Pinkerton, A.B.
    Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes (2014), Bioorg. Med. Chem. Lett., 24, 1000-1004.
    View publication on PubMedView publication on EuropePMC
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Inhibitors

Inhibitors Comment Organism Structure
2-([(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)sulfonyl]amino)-N-(2,5-dimethylphenyl)acetamide potent inhibitor with good selectivity against both placental and tissue-nonspecific alkaline phosphatase, competitive inhibition. A dose of 10 microM completley inhibits the enzyme expressed by transfected COS-1 cells Mus musculus
N-(3-cyanophenyl)-3-([(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)sulfonyl]amino)propanamide potent inhibitor with good selectivity against both placental and tissue-nonspecific alkaline phosphatase Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus P24822
-
-

Source Tissue

Source Tissue Comment Organism Textmining
duodenum
-
 Mus musculus
-

Synonyms

Synonyms Comment Organism
IAP
-
 Mus musculus
intestinal-type alkaline phosphatase
-
 Mus musculus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0032
-
 2-([(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)sulfonyl]amino)-N-(2,5-dimethylphenyl)acetamide pH not specified in the publication, temperature not specified in the publication Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00054
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus 2-([(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)sulfonyl]amino)-N-(2,5-dimethylphenyl)acetamide
0.00182
-
 pH not specified in the publication, temperature not specified in the publication Mus musculus N-(3-cyanophenyl)-3-([(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)sulfonyl]amino)propanamide