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Literature summary for 1.14.11.29 extracted from

  • Chong, M.; Toh, L.; Tumber, A.; Chan, Y.; Chan, M.; Abboud, M.; Schofield, C.; Yeoh, K.
    Evaluation of 3-carbamoylpropanoic acid analogs as inhibitors of human hypoxia-inducible factor (HIF) prolyl hydroxylase domain enzymes (2021), Med. Chem. Res., 30, 977-986 .
No PubMed abstract available

Cloned(Commentary)

Cloned (Comment) Organism
expression of catalytic domain, residues 181-426 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-[(1,3-benzoxazol-2-yl)carbamoyl]propanoic acid
-
Homo sapiens
3-[(5-chloro-1,3-benzoxazol-2-yl)carbamoyl]propanoic acid
-
Homo sapiens
FG-4592 i.e. roxadustat Homo sapiens
additional information compounds with a 3-carbamoylpropanoic acids-containing benzoxazole moiety are inhibitors of PHD-2. However, neither the acids nor their respective ethyl esters upregulate HIF-1alpha levels in cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9GZT9
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00132
-
pH 7.8, temperature not specified in the publication Homo sapiens 3-[(5-chloro-1,3-benzoxazol-2-yl)carbamoyl]propanoic acid
0.00221
-
pH 7.8, temperature not specified in the publication Homo sapiens FG-4592
0.00224
-
pH 7.8, temperature not specified in the publication Homo sapiens 3-[(1,3-benzoxazol-2-yl)carbamoyl]propanoic acid