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Literature summary for 1.1.1.146 extracted from

  • Xia, G.; Liu, L.; Xue, M.; Liu, H.; Yu, J.; Li, P.; Chen, Q.; Xiong, B.; Liu, X.; Shen, J.
    Discovery of novel sulfonamides as potent and selective inhibitors against human and mouse 11beta-hydroxysteroid dehydrogenase type 1 (2012), Mol. Cell. Endocrinol., 358, 46-52.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
-
Homo sapiens
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
-
Mus musculus
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
-
Homo sapiens
1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide 71% and 62% inhibition of enzyme in adipose and liver tissue at 1 h after administration, short-acting compound displaying a significant drop in potency in the subsequent 3 h Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens P28845
-
-
Mus musculus P50172
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000003
-
pH 7.4, 37°C Homo sapiens 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide
0.0000004
-
pH 7.4, 37°C Homo sapiens 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
0.000018
-
pH 7.4, 37°C Mus musculus 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-isopinocampheyl]piperidine-3-carboxamide
0.000123
-
pH 7.4, 37°C Mus musculus 1-[(3-chloro-2-methylcyclohexyl)sulfonyl]-N-[(+)-bornyl]piperidine-3-carboxamide