Cloned (Comment) | Organism |
---|---|
expression of membrane-bound and soluble form, in HEK-293 cell | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
soluble enzyme form, in complex with inhibitor shows chelation of the active site magnesium | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
5-(cyclopentylsulfonyl)-7-fluoroquinolin-8-ol | compound displays good pharmacokinetics in rats. pIC50 value 8.7 for membrane-bound form, 5.6 for soluble form | Homo sapiens | |
7-chloro-5-((4-fluorophenyl)sulfonyl)quinolin-8-ol | compound exhibits very low clearance and long half-life in rat pharmacokinetics studies. pIC50 value 6.7 for membrane-bound form, below 5 for soluble form | Homo sapiens | |
7-chloro-5-(cyclopentylsulfonyl)quinolin-8-ol | compound exhibits very low clearance and long half-life in rat pharmacokinetics studies. pIC50 value 7.7 for membrane-bound form, below 5 for soluble form | Homo sapiens | |
7-chloro-5-(pyrrolidin-1-ylsulfonyl)quinolin-8-ol | compound exhibits very low clearance and long half-life in rat pharmacokinetics studies . pIC50 value 8.0 for membrane-bound form, 5.5 for soluble form | Homo sapiens | |
7-fluoro-5-(pyrrolidin-1-ylsulfonyl)quinolin-8-ol | compound displays good pharmacokinetics in rats. pIC50 value 8.4 for membrane-bound form, 5.8 for soluble form | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P21964 | - |
- |