IndraLab

Statements

KCNH2 inhibits cytochrome P450. 5 / 5
| 1 4
sparser
"Results demonstrated weak hERG inhibition (50.1% inhibition at 25 μM) and marginal inhibition of CYP enzymes at 10 μM ()."
27115835
sparser
"The number of carbocyclic aromatic rings is correlated with lower solubility, higher logD, higher plasma protein binding, hERG inhibition and inhibition of some major cytochrome P450s (3A4, 2C9, 2C19). (3) For compounds required to reach the CNS, there are additional criteria."
23931634
sparser
"Compound 24 demonstrated overall favorable in vitro safety profiles with respect to CYP isoform and hERG inhibition."
28618224
sparser
"Several heterocycles as well as different amido substituents were screened for their antiviral activity, oral bioavailability, and low propensity towards hERG ion channel inhibition and interaction with a range of CYP enzymes."
| PMC
reach
"In this review we discuss the utility of protein-structure-based design and docking approaches aimed at overcoming issues related to plasma protein binding, active transport via P-glycoprotein, hERG channel mediated cardiotoxicity and cytochrome P450 inhibition, metabolism and induction."
21554979