Biomedical Engineering Reference
In-Depth Information
TABLE 18.2
(
Continued
)
Structure
Name
Activity
Assay
Ref.
C
-cyclopropylalkylamide
analog
Human pregnane X
receptor (hPXR)
agonist; EC
50
=
400 nM
Cell-based Gal-hPXR
assay with a luciferase
reporter
35
Lactam carboxamide
analog
Transcription factor
HOXA13 inhibitor;
IC
50
=
Fluorescence
polarization assay
detecting disruption of
transcription
factor-DNA complex
36
6.5
M
Tricyclic pyrrole
carboxamide PSI2106
Mitogen-activated
protein kinase
phosphatase 1 (MKP-1)
inhibitor; IC
50
=
8.0
M
In vitro assay using the
artificial substrate
3-
O
-methylfluorescein
phosphate
37
