Biochemical assays |
|
 |
VDR-SRC2-3 interaction |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| VDR-SRC2 interaction |
Fluorescence |
|
Pull-down assay (ROX-antibody) |
| VDR-ligand interaction |
Fluorescence Polarization |
384 |
Invitrogen Polarscreen |
| VDR-Coregulator interaction (10 coactivators and corepressors) |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| |
|
|
|
|
 |
TR alpha-SRC2-2 interaction |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| TR beta-SRC2-2 interaction |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| AR-SRC2-3 interaction |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| PPAR gamma-DRIP2 interaction |
Fluorescence Polarization |
384 |
Alexa Fluor 647/Texas Red/Fluorescein |
| ER alpha-SRC2-3 interaction |
Fluorescence Polarization |
384 |
in the making |
| ER beta-SRC2-3 interaction |
Fluorescence Polarization |
384 |
in the making |
| RxR alpha-SRC2-3 interaction |
Fluorescence Polarization |
384 |
in the making |
| |
|
|
|
|
 |
GLO1 inhibition |
UV Detection |
384 |
|
| GLO1 inhibition |
Fluorescence Intensity |
384 |
|
| GLO1 inhibition |
UV Detection |
384 |
Kinetic assay |
| |
|
|
|
|
| |
|
|
|
|
In vitro preclinical assays |
|
 |
Aqueous small molecule solubility |
UV/VIS |
384 |
Filter-based Assay (pH range) |
| Permeability(PAMPA) |
UV/VIS |
96 |
Hexadecane method (pH range) |
| Stability assay |
LCMS |
384 |
Single injection (pH range) |
| logP (octanol/water) |
UV/VIS |
384 |
|
| |
|
|
|
|
 |
Heptatoxicity assay |
Luminescence |
384 |
HepG2/CellTiterGlo (Promega) |
| Nephrotoxicity assay |
Luminescence |
384 |
HEK293/CellTiterGlo |
| Cardiotoxicity assay |
Luminescence |
384 |
Cardiomyocytes/CellTiterGlo |
| Neurotoxicity |
Luminescence |
384 |
Glial/CellTiterGlo |
| Cardiotoxicity (hERG) |
automated patch clamp |
96 |
transfected HEK293T |
| |
|
|
|
|
 |
Livermicrosome metabolism |
LCMS |
96 |
stability |
| Hepatocyte metabolism |
LCMS |
96 |
stability |
| P450 metabolism |
LCMS/Luminescence |
96 |
metabolites |
| Enzyme conjugation |
LCMS/Luminescence |
96 |
metabolites |
| |
|
|
|
|
 |
Plasma Protein Binding assay |
Fluorescence |
384 |
multiple fluorophores |
| Plasma Protein Binding assay |
UV Detection |
384 |
filtration-based |
| |
|
|
|
|
| |
|
|
|
|
Cell-based assays |
|
|
VDR-coregulator recruitment |
Fluorescence resonance energy transfer (FRET) |
384 |
GeneBLAzer assay (Invitrogen) |
| Gene-specific VDR-coregulator recruitment |
Luminescence |
384 |
24-hydroxylase promoter transcription assay |
| VDR-coactivator interaction |
Luminescence |
384 |
VDR-SRC1 two-hybrid assay |
| HL60 differentiation assay |
UV Detection |
384 |
|
| |
|
|
|
|
| |
rt-PCR |
Fluorescence |
96 |
A mix of 20 NR target gene primers and 10 cell lines |
| |
|
|
|
|
|
AR-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| ER alpha-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| ER beta-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| PPAR alpha-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| PPAR gamma-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| PPAR delta-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| PxR-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| CAR-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| |
RxR alpha-activated transcription |
Luminescence |
384 |
Agonist and Antagonist |
| |
|
|
|
|
 |
GABA(A) receptor assay (a1b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| GABA(A) receptor assay (a2b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| GABA(A) receptor assay (a3b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| GABA(A) receptor assay (a4b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| GABA(A) receptor assay (a5b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| GABA(A) receptor assay (a6b3y2) |
automated patch clamp |
96 |
Electrophysiology |
| |
|
|
|
|
