| Physicochemical properties | |
Solubility (kinetic, thermodynamic) |
|
Chemical stability (Buffer, Biorelevant media) |
|
Thermodynamic solubility |
| Permeability | |
PAMPA assay |
|
Caco-2 cells permeability |
| Protein binding | |
Plasma (Equilibrium dialysis, Ultrafiltration) |
|
Albumin, Alpha-glycoprotein (Equilibrium dialysis, Ultrafiltration) |
|
Microsomal binding |
| Metabolism study | |
Plasma stability |
|
Microsomal stability |
|
S9 stability |
|
Hepatocyte stability |
|
Metabolite profiling and Met ID (in vitro) |
|
Metabolite profiling and Met ID (in vivo) |
|
Reactive metabolite formation (GSH trapping) |
|
CYP Phenotyping (CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4/5) |
|
UGT Phenotyping (UGT1A1, 1A3, 1A4, 1A6, 1A9, 2B7, 2B15) |
|
Phenotyping_metabolite formation |
|
Non-CYP (FMO, CES, NAT, SULT 외) |
| Transport study | |
ABC transport phenotyping (efflux transporters) |
|
SLC transport phenotyping (uptake transporters) |
|
Peptide based uptake transport phenotyping (PEPT1/2, SMVT) |
|
SLC transport phenotyping in Xenopus oocytes (OATPs, OATs, OCTs, MATEs) |
|
Cryopreserved hepatocytes uptake |
|
Hepatic excretion by Sandwich cultured hepatocytes |
| Enzyme Inhibition | |
CYP Inhibition (Screening, IC50 assay) |
|
CYP inhibition (Ki assay) |
|
UGT Inhibition (Screening, IC50 assay) |
|
UGT inhibition (Ki assay) |
|
Time-Dependent Inhibition (IC50 shift assay) |
|
Time-Dependent Inhibition (Ki and Kinact) |
| Transporter Inhibition | |
ABC transporter inhibition (efflux transporters_accumulation) |
|
ABC transporter inhibition (efflux transporters_bi-direction) |
|
SLC transporter inhibition (uptake transporters) |
|
Time-dependent inhibition of OATP, IC50 shift assay |
| Enzyme/Transporter Induction | |
Cell viability |
|
Transporter (CYPs, UGTs, Transporters) Induction |
|
Enzyme activity in human hepatocytes |
|
Enzyme Induction (EC50 assay) |
| BCS-Biowaiver | |
Solubility |
|
Chemical stability |
|
Caco-2 cell permeability |
| Bioanalytical service | |
Method development |
|
Method validation |
|
Sample analysis |
|
PK analysis |
| - | |
Radiolabeled clinical ADME studies (Mass balance, Metabolite profiling & Identification) |
