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Regulatory Requirements >>
Discovery/IND-Enabling Definitive/NDA-Enabling
DESIGN
System Compatibility None Comprehensive
Assay Rigor Basic Advanced
ASSESSMENTS
Substrate Single
Concentration
Multiple Concentrations Inhibitor
Challenge, Km/Vmax
Inhibition Single
Concentration
Multiple Concentrations, IC50
Cell Line Substrate Inhibitor
MDR1 Digoxin , Etoposide, Fexofenadine, Amprenavir, Talinolol, Loperamide Valspodar, Cyclosporin A, Vinblastin, Ketoconazole, Loperamide
BCRP Cladribine, Topotecan, Prazosin, Cimetidine, Sulfasalazine, Mitoxantrone, Actinomycin D, Doxorubicin, Estrone-3-Sulfate, Etoposide, Irinotecen, Rosuvastatin, Daunorubicin, SN-38, Fexofenadine Ko143, Elacridar, FTC
OCT1 MPP+, Amantadine, Amiloride, Metformin, Pindolol, Procainamide, Propanolol, Ranitidine Repaglinide, Disopyramide, Quinine, Quinidine, Cimetidine, Rosiglitazone, Triethylamine, Metformin
OCT2 MPP+, Pindolol, Ranitidine, Procainamide, Amiloride, Amantadine Imipramine, TPA, Verapamil, Quinidine, Cimetidine, Metformin, Dopamine, Triethylamine
OAT1 PAH, Adefovir, Cidofovir, Furosemide, Lamivudine, Tenofovir, Zidovudine Probenecid, Bumetanide, Novobiocin, Quinaprilat, TEA, Methotrexate, Lamivudine
OAT3 Furosemide, Bumetanide, Cefaclor, Quinaprilat Probenecid, Bumetanide, Novobiocin, Quinaprilat, Rosuvastatin, Naproxen
OATP1B1 Atorvastatin, Rosuvastatin, Pitavastatin Rifamycin SV, Atenolol, Cyclosporin A, Digoxin, Estrone-3-Sulfate, Estradiol-17β Glucuronide, Ketoconazole, Propranolol, Rifampicin, Ritonavir, Rosuvastatin, Taurocholic Acid, Tolbutamide, Verapamil
OATP1B3 Atorvastatin, Pitavastatin, Rosuvastatin Rifamycin SV, Rifampicin, Rosuvastatin, Taurocholic Acid, Ritonavir, Cyclosporin A, Estradiol-17β Glucuronide, Estrone-3-Sulfate, Atenolol, Propranolol, Digoxin
Mate1 Metformin, MPP+, Cimetidine, Amiloride Cimetidine, Atenolol, Triethylamine, Amantadine, Imipramine, Disopyramide, MPP+, Verapamil, Quinidine, Ritonavir
Mate2K Metformin, MPP+, Cimetidine, Amiloride Pyrimethamine, Ondansetron, Quinidine
MRP2 CDCF MK571
BSEP [3H] Taurocholic acid Cyclosporin A, Troglitazone
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