Transporter Assay Catalog Single Transporter Models Single Transporter Models Subcellular Transporter Relevance Gene Transporter Assay Species2 Cell Model3 Probe Substrate Inhibition 1 Localization in Type Type Assay Model Positive Control ASBT Bile acid uptake SLC10A2 Uptake IA H Apical MDCK-II Taurocholate NaCDC asc-1 Amino acid transport SLC7A10 Uptake IA H Basolateral MDCK-II Glycine Serine ASCT2 Amino acid transport SLC1A5 Uptake IA H Apical MDCK-II Glutamine Alanine ATB0+ Amino acid transport SLC6A14 Uptake IA H Apical MDCK-II Leucine N-Ethylmaleimide BAT1, CSNU3 Amino acid transport SLC7A9 Uptake IA H Apical MDCK-II Proline BCRP FDA & EMA DDI guidances; intestinal and BBB efflux, ABCG2 Efflux BD H Apical Caco-2 clone3 Genistein Chrysin biliary secretion, renal tubular secretion and drug resistance VA H, R N/A Vesicle CCK-8 Bromosulfophthalein BD H Apical MDCK-II Prazosin KO143 BSEP EMA DDI guidance; biliary secretion of bile salts, drug ABCB11 Efflux VA H, R, D N/A Vesicle Taurocholate Rifampicin induced liver injury CAT1 Amino acid transport SLC7A1 Uptake IA H Basolateral MDCK-II Arginine Lysine CAT2B Amino acid transport SLC7A2 Uptake IA H Basolateral MDCK-II Arginine CAT3 Amino acid transport SLC7A3 Uptake IA H Basolateral MDCK-II Arginine Lysine CHT Choline transport SLC5A7 Uptake IA H Basolateral MDCK-II Choline CNT1 Nucleoside uptake SLC28A1 Uptake IA H, R Apical MDCK-II Uridine Adenosine CNT2 Nucleoside uptake SLC28A2 Uptake IA H, R Apical MDCK-II Uridine Adenosine CNT3 Nucleoside uptake SLC28A3 Uptake IA H, R Apical MDCK-II Uridine Adenosine 3-Guanidinopropionic CRT Creatine transport SLC6A8 Uptake IA H Basolateral MDCK-II Creatine acid DAT Neurotransmission; validated therapeutic target SLC6A3 Uptake IA H Apical MDCK-II Dopamine Venlafaxine EAAT1 Neurotransmission SLC1A3 Uptake IA H Basolateral MDCK-II Glutamic acid Cysteic acid EAAT2 Neurotransmission SLC1A2 Uptake IA H Basolateral MDCK-II Glutamic acid Cysteic acid EAAT3 Neurotransmission SLC1A1 Uptake IA H Apical MDCK-II Glutamic acid Way-213613 ENT1 Nucleoside transport SCL29A1 Uptake IA H Apical (and MDCK-II Adenosine NBMPR Basolateral) ENT2 Nucleoside transport SLC29A2 Uptake IA H, R Basolateral MDCK-II Hypoxanthine Adenosine ENT4 / PMAT Nucleoside transport and extrasynaptic reuptake SLC29A4 Uptake IA H Basolateral MDCK-II Metformin or MPP+ Decynium-22 GAT1 Neurotransmission; validated therapeutic target SLC6A1 Uptake IA H Apical MDCK-II GABA Nipecotic acid GAT2 Neurotransmission SLC6A13 Uptake IA H Basolateral MDCK-II GABA Nipecotic acid GAT3 Neurotransmission SLC6A11 Uptake IA H Apical MDCK-II GABA Nipecotic acid GLYT1 Neurotransmission SLC6A9 Uptake IA H Basolateral MDCK-II Glycine Sarcosine GLYT2 Neurotransmission SLC6A5 Uptake IA H Basolateral MDCK-II Glycine Org25543 LAT1 Amino acid transport SLC7A5 Uptake IA H Basolateral MDCK-II Leucine JPH203 MATE1 Biliary secretion and renal tubular secretion SLC47A1 Efflux IA H, R Apical MDCK-II Metformin Cimetidine MATE2-K Renal tubular secretion SLC47A2 Efflux IA H Apical MDCK-II Metformin Cimetidine MCT1 Lactate and ketone body transport SLC16A1 Uptake IA H Apical MDCK-II 2-Thiophene-glyoxylic acid Phloretin MRP1 Drug resistance ABCC1 Efflux VA H N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone MRP2 Biliary secretion, renal tubular secretion, drug resistance ABCC2 Efflux VA H, M, R, D N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone Bile acid transport, bilirubin glucuronide transport MRP3 ABCC3 Efflux VA H N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone MRP4 Renal tubular secretion; hepatic efflux; ABCC4 Efflux VA H N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone drug resistance NET Neurotransmission; validated therapeutic target SLC6A2 Uptake IA H Basolateral MDCK-II Dopamine Desipramine NTCP Hepatic bile salt uptake SLC10A1 Uptake IA H Basolateral MDCK-II Taurocholate NaCDC OAT1 FDA & EMA guidances; renal uptake SLC22A6 Uptake IA H Basolateral MDCK-II p-Aminohippurate Probenecid OAT2 Hepatic uptake; renal uptake SLC22A7 Uptake IA H Basolateral MDCK-II cGMP Indomethacin Estrone-3-sulfate or OAT3 FDA & EMA guidances; renal uptake SLC22A8 Uptake IA H, M Basolateral MDCK-II p-Aminohippurate Probenecid OAT4 Renal tubular reabsorption SLC22A11 Uptake IA H Apical MDCK-II Estrone-3-sulfate Indomethacin OATP1A2 Intestinal absorption; BBB penetration SLCO1A2 Uptake IA H Apical MDCK-II Estrone-3-sulfate Bromosulfophthalein OATP1B1 FDA & EMA DDI guidances; hepatic uptake SLCO1B1 Uptake IA H Basolateral MDCK-II, CHO3 Estradiol-17-ß-D-glucuronide Rifampicin OATP1B3 FDA & EMA DDI guidances; hepatic uptake SLCO1B3 Uptake IA H Basolateral MDCK-II, CHO3 Cholecystokinin-8 (CCK-8) Rifampicin OATP2B1 Hepatic uptake; intestinal uptake SLCO2B1 Uptake IA H N/A CHO3 Estrone-3-sulfate Bromosulfophthalein OCT1 EMA guidance; hepatic uptake SLC22A1 Uptake IA H, R Basolateral MDCK-II Metformin or MPP+ Quinidine OCT2BioIFDVA T& EM.cA guidances;om renal uptake SLC22A2 Uptake IA H, M, R, C Basolateral MDCK-II Metformin Quinidine OCT3 Renal uptake; extrasynaptic reuptake SLC22A3 Uptake IA H, R Basolateral MDCK-II Metformin or MPP+ Quinidine NET Neurotransmission; validated therapeutic target SLC6A2 Uptake IA H Basolateral MDCK-II Dopamine Desipramine NTCP Hepatic bile salt uptake SLC10A1 Uptake IA H Basolateral MDCK-II Taurocholate NaCDC OAT1 FDA & EMA guidances; renal uptake SLC22A6 Uptake IA H Basolateral MDCK-II p-Aminohippurate Probenecid OAT2 Hepatic uptake; renal uptake SLC22A7 Uptake IA H Basolateral MDCK-II cGMP Indomethacin Single Transporter Models OAT3 FDA & EMA guidances; renal uptake SLC22A8 Uptake IA H, M SubcellularBasolateral MDCK-II Estrone-3-sulfate or Probenecid Transporter Relevance Gene Transporter Assay Species2 Cell Model3 Probep-Aminohippurate Substrate Inhibition 1 Localization in OAT4 Renal tubular reabsorption SLC22A11 TUptakeype TIAype H AssayApical Model MDCK-II Estrone-3-sulfate PositiveIndomethacin Control ASBTOATP1A2 BileIntestinal acid uptakeabsorption; BBB penetration SLC10A2SLCO1A2 Uptake IA H Apical MDCK-II TEstrone-3-sulfateaurocholate NaCDCBromosulfophthalein asc-1OATP1B1 AminoFDA & acidEMA transport DDI guidances; hepatic uptake SLC7A10SLCO1B1 Uptake IA H Basolateral MDCK-IIMDCK-II, CHO 3 GlycineEstradiol-17-ß-D-glucuronide SerineRifampicin ASCT2OATP1B3 AminoFDA & acidEMA transport DDI guidances; hepatic uptake SLC1A5SLCO1B3 Uptake IA H ApicalBasolateral MDCK-IIMDCK-II, CHO 3 GlutamineCholecystokinin-8 (CCK-8) AlanineRifampicin AOTB0+ATP2B1 AminoHepatic acid uptake; transport intestinal uptake SLC6A14SLCO2B1 Uptake IA H ApicalN/A MDCK-IICHO3 LeucineEstrone-3-sulfate N-EthylmaleimideBromosulfophthalein BOCT1AT1, CSNU3 AminoEMA guidance; acid transport hepatic uptake SLC7A9SLC22A1 Uptake IA HH, R ApicalBasolateral MDCK-II ProlineMetformin or MPP+ Quinidine BCRPOCT2 FDA & EMA DDIguidances; guidances; renal intestinal uptake and BBB efflux, ABCG2SLC22A2 EUptakefflux BDIA HH, M, R, C ApicalBasolateral Caco-2MDCK-II clone3 GenisteinMetformin ChrysinQuinidine biliary secretion, renal tubular secretion and drug OCT3 resistanceRenal uptake; extrasynaptic reuptake SLC22A3 Uptake IA H, R Basolateral MDCK-II Metformin or MPP+ Quinidine OCTN1 Renal tubular reabsorption SLC22A4 Uptake VIAA H,H R N/AApical VMDCK-IIesicle CCK-8Ergothioneine BromosulfophthaleinVerapamil OCTN2 Renal tubular reabsorption, critical genetic polymorphism SLC22A5 Uptake BDIA H Apical MDCK-II PrazosinCarnitine KO143Verapamil SLC51A1 & BSEPOST -OST EMBileA acid DDI transport guidance; biliary secretion of bile salts, drug ABCBSLC 51A211 EUptakefflux VIAA H,H R, D N/ABasolateral VMDCK-IIesicle TTCAaurocholate Rifampicin induced liver injury CPAAT2T1 Amino acid transport SLC7A1SLC36A2 Uptake IA H BasolateralApical MDCK-II ArginineGlycine Lysine CPCFTAT2B AminoVitamin acid transport transport SLC7A2SLC46A1 Uptake IA H BasolateralApical MDCK-II ArginineMethotrexate Bromosulfophthalein CPEPT1AT3 AminoIntestinal acid uptake, transport prodrug strategy SLC7A3SLC15A1 Uptake IA H BasolateralApical MDCK-II ArginineGly-Sar LLosartanysine CHTPEPT2 CholineRenal tubular transport reabsorption SLC5A7SLC15A2 Uptake IA H BasolateralApical MDCK-II CholineGly-Sar Losartan FDA & EMA DDI guidances; intestinal and BBB efflux, ABCB1 BD, VA in MDCK-II, CNT1P-gp Nucleosidebiliary secretion, uptake renal tubular secretion, drug resistance SLC28A1(MDR1) UptakeEfflux IAvesicles H, R Apical (in cells) MDCK-IICaco-2, vesicles UridineDigoxin, quinidine AdenosineVerapamil, elacridar CNT2PROT NucleosideAmino acid uptaketransport SLC28A2SLC6A7 Uptake IA H,H R ApicalBasolateral MDCK-II UridineProline Adenosine CNT3RFC NucleosideFolate transport uptake SLC28A3SLC19A1 Uptake IA H,H R ApicalBasolateral MDCK-II UridineMethotrexate AdenosineBromosulfophthalein 3-Guanidinopropionic CRTSERT CreatineNeurotransmission; transport validated therapeutic target SLC6A8SCL6A4 Uptake IA H Basolateral MDCK-II CreatineSerotonin acidFluoxetine Glucose and galactose transport; validated therapeutic DSGATLT1 Neurotransmission;target validated therapeutic target SLC6A3SLC5A1 Uptake IA H Apical MDCK-II DopamineMethyl- -D-glucopyranoside VPhlorizinenlafaxine EASGALT2T1 NeurotransmissionGlucose transport; validated therapeutic target SLC1A3SLC5A2 Uptake IA H BasolateralApical MDCK-II GlutamicMethyl- -D-glucopyranoside acid CysteicPhlorizin acid Pantothenate (vitamin EASMVTAT2 NeurotransmissionVitamin transport SLC1A2SLC5A6 Uptake IA H BasolateralApical MDCK-II GlutamicBiotin (vitamin acid B7) CysteicB5) acid EASNAT3T1 NeurotransmissionAmino acid transport SLC1A1SLC38A1