Bioivt Transporter Catalog DG V3

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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 Uptake IA H ApicalBasolateral MDCK-II GlutamicMeAIB acid WAlanineay-213613

ENT1SNAT2 NucleosideAmino acid transport SCL29A1SLC38A2 Uptake IA H ApicalBasolateral (and MDCK-II AdenosineMeAIB NBMPRAlanine Basolateral) TAUT Neurotransmission, osmotic balance, muscle tonicity SLC6A6 Uptake IA H Basolateral MDCK-II GABA ß-Alanine ENT2 Nucleoside transport SLC29A2 Uptake IA H, R Basolateral MDCK-II Hypoxanthine Adenosine THTR1 Vitamin transport SLC19A2 Uptake IA H Basolateral MDCK-II Thiamine Amprolium ENT4 / PMAT Nucleoside transport and extrasynaptic reuptake SLC29A4 Uptake IA H Basolateral MDCK-II Metformin or MPP+ Decynium-22 THTR2 Vitamin transport SLC19A3 Uptake IA H Apical MDCK-II Thiamine Amprolium GAT1 Neurotransmission;Uric acid renal tubular validated reabsorption, therapeutic validated target SLC6A1 Uptake IA H Apical MDCK-II GABA Nipecotic acid URAT1 therapeutic target SLC22A12 Uptake IA H Apical MDCK-II Uric acid Benzbromarone GAT2 NeurotransmissionAmino acid transport, neurotransmission, anti-oxidative SLC6A13 Uptake IA H Basolateral MDCK-II GABA Nipecotic acid C=CynomolgusxCT (macaque)defense SLC7A11 Uptake IA H Basolateral MDCK-II Glutamic acid Sulfasalazine 3 AllG cellAT3 models haveNeurotransmission exactly matched control cells except Caco-2 clones and CHOSLC6A cells.11 Uptake IA H Apical MDCK-II GABA Nipecotic acid 1 Assay Type: IA=Intracellular Accumulation; VA=Vesicular Accumulation; BD=Bi-Directional NotesGLYT1 for multipleNeurotransmission transporter models: SLC6A9 Uptake IA H Basolateral MDCK-II Glycine Sarcosine 2 Species 1. In all multipleavailable: transporter H=Human, models, M=Mouse, each transporter R=Rat, is localizedD=Dog, to and the C=Cynomolgusappropriate membrane. (macaque) 3 G All 2.LYT2 Allcell control models cellsNeurotransmission have are exactly exactly matched matched to the control cells used cells in exceptthe assays. Caco-2 clonesSLC6A5 and CHOUptake cells. IA H Basolateral MDCK-II Glycine Org25543 3. All transporters are human, and all cells used are MDCK-II. Multiple Transporter Models LAT1 Amino acid transport SLC7A5 Uptake IA H Basolateral MDCK-II Leucine JPH203 Transporter Relevance Gene Transporter Type Probe Substrate Inhibition MATE1 Biliary secretion and renal tubular secretion SLC47A1 Efflux IA H, R Apical MDCK-II Metformin CimetidinePositive Multiple-Transporter Models Control Renal tubular secretion SLC47A2 Efflux IA H Apical MDCK-II Metformin Cimetidine MOAATE2-KT3 / BCRP Renal clearance of Methotrexate MultipleSLC22A8 Transporter / ABCG2 Models Uptake & efflux Methotrexate Probenecid Inhibition TMCT1ransporter Lactate and ketone body transportRelevance SLC16A1 UptakeGene IA H TransporterApical Type ProbeMDCK-II Substrate 2-Thiophene-glyoxylic acidPositivePhloretin OAT3 / MRP2 Renal clearance of organic anions SLC22A8 / ABCC2 Uptake & efflux p-Aminohippurate Control Probenecid MRP1 Drug resistance ABCC1 Efflux VA H N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone OAT3 / BCRP Renal clearance of Methotrexate SLC22A8 / ABCG2 Uptake & efflux Methotrexate Probenecid MRP2OCT2 / MATE1Biliary secretion, renal tubular secretion,Renal clearance drug resistance of organicABCC2 cations Efflux SLC22A2V /A SLC47A1 H, M, R, D N/A Uptake & eVffluxesicle MetforminEstradiol-17-ß-D-glucuronide BenzbromaroneCimetidine Renal Uptake & efflux OOCT2AT3 / MRP2/ MATE2-KBile acid transport, bilirubin RenalglucuronideRenal clearance clearance transport of organic of organic anions cations SLC22A8SLC22A2 / ABCC2 / SLC47A2 Uptake & p-Aminohippurateefflux Metformin Probenecid Cimetidine Transporter MRP3 ABCC3 Efflux VA H N/A Vesicle Estradiol-17-ß-D-glucuronide Benzbromarone Models Renal clearance of creatinine and organic SLC22A2 / SLC22A3 / SLC47A1 Uptake & efflux Creatinine Cimetidine MRP4OCT2OCT2 / M/ OCT3ATE1 Renal/ MATE1 tubular secretion; hepaticRenal e fclearanceflux; of organic cationsABCC4 ESLC22A2fflux / SLC47A1VA H UptakeN/A & efflux MetforminVesicle Estradiol-17-ß-D-glucuronideCimetidineBenzbromaroneRenal drug resistance cations Renal OCT2OCT2 / M/ MATE2-KATE1 / MATE2K RenalRenal clearance clearance of organic of organic cations cations SLC22A2SLC22A2 / SLC47A2 / SLC47A1 / SLC47A2Uptake & eUptakefflux & Metforminefflux Metformin Cimetidine CimetidineTransporterransporter Renal clearance of creatinine and organic Creatinine Models OCT2 / OCT3 / MATE1 SLC22A2 / SLC22A3 / SLC47A1 Uptake & efflux Creatinine Cimetidine Models OCT2 / OAT2 / OCT3 / MATE1 / MATE2KcationsRenal clearance of creatinine SLC22A2 / SLC22A7 / SLC22A3 / Uptake & efflux Creatinine Cimetidine SLC47A1 / SLC47A2 Metformin OCT2 / MATE1 / MATE2-K Renal clearance of organic cations SLC22A2 / SLC47A1 / SLC47A2 Uptake & efflux Cimetidine OATP1A2 / P-gp BBB penetration SLCO1A2 / ABCB1 Uptake & Creatinineefflux Almotriptan Sumatriptan SLC22A2 / SLC22A7 / SLC22A3 / OCT2 / OAT2 / OCT3 / MATE1 / MATE2-K Renal clearance of creatinine Uptake & efflux Creatinine Cimetidine OCT1 / MATE1 Hepatic clearance of organic cations SLC47A1SLC22A1 / SLC47A2 / SLC47A1 Uptake & efflux Metformin Cimetidine OATP1A2 / P-gp BBB penetration SLCO1A2 / ABCB1 Uptake & efflux Almotriptan Sumatriptan OATP1B1 / NTCP / BSEP Hepatic clearance of bile salts, SLC01B1 / SLC10A1/ ABCB11 Uptake & efflux Taurocholate Rifampicin OCT1 / MATE1 Hepaticcholestatic clearance liver of injuryorganic cations SLC22A1 / SLC47A1 Uptake & efflux Metformin Cimetidine OATP1B1 / MRP2 Hepatic clearance of organic anions SLC01B1 / ABCC2 Uptake & efflux Estradiol-17-ß-D-glucuronide MK571 Hepatic clearance of bile salts, Uptake & efflux OATP1B1 / NTCP / BSEP cholestatic liver injury SLCO1B1 / SLC10A1/ ABCB11 Taurocholate Rifampicin Hepatic OATP1B1 / BCRP Hepatic clearance of organic anions SLC01B1 / ABCG2 Uptake & efflux Estrone-3-sulfate KO143 Transporter OATP1B1 / MRP2 Hepatic clearance of organic anions SLCO1B1 / ABCC2 Uptake & efflux Estradiol-17-ß-D-glucuronide MK571 Hepatic Models OATP1B3 / BCRP Hepatic clearance of organic anions SLCO1B3 / ABCG2 Uptake & efflux Bromosulfophthalein CCK-8Hepatic OATP1B1 / BCRP Hepatic clearance of organic anions SLCO1B1 / ABCG2 Uptake & efflux Estrone-3-sulfate KO143 Transporterransporter OATP1B3 / MRP2 Hepatic clearance of organic anions SLCO1B3 / ABCC2 Uptake & efflux Bromosulfophthalein CCK-8Models OATP1B3 / BCRP Hepatic clearance of organic anions SLCO1B3 / ABCG2 Uptake & efflux Bromosulfophthalein CCK-8 Models OATP1B3 / P-gp Hepatic clearance of organic anions SLCO1B3 / ABCB1 Uptake & efflux Quinidine for MDR1, CCK-8 for OATP1B3 Verapamil OATP1B3 / MRP2 Hepatic clearance of organic anions SLCO1B3 / ABCC2 Uptake & efflux Bromosulfophthalein CCK-8 OATP1B3 / P-gp Hepatic clearance of organic anions SLCO1B3 / ABCB1 Uptake & efflux Quinidine for MDR1, CCK-8 for OATP1B3 Verapamil

Notes for multiple-transporter models: 1. In all multiple-transporter models, each transporter is localized to the appropriate membrane. 2. All control cells are exactly matched to the cells used in the assays. 3. All transporters are human, and all cells used are MDCK-II.

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