Transporters Moving this Compound Across a Lipid Membrane
Transporter EC number Reaction Reference OATP2B1

Selectivity at ion channels
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Target Sp. Type Action Value Parameter Concentration range (M) Reference Kir6.2 Rn Channel blocker Antagonist - - 1x10-6 23 ⤷ Conc range: 1x10-6 M [23] Voltage: -60.0 mV CFTR Hs Channel blocker - 4.7 pKi - 39 ⤷ pKi 4.7 (Ki 2.18x10-5 M) [39] Kir6.2 Mm Channel blocker Antagonist 5.7 pIC50 1x10-6 20-21 ⤷ pIC50 5.7 Conc range: 1x10-6 M [20-21] Voltage: Physiological / -60.0 mV Kir6.1 Hs Inhibitor - - - - ⤷ Kir6.2 Hs Inhibitor - - - - ⤷

Selectivity at transporters
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Target Sp. Type Action Value Parameter Concentration range (M) Reference OATP2B1 Hs Inhibitor Inhibition - - - ⤷

Targets where the ligand is described in the comment field
Target	Comment
Peptide transporter 1	Although most di/tripeptides can bind PEPT1, not all of them are substrates. The uptake depends on the structural features (charge, hydrophobicity, size, side chain flexibility, etc.) of the di/tripeptide. A variety of dipeptides and drugs interact with PEPT1, including D-Phe-Ala [9,26], D-Phe-Gln [1], cyclo(L-Hyp-L-Ser) (i.e. JBP485) [4,31], nateglinide [45], glibenclamide [38] and penicillin G (benzylpenicillin) [2]. Among many other molecules, PEPT1 has been shown to interact with L-Dopa-L-Phe [42,48], D-Phe-Gly-L-Dopa [51], JBP485 prodrugs (e.g. JBP485-3-CH2-O-valine, J3V) [24], 5-Aminosalicylic acid (5-ASA) derivatives (i.e. Gly-ASA, Glu-ASA, Val-ASA) [35,62], cinnabar (i.e. α-HgS >96%) [55], doxorubicin-tripeptide (i.e. doxorubicin-Gly-Gly-Gly) [13], scutellarin methyl ester-4'-dipeptide conjugates (e.g. scutellarin methyl ester-4'-Val-homo-Leu) [30], curcumin (CUR)-peptide derivatives (i.e. CUR-Phe-Val, CUR-Ile-Val) [63], gemcitabine amino acid ester prodrugs (i.e. 5'-L-valyl-gemcitabine, V-Gem) [40,47], decitabine amino acid ester prodrugs (e.g. 5'-O-L-valyl-decitabine, L-Val-DAC) [43-44], didanosine amino acid ester prodrugs (e.g. 5'-O-L-valyl-didanosine, L-Val-DDI) [61], floxuridine amino acid ester prodrugs (e.g. 5'-L-isoleucyl and 5'-L-valyl amino acid ester prodrugs of floxuridine) [28-29], floxuridine amino acid monoester prodrugs (e.g. 5'-O-D-valyl-floxuridine) [50], floxuridine dipeptide monoester prodrugs (e.g. 5'-L-phenylalanyl-L-tyrosyl-floxuridine, 5'-L-phenylalanyl-L-glycyl-floxuridine, and 5'-L-isoleucyl-L-glycyl-floxuridine) [49], amino acid acyloxy ester prodrugs of guanidine oseltamivir carboxylate (GOC) (e.g. GOC-L-Val, the L-valyl acyloxy ethyl prodrug of GOC) [17] and the valyl amino acid prodrug of GOC with the isopropyl-methylene-dioxy linker (i.e. GOC-ISP-Val) [22], amino acid acyloxy ester prodrugs of zanamivir (Zan, e.g. Zan-L-Val, the L-valyl acycloxy ethyl prodrug of Zan) [18], peramivir-(CH2)2-L-Val and peramivir-L-Ile [41], thiodipeptide prodrugs of for example, ibuprofen and propofol [10], alanylpyrraline (Ala-Pyrr) and pyrralylalanine (Pyrr-Ala) [11], dipeptide-bound derivatives of N6-(carboxymethyl)lysine (CML) and N6-(1-carboxyethyl)-lysine (CEL) (i.e. Ala-CML, CML-Ala, Ala-CEL, CEL-Ala) [19], Flammulina velutipes polysaccharide(FVP)-iron(III) complex [FVP-Fe(III) complex] [5], dipeptides of p-borono-L-phenylalanine (BPA) and tyrosine (i.e. L-Tyr-p-L-BPA (Tyr-BPA), p-L-BPA-L-tyrosine (BPA-Tyr)) [34] and AuIII‐peptidodithiocarbamato complexes of the type [AuIIIBr2(dtc‐AA1‐AA2‐OR], in which AA1 = N‐methylglycine (Sar), L/D-Pro; AA2 = L/D-Ala, α‐aminoisobutyric acid (Aib); R = OtBu, triethylene glycol methyl ether) (e.g. dtc‐Pro‐Aib‐OtBu) [3]. In recent years, PEPT1 has been shown to interact with a large variety of specifically targeted (i.e. peptide- or amino acid-functionalized) nanoparticles [6-8,14-15,56], (nano)micelles [25,52,54,60] and nanocomposites [16,53,58-59].
Peptide transporter 2	Although most di/tripeptides can bind PEPT2, not all of them are substrates. The uptake depends on the structural features (charge, hydrophobicity, size, side chain flexibility, etc.) of the di/tripeptide. Like PEPT1, PEPT2 interacts with dipeptides and drugs including D-Phe-Ala [9,46], nateglinide [45], glibenclamide [38], penicillin G (benzylpenicillin) [36], polymyxins (i.e. polymyxin B and colistin) [32] and entecavir [57]. PEPT2 has been shown to interact with dipeptides of p-borono-L-phenylalanine (BPA) and tyrosine (i.e. L-Tyr-p-L-BPA (Tyr-BPA), p-L-BPA-L-tyrosine (BPA-Tyr)) [34] and with AuIII‐peptidodithiocarbamato complexes of the type [AuIIIBr2(dtc‐AA1‐AA2‐OR), in which AA1 = N‐methylglycine (Sar), L/D‐Pro; AA2 = L/D‐Ala, α‐aminoisobutyric acid (Aib); R = OtBu, triethylene glycol methyl ether, e.g. dtc‐Pro‐Aib‐OtBu) [3].