Selectivity at ion channels
Key to terms and symbols		Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference TRPV4 Hs Activator Activation 5.2 pEC50 - 32 ⤷ pEC50 5.2 (EC50 6.6x10-6 M) [32]

Selectivity at other protein targets
Key to terms and symbols		Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference E1A binding protein p300 Hs Inhibitor Inhibition 4.6 pIC50 - 2 ⤷ pIC50 4.6 (IC50 2.5x10-5 M) [2]

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 [10,23], D-Phe-Gln [1], cyclo(L-Hyp-L-Ser) (i.e. JBP485) [5,27], nateglinide [38], glibenclamide [31] and penicillin G (benzylpenicillin) [3]. Among many other molecules, PEPT1 has been shown to interact with L-Dopa-L-Phe [35,40], D-Phe-Gly-L-Dopa [43], JBP485 prodrugs (e.g. JBP485-3-CH2-O-valine, J3V) [21], 5-Aminosalicylic acid (5-ASA) derivatives (i.e. Gly-ASA, Glu-ASA, Val-ASA) [29,53], cinnabar (i.e. α-HgS >96%) [47], doxorubicin-tripeptide (i.e. doxorubicin-Gly-Gly-Gly) [13], scutellarin methyl ester-4'-dipeptide conjugates (e.g. scutellarin methyl ester-4'-Val-homo-Leu) [26], curcumin (CUR)-peptide derivatives (i.e. CUR-Phe-Val, CUR-Ile-Val) [54], gemcitabine amino acid ester prodrugs (i.e. 5'-L-valyl-gemcitabine, V-Gem) [33,39], decitabine amino acid ester prodrugs (e.g. 5'-O-L-valyl-decitabine, L-Val-DAC) [36-37], didanosine amino acid ester prodrugs (e.g. 5'-O-L-valyl-didanosine, L-Val-DDI) [52], floxuridine amino acid ester prodrugs (e.g. 5'-L-isoleucyl and 5'-L-valyl amino acid ester prodrugs of floxuridine) [24-25], floxuridine amino acid monoester prodrugs (e.g. 5'-O-D-valyl-floxuridine) [42], 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) [41], 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) [20], 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 [34], thiodipeptide prodrugs of for example, ibuprofen and propofol [11], alanylpyrraline (Ala-Pyrr) and pyrralylalanine (Pyrr-Ala) [12], 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] [6], 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)) [28] 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) [4]. In recent years, PEPT1 has been shown to interact with a large variety of specifically targeted (i.e. peptide- or amino acid-functionalized) nanoparticles [7-9,14-15,48], (nano)micelles [22,44,46,51] and nanocomposites [16,45,49-50].

Ligand mentioned in the following text fields
Sphingolipid Δ4-desaturase comments