Drug Information

General Information of This Drug
Drug ID DRG00040
Drug Name NLG919
Synonyms
NLG919; 1402836-58-1; 1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol; NLG919 (GDC-0919); 1-Cyclohexyl-2-(5H-imidazo-[5,1-a]isoindol-5-yl)ethanol; CHEMBL3629569; NLG919(GDC-0919,Navoximod); MFCD26142661; 5H-Imidazo[5,1-a]isoindole-5-ethanol, alpha-cyclohexyl-; 1-Cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethan-1-ol; 1-CYCLOHEXYL-2-{5H-IMIDAZO[4,3-A]ISOINDOL-5-YL}ETHANOL; YTRRAUACYORZLX-UHFFFAOYSA-N; GTPL9019; SCHEMBL13280897; DTXSID20735206; EX-A574; HMS3653M05; AMY12328; BCP09887; BDBM50126144; s7111; AKOS025287054; CCG-267268; CS-3512; SB16495; NCGC00386274-04; AC-30124; AS-35112; DA-45347; HY-13983; SY046802; FT-0700192; SW219857-1; A853907; J-690162; Q27087945; 1-cyclohexyl-2-[5H-imidazo[4,3-a]isoindol-5-yl]ethan-1-ol; 5-(2-Cyclohexyl-2-hydroxyethyl)-5H-imidazo[5,1-a]isoindole; 3-(2-Amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione hydrochloride; a-Cyclohexyl-5H-imidazo[5,1-a]isoindole-5-ethanol; 1-Cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol; NLG919; alpha-Cyclohexyl-5H-imidazo[5,1-a]isoindole-5-ethanol;1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
   Click to Show/Hide
Target(s) Indoleamine 2,3-dioxygenase 1 (IDO1)  Target Info 
Structure
Formula
C18H22N2O
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 282.4
Lipid-water partition coefficient (xlogp) 3.5
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
Rotatable Bond Count (rotbonds) 3
PubChem CID
66558287
Canonical smiles
C1CCC(CC1)C(CC2C3=CC=CC=C3C4=CN=CN24)O
InChI
InChI=1S/C18H22N2O/c21-18(13-6-2-1-3-7-13)10-16-14-8-4-5-9-15(14)17-11-19-12-20(16)17/h4-5,8-9,11-13,16,18,21H,1-3,6-7,10H2
InChIKey
YTRRAUACYORZLX-UHFFFAOYSA-N
IUPAC Name
1-cyclohexyl-2-(5H-imidazo[5,1-a]isoindol-5-yl)ethanol
Each Peptide-drug Conjugate Related to This Drug
Full Information of The Activity Data of The PDC(s) Related to This Drug
NLG-RGD [Investigative]
 PDC Info 
Obtained from the Model Organism Data
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of Treg cells 1%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L5 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal Regulatory CD4+ T cell Homo sapiens
Experiment 2 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of NK cells 2%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L6 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal Natural killer cell Homo sapiens
Experiment 3 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of IFN-γ-producing CD8 T cells 40%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L4 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal IFN-gamma-producing CD4 T cell Homo sapiens
Experiment 4 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of IFN-γ-producing CD4 T cells 16%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L3 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal IFN-gamma-producing CD4 T cell Homo sapiens
Experiment 5 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of CD8 T cells 34%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L2 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal CD8 T cell Homo sapiens
Experiment 6 Reporting the Activity Data of This PDC [1]
Indication Tumor
Efficacy Data Percentage of CD4 T cells 32%
Evaluation Method Quantification of tumor-infiltrating immune cells assay
Administration Time 30 min
Administration Dosage 25 µM
MOA of PDC
Significantly, this nanoinhibitor boosts the antitumor immune response of PD-L1 blockade by increasing immune effector cells and reducing immunosuppressive cells.
Description
These findings support that aPD-L1 plus NLG-RGD NI efficiently elicits antitumor immunity by enhancing the activation and survival of immune effector cells and attenuating the accumulation immunosuppressive Treg cells.
In Vivo Model Pan02 tumor model.
In Vitro Model Normal CD4 T cell Homo sapiens
References
Ref 1 Modularly Designed Peptide Nanoprodrug Augments Antitumor Immunity of PD-L1 Checkpoint Blockade by Targeting Indoleamine 2,3-Dioxygenase. J Am Chem Soc. 2020 Feb 5;142(5):2490-2496. doi: 10.1021/jacs.9b12232. Epub 2020 Jan 24.