BMS-986205 is an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic activity, alone and in combination with nivolumab in advanced cancers in a phase 1/2a trial

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).

IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.

INCB024360 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.

NLG-8189 is an inhibitor of IDO and INDOL1 (IDO2)

PF-06840003 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1),with potential immunomodulating and antineoplastic activities.

Roxyl-WL is a highly potent and selective inhibitor of IDO1 with IC50 of 1 nM.

(Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

(S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.

IDO1-IN-2 (compound 16) is a potent and selective IDO1 inhibitor with IC50s of 81 nM, 59 nM (mouse) and 28 nM (rat), respectively. IDO1-IN-2 has anti-cancer activity.

(Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes.

IDO-IN-6 (NLG-1486) is an indoleamine 2,3-dioxygenase (IDO) extracted from patent WO WO2012142237A1, Compound 1486, has an IC50 of <1 μM.

IDO-IN-8 (NLG-1487) is an indoleamine 2,3-dioxygenase (IDO) extracted from patent WO WO2012142237A1, compound 1487, has an IC50 of 1-10 μM.

BMT-297376, the optimized Linrodostat, is a potent IDO1 inhibitor.

IDO-IN-15 is an IDO1 inhibitor (IC50 < 0.51 nM).

IDO-IN-14 is an IDO inhibitor with an IC50 value of 0.6928 nM.

NLG802 is a prodrug of indoximod, an orally active indoleamine 2,3-dioxygenase (IDO) inhibitor.

IDO1-IN-11 is an IDO1 inhibitor with an IC50 value of 0.6 nM.

IDO1-IN-12 is a potent and orally available IDO1 inhibitor.

IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active.

IDO1-IN-13 (compound 27a) is a potent IDO1 inhibitor with an IC50 of 61.6 nM. IDO1-IN-13 has cellular IDO1 inhibition (HeLa EC50= 30 nM). IDO1-IN-13 decreases 51% of the kyn/trp ratio in SK-OV-3 xenograft tumor tissues.

IDO1-IN-14 (compound 4a) is a potent IDO1 inhibitor with an IC50 of 396.9 nM. IDO1-IN-14 has cellular IDO1 inhibition (HeLa EC50=3393 nM).

IDO1-IN-15 is a potent IDO1 inhibitor (IC50=127 nM). IDO1-IN-15 has comparable potency against IDO1 enzyme in vitro with Epacadostat.

ZC0101 is a potent, orally active IDO1 and TrxR dual inhibitor with IC50 values of 0.084 μM and 7.98 μM, respectively. ZC0101 effectively induces apoptosis and ROS accumulation in cancer cells.

DP00477 is a potent IDO1 (indoleamine 2,3-dioxygenase 1) inhibitor with an IC50 value of 7.0 µM. DP00477 has the potential for the research of cancer.

ZC0109 is a dual inhibitor of IDO1 and thioredoxin reductase 1 (TrxR1) with IC50s of 50 nM and 3.0 μM, respectively. ZC0109 induces ROS accumulation and cell cycle arrest at G1/S phase, thus leads to cancer cells Apoptosis.

CAY10581, a pyranonaphthoquinone derivative, is a highly specific and reversible uncompetitive IDO Inhibitor with an IC50 of 55 nM.