Target Validation Information
TTD ID T89697
Target Name Indoleamine 2,3-dioxygenase 1 (IDO1)
Type of Target
Successful
Drug Potency against Target 1,2-NAPHTHOQUINONE Drug Info IC50 = 7100 nM [3]
1,4-Naphthoquinone Drug Info IC50 = 990 nM [3]
1H-indole-4,7-dione Drug Info Ki = 190 nM [4]
2,2-dimethyl-2H-benzo[g]chromene-5,10-dione Drug Info IC50 = 214 nM [3]
2,3-dichloro-1,4-naphthoquinone Drug Info IC50 = 280 nM [3]
2,3-dihydrobenzo[d]thiazole-2-thiol Drug Info IC50 = 7000 nM [8]
2,4-Dichlorobenzenemethanethiol Drug Info IC50 = 4600 nM [9]
2-(1H-Imidazol-4-yl)benzene-1,3-diol Drug Info IC50 = 5300 nM [5]
2-(1H-Imidazol-4-yl)phenol Drug Info Ki = 8900 nM [5]
2-Chlorobenzenemethanethiol Drug Info IC50 = 15000 nM [9]
2-hydroxygarveatin E Drug Info Ki = 1400 nM [2]
2-HYDROXYGARVIN A Drug Info Ki = 2300 nM [2]
2-methoxy-1,4-naphthoquinone Drug Info IC50 = 720 nM [3]
3,4-Dichlorobenzenemethanethiol Drug Info IC50 = 1100 nM [9]
3-(1H-Imidazol-4-yl)benzenethiol Drug Info Ki = 5300 nM [5]
3-(4H-Imidazol-4-yl)benzenethiol Drug Info Ki = 4800 nM [5]
4-(1H-1,2,3-triazol-5-yl)pyridine Drug Info IC50 = 5000 nM [8]
4-(2-(diethylamino)ethylamino)-1-naphthol Drug Info IC50 = 3000 nM [8]
4-(2-Hydroxyethoxy)-1-naphthol Drug Info IC50 = 12500 nM [8]
4-(Benzylamino)-1-naphthol Drug Info IC50 = 2500 nM [8]
4-(Cyclohexylamino)-1-naphthol Drug Info IC50 = 15000 nM [8]
4-(ethylamino)naphthalen-1-ol Drug Info IC50 = 16000 nM [8]
4-(Isopropylamino)-1-naphthol Drug Info IC50 = 12500 nM [8]
4-(methylamino)naphthalen-1-ol Drug Info IC50 = 12500 nM [8]
4-(Pent-3-ylamino)-1-naphthol Drug Info IC50 = 3500 nM [8]
4-(propylamino)naphthalen-1-ol Drug Info IC50 = 4500 nM [8]
4-(tert-butylamino)naphthalen-1-ol Drug Info IC50 = 4000 nM [8]
4-amino-1,2,5-oxadiazole-3-carboximidamide Drug Info IC50 = 1000 nM [7]
4-aminonaphthalen-1-ol Drug Info IC50 = 6000 nM [8]
4-Chlorobenzenemethanethiol Drug Info IC50 = 1100 nM [9]
4-Fluorobenzenemethanethiol Drug Info IC50 = 1900 nM [9]
4-Methoxybenzenemethanethiol Drug Info IC50 = 9400 nM [9]
4-methoxynaphthalen-1-amine Drug Info IC50 = 5500 nM [8]
4-Methylbenzenemethanethiol Drug Info IC50 = 6500 nM [9]
4-Phenylimidazole Drug Info Ki = 4400 nM [5]
4-phenylthiazole-2-thiol Drug Info IC50 = 4000 nM [8]
5-(isopropylamino)quinolin-8-ol Drug Info IC50 = 15000 nM [8]
5-aminoquinolin-8-ol Drug Info IC50 = 1000 nM [8]
5-phenyl-1H-1,2,3-triazole Drug Info IC50 = 5000 nM [8]
ANNULIN A Drug Info Ki = 690 nM [2]
ANNULIN B Drug Info Ki = 120 nM [2]
ANNULIN C Drug Info Ki = 140 nM [2]
Avastin+/-Tarceva Drug Info IC50 = 1000 nM [3]
BENZENEMETHANETHIOL Drug Info IC50 = 13000 nM [9]
Exiguamine A Drug Info Ki = 41 nM [4]
EXIGUAMINE B Drug Info Ki = 80 nM [6]
GARVEATIN A Drug Info Ki = 3200 nM [2]
Garveatin C Drug Info Ki = 1200 nM [2]
Garveatin E Drug Info Ki = 3100 nM [2]
N-[2-(Indol-3-yl)ethyl]-S-benzyl-dithiocarbamate Drug Info Ki = 17150 nM [1]
Naphthalene-1,4-diol Drug Info IC50 = 10000 nM [8]
NLG8189 Drug Info Ki = 6600 nM [2]
S-(2,4-Dichlorobenzyl)isothiourea hydrobromide Drug Info IC50 = 1100 nM [9]
S-(2-Chlorobenzyl)isothiourea hydrochloride Drug Info IC50 = 4800 nM [9]
S-(3,4-Dichlorobenzyl)isothiourea hydrochloride Drug Info IC50 = 7300 nM [9]
S-(3-Chlorobenzyl)isothiourea hydrochloride Drug Info IC50 = 1400 nM [9]
S-(4-Bromobenzyl)isothiourea hydrobromide Drug Info IC50 = 800 nM [9]
S-(4-Chlorobenzyl)isothiourea hydrochloride Drug Info IC50 = 600 nM [9]
S-(4-Cyanobenzyl)isothiourea hydrobromide Drug Info IC50 = 2600 nM [9]
S-(4-Ethylbenzyl)isothiourea hydrochloride Drug Info IC50 = 2500 nM [9]
S-(4-Fluorobenzyl)isothiourea hydrochloride Drug Info IC50 = 2000 nM [9]
S-(4-Methoxybenzyl)isothiourea hydrochloride Drug Info IC50 = 10000 nM [9]
S-(4-Methylbenzyl)isothiourea hydrochloride Drug Info IC50 = 6800 nM [9]
S-(4-Nitrobenzyl)isothiourea hydrochloride Drug Info IC50 = 2200 nM [9]
S-Benzyl-brassinin Drug Info Ki = 13220 nM [1]
Seco-exiguamine Drug Info Ki = 80 nM [6]
References
REF 1 Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors. J Med Chem. 2006 Jan 26;49(2):684-92.
REF 2 Indoleamine 2,3-dioxygenase inhibitors from the Northeastern Pacific Marine Hydroid Garveia annulata. J Nat Prod. 2006 Oct;69(10):1496-9.
REF 3 Indoleamine 2,3-dioxygenase is the anticancer target for a novel series of potent naphthoquinone-based inhibitors. J Med Chem. 2008 Mar 27;51(6):1706-18.
REF 4 Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine A. J Med Chem. 2008 May 8;51(9):2634-7.
REF 5 Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase. J Med Chem. 2008 Aug 28;51(16):4968-77.
REF 6 Biomimetic synthesis of the IDO inhibitors exiguamine A and B. Nat Chem Biol. 2008 Sep;4(9):535-7.
REF 7 Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma mo... J Med Chem. 2009 Dec 10;52(23):7364-7.
REF 8 Rational design of indoleamine 2,3-dioxygenase inhibitors. J Med Chem. 2010 Feb 11;53(3):1172-89.
REF 9 S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5126-9.

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