| Assay ID | Title | Year | Journal | Article |
|---|
| AID1053470 | Antiproliferative activity against mouse LLC cells at 50 uM by WST-1 assay | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1728719 | Inhibition of recombinant human IDO1 expressed in Escherichia coli BL21(DE3) assessed as effect on kynurenine level using L-tryptophan as substrate incubated for 1 hr by Ehrlich's reagent based assay | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective. |
| AID1558437 | Competitive inhibition of recombinant human IDO1 expressed in Escherichia coli BL21 cells assessed as apparent inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysis | | | |
| AID1558472 | Antitumor activity against mouse H22 cells implanted in Kunming mouse assessed as reduction in tumor weight at 100 mg/kg, po qd administered for 2 weeks and measured post-treatment | | | |
| AID1053462 | Reduction of Foxp3 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, po qd after 14 days by RT-PCR analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1053465 | Induction of IDO1 mRNA expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, po qd after 14 days by RT-PCR analysis relative to control | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1332713 | Inhibition of recombinant human IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate after 30 mins in presence of catalase | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. |
| AID568286 | Inhibition of human IDO activity by spectrophotometry | 2011 | Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
| Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1053471 | Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID443996 | Inhibition of human recombinant IDO expressed in HEK293 cells assessed as blockade of tryptophan degradation by HPLC | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1416466 | Cytotoxicity against human MDA-MB-231 cells assessed as induction of morphological changes at 2 times IDO1 inhibitory IC50 after 48 hrs by cytell imaging analysis | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1. |
| AID1557375 | Tmax in human cancer patient at 2000 mg bid for 28 days by LC-MS method | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10
| Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1154624 | Inhibition of recombinant N-terminal His-tagged human IDO (Ala2 to Gly403) overexpressed in Escherichia coli BL21 AI using L-tryptophan as substrate assessed as formation of kynurenine incubated for 5 mins in presence of p-dimethylaminobenzaldehyde | 2014 | European journal of medicinal chemistry, Jul-23, Volume: 82 | Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties. |
| AID1557374 | Cmax in human cancer patient at 2000 mg bid for 28 days by LC-MS method | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10
| Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID604724 | Cytotoxicity against mouse mastocytoma P815B cells assessed as cell viability at 20 uM after overnight incubation by MTT assay | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
| Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1558479 | In vivo blockade of kynurenine pathway in Kunming mouse implanted with mouse H22 cells assessed as decrease in kynurenine level in serum at 100 mg/kg, po qd for 2 weeks by HPLC analysis | | | |
| AID1558465 | Antitumor activity against mouse LLC cells implanted in C57BL/6 mouse assessed as reduction in tumor weight at 100 mg/kg, po qd administered for 2 weeks and measured post-treatment | | | |
| AID1545103 | Inhibition of IDO1 in interferon-gamma-induced human HeLa cells at 10 uM using L-tryptophan substrate incubated for 24 hrs relative to untreated control | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Design, synthesis and biological evaluation of novel aryl-acrylic derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID734358 | Inhibition of mouse TDO overexpressed in mouse P815B cells using L-Trp as substrate assessed as kynurenine level at 22 uM by HPLC analysis relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A. |
| AID1053475 | Inhibition of human IDO1-mediated tryptophan degradation expressed in human tumor cells | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1416458 | Inhibition of recombinant human IDO1 assessed as reduction in conversion of L-tryptophan to kynurenine after 1 hr by methylene blue dye based HPLC method | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1. |
| AID1583596 | Antitumor activity against wild type mouse B16F10 cells xenografted in C57BL/6 mouse assessed as reduction in tumor volume at 200 mg/kg, iv administered once every 2 days for 3 weeks and measured after 21 days relative to control | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. |
| AID1558487 | Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as reduction in kynurenine formation after 5 hrs by microplate reader analysis | | | |
| AID1660990 | Inhibition of human DHFR in presence of DHF and NADPH by UV-vis spectrometry by Lineweaver-Burk plot analysis | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15
| The Structural Basis for Nonsteroidal Anti-Inflammatory Drug Inhibition of Human Dihydrofolate Reductase. |
| AID1226035 | Activity of 1 uM recombinant human TDO assessed as substrate consumption at 100 uM at 37 degC at pH 7.5 after 1 hr by HPLC with fluorescence detection method | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1558447 | Binding affinity to human IDO2 assessed as change in spectral signal at 200 uM by CPMG NMR spectrometry analysis | | | |
| AID1558467 | Antitumor activity against mouse LLC cells implanted in C57BL/6 mouse assessed as reduction in tumor volume at 100 mg/kg, po qd administered for 2 weeks and measured at 2 days interval during compound dosing relative to control | | | |
| AID1373982 | Cytotoxicity in human A375 cells assessed as cell viability at 10 uM incubated for 48 hrs by MTT assay | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
| A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: Synthesis, biological investigation and docking studies. |
| AID1053474 | Competitive inhibition of human recombinant IDO1 using L-tryptophan as substrate | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1053467 | Antitumor activity against mouse LLC cells allografted in C57BL/6 mouse assessed as reduction in tumor volume at 200 mg/kg, po qd after 14 days | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1377500 | Inhibition of IDO1 (unknown origin) | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent IDO1 inhibitors derived from tryptophan using scaffold-hopping and structure-based design approaches. |
| AID443994 | Inhibition of IDO by cell-free assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1558450 | Binding affinity to human IDO2 at 200 uM by STD NMR spectrometry analysis | | | |
| AID1377488 | Inhibition of IFNgamma-induced IDO1 in human HeLa cells using L-tryptophan as substrate after 24 hrs | 2017 | European journal of medicinal chemistry, Sep-29, Volume: 138 | Discovery of potent IDO1 inhibitors derived from tryptophan using scaffold-hopping and structure-based design approaches. |
| AID1627819 | Inhibition of human IDO2 expressed in Escherichia coli BL21 Star assessed as kynurenine formation using L-Trp as substrate preincubated for 90 mins measured after 30 mins by bridge-IT fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
| 1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2). |
| AID1558446 | Binding affinity to human IDO1 assessed as change in spectral signal at 200 uM by CPMG NMR spectrometry analysis | | | |
| AID568290 | Inhibition of IDO | 2011 | Bioorganic & medicinal chemistry, Feb-15, Volume: 19, Issue:4
| Indol-2-yl ethanones as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1558451 | Binding affinity to human TDO at 200 uM by STD NMR spectrometry analysis | | | |
| AID1226031 | Ratio of Kcat to Km for recombinant human IDO assessed as formation of N-formyl-L-kynurenine at 37 degC at pH 6.5 after 5 to 15 mins by HPLC with fluorescence detection method | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1416462 | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 2 times IDO1 inhibitory IC50 after 48 hrs by MTT assay | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1. |
| AID1557376 | Half life in human cancer patient at 2000 mg bid for 28 days by LC-MS method | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10
| Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1053476 | Competitive inhibition of human IDO1 in presence of tryptophan | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID361929 | Inhibition of rabbit small intestine indoleamine 2,3-dioxygenase | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
| Structure based development of phenylimidazole-derived inhibitors of indoleamine 2,3-dioxygenase. |
| AID604723 | Competitive inhibition of histidine-tagged human recombinant IDO expressed in bacterial strain BL21 AI using L-Trptophan as substrate measured at 490 nm wavelength after 6 min by colorimetric assay | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
| Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1557373 | AUC in human cancer patient at 2000 mg bid for 28 days by LC-MS method | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10
| Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1373985 | Inhibition of IDO1 in IFN-gamma-stimulated human A375 cells assessed as decrease in L-kynurenine levels at 10 uM in presence of L-Trp incubated for 48 hrs by HPLC method | 2018 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 28, Issue:4
| A multicomponent approach in the discovery of indoleamine 2,3-dioxygenase 1 inhibitors: Synthesis, biological investigation and docking studies. |
| AID1226027 | Retention time of the compound by HPLC analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID734359 | Inhibition of mouse IDO1 overexpressed in mouse P815B cells using L-Trp as substrate assessed as kynurenine level at 22 uM by HPLC analysis relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A. |
| AID734361 | Cytotoxicity against mouse P815B cells assessed as cell viability at 10 uM by MTT assay relative to control | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A. |
| AID734365 | Inhibition of human recombinant IDO1 using L-Trp as substrate assessed as kynurenine level after 30 mins | 2013 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 23, Issue:1
| Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A. |
| AID1558436 | Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs | | | |
| AID1685222 | Inhibition of rabbit IDO using L or D-tryptophan as substrate | 2021 | ACS medicinal chemistry letters, Feb-11, Volume: 12, Issue:2
| Discovery of Carbono(di)thioates as Indoleamine 2,3-Dioxygenase 1 Inhibitors. |
| AID1226029 | Activity of recombinant human IDO assessed as formation of N-formyl-L-kynurenine at 37 degC at pH 6.5 by UV-visible spectrophotometric analysis | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1728748 | Inhibition of IDO1 in human HeLa cells | 2020 | Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24
| Development of Indoleamine 2,3-Dioxygenase 1 Inhibitors for Cancer Therapy and Beyond: A Recent Perspective. |
| AID409715 | Inhibition of indoleamine 2,3-dioxygenase in aerobic condition | 2008 | Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18
| Synthesis and biological activity of 1-methyl-tryptophan-tirapazamine hybrids as hypoxia-targeting indoleamine 2,3-dioxygenase inhibitors. |
| AID443999 | Cytotoxicity against HEK293 cells expressing human recombinant IDO by MTT assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1226026 | Activity of 0.1 uM recombinant human IDO assessed as compound consumption at 100 uM after 1 hr by fluorescence detection method relative to control | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1226025 | Activity of 0.5 uM recombinant human IDO assessed as compound consumption at 100 uM after 1 hr by fluorescence detection method relative to control | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1585058 | Inhibition of IDO1 (unknown origin) using L-Trp as substrate | 2018 | European journal of medicinal chemistry, Dec-05, Volume: 160 | Tryptophan 2,3-dioxygenase inhibitory activities of tryptanthrin derivatives. |
| AID1558453 | Inhibition of IDO1/TDO in IFNgamma-treated human HeLa cells assessed as T cell proliferation at 1 uM measured after 2 days in presence of IL-2, anti-CD3 and IFN-gamma by CFSE dye based flow cytometry analysis (Rvb = 11.7 %) | | | |
| AID1053456 | Antitumor activity against mouse LLC cells allografted in C57BL/6 mouse assessed as reduction in total tumor weight at 200 mg/kg, po qd after 14 days | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1557372 | Inhibition of IDO1 (unknown origin) | 2019 | MedChemComm, Oct-01, Volume: 10, Issue:10
| Recent advances in the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID443997 | Inhibition of mouse recombinant TDO expressed in mouse P815B cells assessed as blockade of tryptophan degradation by HPLC | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID638470 | Inhibition of His-tagged recombinant human IDO1 expressed in Escherichia coli using tryptophan as substrate by spectrophotometric analysis | 2012 | Bioorganic & medicinal chemistry, Feb-01, Volume: 20, Issue:3
| Novel indoleamine 2,3-dioxygenase-1 inhibitors from a multistep in silico screen. |
| AID1416457 | Inhibition of recombinant human IDO1 assessed as reduction in conversion of L-tryptophan to kynurenine by methylene blue dye based spectrometric method | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1. |
| AID1558470 | Antitumor activity against mouse H22 cells implanted in Kunming mouse assessed as reduction in tumor volume at 100 mg/kg, po qd administered for 2 weeks and measured at 2 days interval during compound dosing relative to control | | | |
| AID1053464 | Induction of IDO1 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, po qd after 14 days by Western blotting analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1558443 | Uncompetitive inhibition of recombinant human TDO expressed in Escherichia coli BL21 (DE3) assessed as assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysis | | | |
| AID1558433 | Inhibition of recombinant human TDO expressed in Escherichia coli BL21 (DE3) assessed as reduction in conversion of L-tryptophan to N-formyl kynurenine using L-tryptophan as substrate after 30 mins by methylene blue assay | | | |
| AID1558480 | In vivo blockade of kynurenine pathway in Kunming mouse implanted with mouse H22 cells assessed as increase in tryptophan level in serum at 100 mg/kg, po qd for 2 weeks by HPLC analysis | | | |
| AID1558444 | Mixed uncompetitive inhibition of recombinant human TDO expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysis | | | |
| AID443995 | Inhibition of mouse recombinant IDO expressed in mouse P815B cells assessed as blockade of tryptophan degradation by HPLC | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1332708 | Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. |
| AID1545104 | Inhibition of purified recombinant human IDO1 using L-tryptophan substrate incubated fro 30 mins | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Design, synthesis and biological evaluation of novel aryl-acrylic derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1327829 | Inhibition of IDO1 in IFNgamma-induced human MDA-MB-231 cells using tryptophan as substrate preincubated for 4 hrs followed by substrate addition for 5 hrs by spectrophotometric method | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Fused Heterocyclic Compounds as Potent Indoleamine-2,3-dioxygenase 1 Inhibitors. |
| AID379168 | Inhibition of human indoleamine 2,3-dioxygenase expressed in Escherichia coli by spectrophotometric activity assay | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10
| Indoleamine 2,3-dioxygenase inhibitors from the Northeastern Pacific Marine Hydroid Garveia annulata. |
| AID1053461 | Reduction of Foxp3 protein expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, po qd after 14 days by Western blotting analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1327825 | Inhibition of N-terminus 6xHis-tagged human IDO1 expressed in Escherichia coli M15 using L-tryptophan as substrate preincubated for 1 hr measured after 15 mins in presence of bovine liver and methylene blue by spectrophotometric analysis | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Fused Heterocyclic Compounds as Potent Indoleamine-2,3-dioxygenase 1 Inhibitors. |
| AID1053463 | Reduction of Foxp3 mRNA expression in tumor of C57BL/6 mouse allografted with mouse LLC cells at 200 mg/kg, po qd after 14 days by PCR analysis | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID1332702 | Competitive inhibition of recombinant human C-terminal His6-tagged IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) in presence of varying concentration of L-tryptophan substrate after 30 mins | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. |
| AID1558431 | Inhibition of recombinant human IDO1 expressed in Escherichia coli BL21 cells assessed as reduction in conversion of L-tryptophan to N-formyl kynurenine using L-tryptophan as substrate after 30 mins by methylene blue dye based microplate reader analysis | | | |
| AID1327826 | Inhibition of N-terminus 6xHis-tagged human IDO1 expressed in Escherichia coli M15 using L-tryptophan as substrate preincubated for 1 hr measured after 15 mins in presence of bovine liver and methylene blue by HPLC analysis | 2016 | ACS medicinal chemistry letters, Dec-08, Volume: 7, Issue:12
| Fused Heterocyclic Compounds as Potent Indoleamine-2,3-dioxygenase 1 Inhibitors. |
| AID444000 | Cytotoxicity against mouse P815B cells expressing mouse recombinant TDO by MTT assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1545105 | Inhibition of IDO1 in interferon-gamma-induced human HeLa cells using L-tryptophan substrate incubated for 24 hrs | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Design, synthesis and biological evaluation of novel aryl-acrylic derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1627818 | Inhibition of human IDO1 expressed in Escherichia coli BL21 Star assessed as kynurenine formation using L-Trp as substrate preincubated for 90 mins measured after 30 mins by bridge-IT fluorescence assay | 2016 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
| 1,2,3-Triazoles as inhibitors of indoleamine 2,3-dioxygenase 2 (IDO2). |
| AID1558448 | Binding affinity to human TDO assessed as change in spectral signal at 200 uM by CPMG NMR spectrometry analysis | | | |
| AID443998 | Cytotoxicity against mouse P815B cells expressing mouse recombinant IDO by MTT assay | 2010 | Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
| Rational design of indoleamine 2,3-dioxygenase inhibitors. |
| AID1226024 | Activity of 5 uM recombinant human IDO assessed as compound consumption at 1000 uM after 4 hrs by UV detection method relative to control | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1416461 | Inhibition of IFNgamma-stimulated IDO1 in human MDA-MB-231 cells preincubated for 4 hrs followed by tryptophan addition measured after 5 hrs by methylene blue dye based spectrophotometric method | 2017 | MedChemComm, Aug-01, Volume: 8, Issue:8
| Synthesis and evaluation of oxindoles as promising inhibitors of the immunosuppressive enzyme indoleamine 2,3-dioxygenase 1. |
| AID1583618 | Antitumor activity against mouse B16F10 cells implanted in C57BL/6 cells assessed as tumor growth inhibition at 200 mg/kg, iv administered once every 2 days for 3 weeks and measured after 21 days relative to control | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. |
| AID1350378 | Inhibition of rabbit IDO using tryptophan as substrate | 2018 | ACS medicinal chemistry letters, Feb-08, Volume: 9, Issue:2
| Identification of Potent Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors Based on a Phenylimidazole Scaffold. |
| AID604718 | Inhibition of mouse TDO expressed in mouse mastocytoma P815B cells using L-Trptophan as substrate at 20 uM after overnight by HPLC | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
| Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1545102 | Inhibition of IDO1 in interferon-gamma-induced human HeLa cells at 1 uM using L-tryptophan substrate incubated for 24 hrs relative to untreated control | 2019 | Bioorganic & medicinal chemistry, 07-15, Volume: 27, Issue:14
| Design, synthesis and biological evaluation of novel aryl-acrylic derivatives as novel indoleamine-2,3-dioxygenase 1 (IDO1) inhibitors. |
| AID1226036 | Activity of 10 uM recombinant human TDO assessed as substrate consumption at 100 uM at 37 degC at pH 7.5 after 1 hr by HPLC with fluorescence detection method | 2015 | ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
| N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase. |
| AID1583619 | Antitumor activity against mouse B16F10 cells implanted in C57BL/6 cells assessed as tumor growth inhibition at 200 mg/kg, iv administered once every 2 days for 3 weeks in combination with stattic at 50 mg/kg and measured after 21 days relative to control | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. |
| AID1583622 | Toxicity in C57BL/6 mouse xenografted with wild type mouse B16F10 cells assessed as increase in body weight at 200 mg/kg, iv administered once every 2 days for 3 weeks in combination with static at 50 mg/kg and measured after 21 days | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. |
| AID1558449 | Binding affinity to human IDO1 at 200 uM by STD NMR spectrometry analysis | | | |
| AID1583620 | Toxicity in C57BL/6 mouse xenografted with wild type mouse B16F10 cells assessed as increase in body weight at 200 mg/kg, iv administered once every 2 days for 3 weeks and measured after 21 days | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Bifunctional Naphthoquinone Aromatic Amide-Oxime Derivatives Exert Combined Immunotherapeutic and Antitumor Effects through Simultaneous Targeting of Indoleamine-2,3-dioxygenase and Signal Transducer and Activator of Transcription 3. |
| AID1332706 | Inhibition of recombinant human C-terminal His6-tagged IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate after 30 mins in presence of catalase by methylene blue d | 2016 | European journal of medicinal chemistry, Nov-10, Volume: 123 | Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. |
| AID1346186 | Human indoleamine 2,3-dioxygenase 1 (1.13.11.- Dioxygenases) | 2013 | Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
| Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice. |
| AID625725 | Inhibition of human recombinant indoleamine-2,3-dioxygenase expressed in Escherichia coli BL21 using L-tryptophan as substrate after 30 mins by microplate reader analysis | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
| Structure-activity relationship and enzyme kinetic studies on 4-aryl-1H-1,2,3-triazoles as indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1379946 | Inhibition of IDO1 in human IFN-gamma stimulated human HeLa cells assessed as inhibition of kynurenine production using L-tryptophan substrate incubated for 24 hrs | 2017 | European journal of medicinal chemistry, Nov-10, Volume: 140 | Discovery of imidazoleisoindole derivatives as potent IDO1 inhibitors: Design, synthesis, biological evaluation and computational studies. |
| AID1348816 | Inhibition of human IDO1 assessed as reduction in kynurenine production | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy. |
| AID422790 | Activity at 1.62 uM Aspergillus fumigatus CdpNPT assessed as compound conversion rate at 1 mM after 2 hrs by HPLC analysis in presence of dimethylallyl diphosphate relative to L-tryptophan | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Substrate promiscuity of the cyclic dipeptide prenyltransferases from Aspergillus fumigatus ( section sign). |
| AID1180153 | Inhibition of human recombinant IDO using L-tryptophan as substrate | 2014 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
| Discovery and structure-activity relationships of phenyl benzenesulfonylhydrazides as novel indoleamine 2,3-dioxygenase inhibitors. |
| AID625724 | Competitive inhibition of indoleamine-2,3-dioxygenase | 2011 | European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
| Structure-activity relationship and enzyme kinetic studies on 4-aryl-1H-1,2,3-triazoles as indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID422795 | Activity at 1.68 uM Aspergillus fumigatus FtmPT1 assessed as compound conversion rate at 1 mM after 16 hrs by HPLC analysis in presence of dimethylallyl diphosphate relative to L-tryptophan | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Substrate promiscuity of the cyclic dipeptide prenyltransferases from Aspergillus fumigatus ( section sign). |
| AID422794 | Activity at 1.68 uM Aspergillus fumigatus FtmPT1 assessed as compound conversion rate at 1 mM after 2 hrs by HPLC analysis in presence of dimethylallyl diphosphate relative to L-tryptophan | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Substrate promiscuity of the cyclic dipeptide prenyltransferases from Aspergillus fumigatus ( section sign). |
| AID731011 | Inhibition of human recombinant IDO assessed as inhibition of indoleamine 2,3-dioxygenase to kynurenine conversion after 60 mins by HPLC analysis | 2013 | Bioorganic & medicinal chemistry, Mar-01, Volume: 21, Issue:5
| Synthesis and biological evaluation of novel tryptoline derivatives as indoleamine 2,3-dioxygenase (IDO) inhibitors. |
| AID1348829 | Inhibition of human IDO1 expressed in African green monkey COS1 cells | 2018 | European journal of medicinal chemistry, Jan-01, Volume: 143 | Recent discovery of indoleamine-2,3-dioxygenase 1 inhibitors targeting cancer immunotherapy. |
| AID384942 | Inhibition of human recombinant indoleamine 2,3-dioxygenase | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine A. |
| AID1252323 | Inhibition of IDO1 (unknown origin) | 2015 | Journal of medicinal chemistry, Nov-25, Volume: 58, Issue:22
| Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway. |
| AID422792 | Activity at 1.62 uM Aspergillus fumigatus CdpNPT assessed as compound conversion rate at 1 mM after 16 hrs by HPLC analysis in presence of dimethylallyl diphosphate relative to L-tryptophan | 2009 | Journal of natural products, Jan, Volume: 72, Issue:1
| Substrate promiscuity of the cyclic dipeptide prenyltransferases from Aspergillus fumigatus ( section sign). |
| AID1798147 | Enzyme Inhibition Assay from Article 10.1021/jm800143h: \\Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine a.\\ | 2008 | Journal of medicinal chemistry, May-08, Volume: 51, Issue:9
| Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine A. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |