epacadostat [Ligand Id: 8221] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL3545369 (Epacadostat, INCB-024360, INCB024360)
There should be some charts here, you may need to enable JavaScript!
  • indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902]
There should be some charts here, you may need to enable JavaScript!
  • indoleamine 2,3-dioxygenase 1 in Human [GtoPdb: 2829] [UniProtKB: P14902]
  • indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776]
There should be some charts here, you may need to enable JavaScript!
  • indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Human [ChEMBL: CHEMBL3627587] [GtoPdb: 3019] [UniProtKB: Q6ZQW0]
  • indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5]
There should be some charts here, you may need to enable JavaScript!
  • tryptophan 2,3-dioxygenase/Tryptophan 2,3-dioxygenase in Human [ChEMBL: CHEMBL2140] [GtoPdb: 2887] [UniProtKB: P48775]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 4.4 pIC50 >40000 nM IC50 Eur J Med Chem (2019) 179: 38-55 [PMID:31233921]
ChEMBL Inhibition of human ERG by fluorescence polarization assay B 4.44 pIC50 >36000 nM IC50 J Med Chem (2021) 64: 11302-11329 [PMID:34292726]
indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902]
ChEMBL Binding affinity to NT650-NHS fluorophore-labeled recombinant human N-terminal His-tagged IDO1 expressed in Escherichia coli measured after 10 mins by microscale thermophoresis assay B 5.46 pKd 3460 nM Kd J Med Chem (2020) 63: 3047-3065 [PMID:32150677]
ChEMBL Enzyme Assay: Human indoleamine 2,3-dioxygenasae (IDO) with an N-terminal His tag was expressed in E. coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N′-formylkynurenine. The assays were performed at room temperature as described in the literature using 95 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 5 μM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates were recorded by continuously following the absorbance increase at 321 nm due to the formation of N′-formlylkynurenine (See: Sono, M., et al., 1980, J. Biol. Chem. 255, 1339-1345). B 6.7 pIC50 <200 nM IC50 US-9320732-B2. 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase (2016)
ChEMBL Inhibition of IDO1 in IFN-gamma/LPS-stimulated human whole blood assessed as decrease in kynurenine levels preincubated for 15 mins followed by IFN-gamma/LPS stimulation for overnight by LC/MS/MS analysis B 6.9 pIC50 125 nM IC50 ACS Med Chem Lett (2017) 8: 486-491 [PMID:28523098]
ChEMBL Inhibition of recombinant human IDO1 expressed in Escherichia coli B 7.01 pIC50 97 nM IC50 Bioorg Med Chem Lett (2020) 30: 126901-126901 [PMID:31882299]
ChEMBL Inhibition of recombinant human IDO1 B 7.03 pIC50 93 nM IC50 Bioorg Med Chem Lett (2021) 52: 128373-128373 [PMID:34560264]
ChEMBL Inhibition of IDO1 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assay B 7.04 pIC50 91 nM IC50 J Med Chem (2021) 64: 17950-17968 [PMID:34854662]
ChEMBL Inhibition of IDO1 (unknown origin) B 7.05 pIC50 90 nM IC50 Bioorg Med Chem Lett (2020) 30: 127159-127159 [PMID:32247733]
ChEMBL Inhibition of recombinant human IDO1 assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 30 mins by microplate reader analysis B 7.06 pIC50 87.4 nM IC50 Eur J Med Chem (2020) 189: 112059-112059 [PMID:31981851]
ChEMBL Inhibition of recombinant human IDO1 assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate and measured after 15 mins B 7.1 pIC50 80 nM IC50 Eur J Med Chem (2022) 235: 114294-114294 [PMID:35358772]
ChEMBL Inhibition of recombinant human GST-tagged IDO1 (1 to 404 residues) using D-Tryptophan as substrate B 7.11 pIC50 77.8 nM IC50 ACS Med Chem Lett (2018) 9: 312-317 [PMID:29670692]
ChEMBL Inhibition of human recombinant IDO1 assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate preincubated for 30 mins followed by substrate addition and measured after 10 mins by SpectraMax microplate reader analysis B 7.11 pIC50 77.8 nM IC50 J Med Chem (2023) 66: 1027-1047 [PMID:36595482]
ChEMBL Inhibition of human recombinant IDO1 assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate preincubated for 30 mins followed by substrate addition and measured after 20 mins by SpectraMax microplate reader analysis B 7.12 pIC50 75.9 nM IC50 Eur J Med Chem (2023) 250: 115217-115217 [PMID:36842272]
ChEMBL Inhibition of IDO1 (unknown origin) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate incubated for 30 mins by microplate spectrophotometry analysis B 7.12 pIC50 75 nM IC50 Eur J Med Chem (2020) 207: 112703-112703 [PMID:32871341]
ChEMBL Inhibition of human N-terminal His-tagged IDO1 expressed in Escherichia coli using D-Trp as substrate B 7.14 pIC50 73 nM IC50 ACS Med Chem Lett (2017) 8: 486-491 [PMID:28523098]
ChEMBL Inhibition of IDO1 (unknown origin) B 7.14 pIC50 73 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL Inhibition of IDO1 (unknown origin) B 7.14 pIC50 73 nM IC50 Eur J Med Chem (2022) 238: 114524-114524 [PMID:35696861]
ChEMBL Inhibition of human N-terminal GST-tagged IDO1 expressed in Escherichia coli Rosetta(DE3) pLysS using L-tryptophan as substrate measured after 1 hr by fluorescence assay B 7.14 pIC50 73 nM IC50 ACS Med Chem Lett (2020) 11: 179-187 [PMID:32071686]
ChEMBL Inhibition of IDO1 (unknown origin) B 7.14 pIC50 73 nM IC50 Eur J Med Chem (2022) 227: 113967-113967 [PMID:34752953]
ChEMBL Inhibition of recombinant N-terminal His-tagged human IDO1 expressed in Escherichia coli assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate B 7.14 pIC50 72 nM IC50 Eur J Med Chem (2019) 182: 111629-111629 [PMID:31445231]
ChEMBL Inhibition of IDO1 (unknown origin) B 7.14 pIC50 72 nM IC50 J Med Chem (2015) 58: 8762-8782 [PMID:26207924]
ChEMBL Inhibition of human IDO1 B 7.14 pIC50 72 nM IC50 Bioorg Med Chem (2019) 27: 1087-1098 [PMID:30773421]
ChEMBL Inhibition of IDO1 (unknown origin) using D-tryptophan as substrate by spectrophotometric analysis B 7.14 pIC50 72 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of N-terminal His-tagged human recombinant IDO1 expressed in Escherichia coli using D-tryptophan as substrate by methylene blue/ascorbate assay B 7.14 pIC50 72 nM IC50 J Med Chem (2015) 58: 9421-9437 [PMID:25970480]
ChEMBL Inhibition of N-terminal His-tagged human IDO1 expressed in Escherichia coli assessed as reduction in conversion of D-tryptophan to N-formyl kynurenine by methylene blue dye assay B 7.14 pIC50 71.8 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of human IDO1 B 7.14 pIC50 71.8 nM IC50 J Med Chem (2016) 59: 9760-9773 [PMID:27690429]
ChEMBL Inhibition of human IDO1 incubated for 60 mins in presence of L-tryptophan by HPLC analysis B 7.14 pIC50 71.8 nM IC50 J Med Chem (2016) 59: 9760-9773 [PMID:27690429]
ChEMBL Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2019) 162: 455-464 [PMID:30469041]
ChEMBL Inhibition of recombinant human IDO1 using L-Trp as substrate incubated for 1 hr B 7.15 pIC50 70 nM IC50 Eur J Med Chem (2023) 245: 114860-114860 [PMID:36370550]
ChEMBL 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 B 7.15 pIC50 70 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
GtoPdb - - 7.17 pIC50 67 nM IC50 J Med Chem (2009) 52: 7364-7 [PMID:19507862]
ChEMBL Inhibition of recombinant human N-terminus IDO1 expressed in Escherichia coli assessed as N-formylkynurenine formation using L-tryptophan as substrate measured after 180 mins by UV absorbance based assay B 7.17 pIC50 67 nM IC50 Bioorg Med Chem (2016) 24: 6194-6205 [PMID:27769672]
ChEMBL Inhibition of human IDO1 expressed in Escherichia coli using L-tryptophan as substrate after 1 hr by UV absorption analysis B 7.17 pIC50 67 nM IC50 Bioorg Med Chem (2019) 27: 1087-1098 [PMID:30773421]
ChEMBL Inhibition of IDO1 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 60 mins by fluorescence based assay B 7.18 pIC50 66 nM IC50 Bioorg Med Chem Lett (2020) 30: 127038-127038 [PMID:32088128]
ChEMBL Inhibition of human IDO1 using D-Trp as substrate B 7.19 pIC50 64.6 nM IC50 Eur J Med Chem (2018) 157: 423-436 [PMID:30103191]
ChEMBL Inhibition of recombinant human IDO1 assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 45 mins by microplate reader assay B 7.24 pIC50 58 nM IC50 Eur J Med Chem (2020) 188: 111985-111985 [PMID:31881488]
ChEMBL Inhibition of human IDO1 (12 to 403 aa) expressed in Escherichia coli Transetta (DE3) by nanodrop 2000c spectrophotometric analysis B 7.25 pIC50 56 nM IC50 J Med Chem (2021) 64: 8303-8332 [PMID:34110158]
ChEMBL Inhibition of human recombinant IDO1 measured after 60 mins by fluorescence based analysis B 7.32 pIC50 48 nM IC50 Eur J Med Chem (2023) 254: 115349-115349 [PMID:37060754]
ChEMBL Inhibition of recombinant human IDO1 expressed in Escherichia coli BL21 (DE3) using tryptophan as substrate B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2021) 213: 113163-113163 [PMID:33482599]
ChEMBL Inhibition of human N-terminal His-tagged IDO1 expressed in Escherichia coli assessed as formation of N'-formyl-kynurenine using D-tryptophan as a substrate by methylene blue based assay B 7.34 pIC50 46 nM IC50 Eur J Med Chem (2021) 223: 113631-113631 [PMID:34147748]
ChEMBL Inhibition of recombinant human IDO1 expressed in Escherichia coli BL21 cells using L-tryptophan as substrate incubated for 30 mins by methylene blue dye based microplate reader analysis B 7.39 pIC50 40.9 nM IC50 Eur J Med Chem (2019) 179: 38-55 [PMID:31233921]
ChEMBL Inhibition of recombinant human IDO1 expressed in Escherichia coli EC538 assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate incubated for 30 mins by methylene blue reagent based concurrent assay B 7.4 pIC50 40 nM IC50 Bioorg Med Chem (2021) 39: 116160-116160 [PMID:33901770]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells assessed as reduction in kynurenine formation measured after 48 hrs by spectrophotometry B 7.45 pIC50 35.76 nM IC50 J Med Chem (2021) 64: 17950-17968 [PMID:34854662]
ChEMBL Inhibition of recombinant human IDO1 expressed in Escherichia coli EC538 assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate incubated for 30 mins by methylene blue reagent based assay B 7.52 pIC50 30 nM IC50 Bioorg Med Chem (2021) 39: 116160-116160 [PMID:33901770]
ChEMBL Inhibition of human IDO1 expressed in Escherichia coli Rosetta using tryptophan as substrate incubated for 1 hr by methylene blue based assay B 7.59 pIC50 26 nM IC50 ACS Med Chem Lett (2021) 12: 195-201 [PMID:33603965]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human THP1 cells assessed as reduction in kynurenine productio by spectrophotometric analysis B 7.64 pIC50 23 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of IDO1 in IFN-gamma-induced human HeLa cells assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate preincubated for 24 hrs followed by substrate addition and measured after 30 mins by SpectraMax microplate reader analysis B 7.69 pIC50 20.6 nM IC50 Eur J Med Chem (2023) 250: 115217-115217 [PMID:36842272]
ChEMBL Inhibition of IDO1 in human HeLa cells B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2020) 30: 127159-127159 [PMID:32247733]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate by absorbance based analysis B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2022) 235: 114294-114294 [PMID:35358772]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells using tryptophan as substrate measured after 48 hrs B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2021) 213: 113163-113163 [PMID:33482599]
ChEMBL Inhibition of IDO1 in IFN-gamma treated human HeLa cells incubated for 48 hrs by absorbance based analysis B 7.72 pIC50 19 nM IC50 Eur J Med Chem (2023) 254: 115349-115349 [PMID:37060754]
ChEMBL Inhibition of human recombinant IDO1 in human HeLa cells assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate preincubated for 24 hrs followed by substrate addition and measured after 30 mins B 7.73 pIC50 18.6 nM IC50 J Med Chem (2023) 66: 1027-1047 [PMID:36595482]
ChEMBL Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs B 7.8 pIC50 16 nM IC50 Eur J Med Chem (2019) 184: 111750-111750 [PMID:31610376]
ChEMBL Inhibition of human IDO1 expressed in HEK293/MSR cells assessed as reduction in kynurenine production incubated fro 2 days B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of IDO1 in IFNgamma and LPS-stimulated human dendritic cells co-cultured with human T cells assessed as inhibition of T-cell proliferation in presence of soluble anti-CD3 antibody and human recombinant IL-2 incubated for 2 days B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of IDO1 in human HeLa cells B 7.9 pIC50 12.6 nM IC50 Eur J Med Chem (2022) 238: 114524-114524 [PMID:35696861]
ChEMBL Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis B 7.9 pIC50 12.6 nM IC50 Eur J Med Chem (2019) 179: 38-55 [PMID:31233921]
ChEMBL Inhibition of IDO1 in human HeLa cells assessed as production of N-formylkynurenine using tryptophan as substrate in presence of inactivated fetal bovine serum B 7.9 pIC50 12.5 nM IC50 Bioorg Med Chem Lett (2021) 49: 128314-128314 [PMID:34391891]
ChEMBL Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay B 7.9 pIC50 12.5 nM IC50 ACS Med Chem Lett (2020) 11: 1548-1554 [PMID:32832022]
ChEMBL Inhibition of human IDO1 using L-tryptophan as substrate assessed as reduction in N-formyl kynurenine formation by UV-visible spectroscopic analysis B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2023) 96: 129532-129532 [PMID:37866714]
ChEMBL Inhibition of IDO1 in human HeLa cells using tryptophan as substrate incubated for 24 hrs by RFMS assay B 7.96 pIC50 11 nM IC50 J Med Chem (2021) 64: 11302-11329 [PMID:34292726]
ChEMBL Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control B 7.99 pIC50 10.3 nM IC50 Bioorg Med Chem (2019) 27: 1605-1618 [PMID:30858027]
ChEMBL Inhibition of human recombinant IDO1 assessed as reduction in kynurenine production using L-tryptophan incubated for 60 mins by Ehrlich's reagent based assay B 8 pIC50 10 nM IC50 Bioorg Med Chem Lett (2018) 28: 651-657 [PMID:29398544]
ChEMBL Inhibition of human IDO1 B 8 pIC50 10 nM IC50 Eur J Med Chem (2022) 238: 114524-114524 [PMID:35696861]
ChEMBL Inhibition of human IDO1 B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 17950-17968 [PMID:34854662]
ChEMBL Inhibition of human IDO1 B 8 pIC50 10 nM IC50 J Med Chem (2021) 64: 8303-8332 [PMID:34110158]
ChEMBL Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs B 8 pIC50 10 nM IC50 Eur J Med Chem (2019) 182: 111629-111629 [PMID:31445231]
ChEMBL Inhibition of human IDO1 expressed in HEK293T cells assessed as reduction in N-formylkynurenine production incubated for 12 hrs by microplate reader analysis B 8.02 pIC50 9.63 nM IC50 Eur J Med Chem (2020) 189: 112059-112059 [PMID:31981851]
ChEMBL Inhibition of IDO1 in interferon-gamma-induced human SKOV3 cells assessed as N-formylkynurenine formation using L-tryptophan as substrate measured after 24 hrs by fluorescence assay B 8.1 pIC50 7.9 nM IC50 ACS Med Chem Lett (2020) 11: 179-187 [PMID:32071686]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human A375 cells assessed as reduction in L-Kyn level measured after 48 hrs by HPLC analysis B 8.11 pIC50 7.7 nM IC50 J Med Chem (2020) 63: 3047-3065 [PMID:32150677]
ChEMBL Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs B 8.13 pIC50 7.4 nM IC50 ACS Med Chem Lett (2017) 8: 486-491 [PMID:28523098]
ChEMBL Inhibition of IDO1 in human HeLa cells B 8.13 pIC50 7.4 nM IC50 Eur J Med Chem (2022) 227: 113967-113967 [PMID:34752953]
ChEMBL Inhibition of IDO1 in recombinant human IFNgamma and LPS-induced human HeLa assessed as reduction in kynurenine production incubated for 2 days by spectrophotometric analysis B 8.15 pIC50 7.1 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay B 8.15 pIC50 7.1 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis B 8.15 pIC50 7.1 nM IC50 J Med Chem (2015) 58: 9421-9437 [PMID:25970480]
ChEMBL Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs B 8.15 pIC50 7 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs B 8.25 pIC50 5.6 nM IC50 Bioorg Med Chem (2019) 27: 1605-1618 [PMID:30858027]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human HeLa cells using L-tryptophan as substrate measured after 48 hrs B 8.3 pIC50 5 nM IC50 ACS Med Chem Lett (2021) 12: 195-201 [PMID:33603965]
ChEMBL Inhibition of recombinant human His-tagged IDO1 (Ala2 to Gly403 residues) expressed in Escherichia coli using tryptophan as substrate preincubated for 10 mins followed by substrate addition and measured after 1 hr by RFMS assay B 8.46 pIC50 3.5 nM IC50 J Med Chem (2021) 64: 11302-11329 [PMID:34292726]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated human OCI-AML2 cells assessed as reduction in kynurenine production B 8.47 pIC50 3.4 nM IC50 Eur J Med Chem (2018) 143: 656-669 [PMID:29220788]
ChEMBL Inhibition of IDO1 in human HeLa cells using L-Tryptophan as substrate incubated for 24 hrs by microplate reader analysis B 4.27 pEC50 53920 nM EC50 Eur J Med Chem (2023) 245: 114860-114860 [PMID:36370550]
ChEMBL Inhibition of IDO1 in human HCT-116 cells using L-Tryptophan as substrate incubated for 24 hrs by microplate reader analysis B 4.29 pEC50 50750 nM EC50 Eur J Med Chem (2023) 245: 114860-114860 [PMID:36370550]
ChEMBL Inhibition of IDO1 in IFN-gamma induced overexpressing human HeLa cells B 7.1 pEC50 80 nM EC50 J Med Chem (2021) 64: 8303-8332 [PMID:34110158]
ChEMBL Inhibition of IFNgamma-stimulated IDO1 in human HeLa cells B 7.89 pEC50 13 nM EC50 Bioorg Med Chem Lett (2020) 30: 126901-126901 [PMID:31882299]
ChEMBL Inhibition of human IDO1 expressed in HEK293 cells assessed as reduction in kynurenine production after 30 mins B 8.06 pEC50 8.74 nM EC50 ACS Med Chem Lett (2018) 9: 131-136 [PMID:29456801]
ChEMBL Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry B 8.1 pEC50 8 nM EC50 Bioorg Med Chem Lett (2020) 30: 127038-127038 [PMID:32088128]
indoleamine 2,3-dioxygenase 1 in Human [GtoPdb: 2829] [UniProtKB: P14902]
GtoPdb - - 7.17 pIC50 67 nM IC50 J Med Chem (2009) 52: 7364-7 [PMID:19507862]
indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776]
ChEMBL Inhibition of IDO1 in mouse Panc02 cells assessed as reduction in NFK level incubated for 48 hrs by RFMS analysis B 7.13 pIC50 74 nM IC50 J Med Chem (2021) 64: 11302-11329 [PMID:34292726]
ChEMBL Inhibition of IDO1 in IFNgamma-stimulated mouse Panc02 cells incubated for 48 hrs by RFMS method B 7.13 pIC50 74 nM IC50 J Med Chem (2021) 64: 11302-11329 [PMID:34292726]
indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3627587] [GtoPdb: 3019] [UniProtKB: Q6ZQW0]
ChEMBL Inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) 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 dye based microplate reader analysis B 4.99 pIC50 10340 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of N-terminal His-tagged human IDO2 expressed in Escherichia coli expression system B 6.15 pIC50 710 nM IC50 Eur J Med Chem (2019) 182: 111629-111629 [PMID:31445231]
ChEMBL Inhibition of IDO2 (unknown origin) using D-Trp as substrate incubated for 1 hr B 6.2 pIC50 630 nM IC50 Eur J Med Chem (2023) 245: 114860-114860 [PMID:36370550]
indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5]
ChEMBL Inhibition of mouse IDO2 expressed in human T-REx cells using L-tryptophan as substrate after 20 hrs B 4.72 pIC50 18900 nM IC50 Eur J Med Chem (2019) 162: 455-464 [PMID:30469041]
tryptophan 2,3-dioxygenase/Tryptophan 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2140] [GtoPdb: 2887] [UniProtKB: P48775]
ChEMBL 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 B 4.66 pKi 21700 nM Ki J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Uncompetitive inhibition of recombinant full length C-terminal His-tagged human TDO expressed in Escherichia coli using L-Trp as substrate after 30 mins by Dixon plot analysis B 4.66 pKi 21700 nM Ki Eur J Med Chem (2018) 160: 133-145 [PMID:30321802]
ChEMBL Inhibition of human TDO expressed in Escherichia coli Rosetta using tryptophan as substrate incubated for 1 hr by methylene blue based assay B 4 pIC50 >100000 nM IC50 ACS Med Chem Lett (2021) 12: 195-201 [PMID:33603965]
ChEMBL Inhibition of recombinant full length C-terminal His-tagged human TDO expressed in Escherichia coli using L-Trp as substrate after 30 mins B 4.19 pIC50 64500 nM IC50 Eur J Med Chem (2018) 160: 133-145 [PMID:30321802]
ChEMBL 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 B 4.19 pIC50 64500 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of human TDO expressed in human T-REx cells using L-tryptophan as substrate after 20 hrs B 4.6 pIC50 25200 nM IC50 Eur J Med Chem (2019) 162: 455-464 [PMID:30469041]
ChEMBL Inhibition of recombinant human TDO assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate and measured after 15 mins B 4.79 pIC50 16100 nM IC50 Eur J Med Chem (2022) 235: 114294-114294 [PMID:35358772]
ChEMBL Inhibition of TDO in human HEK293 cells assessed as reduction in kynurenine formation using L-tryptophan as substrate by absorbance based analysis B 4.98 pIC50 10400 nM IC50 Eur J Med Chem (2022) 235: 114294-114294 [PMID:35358772]
ChEMBL Inhibition of TDO (unknown origin) B 5 pIC50 >10000 nM IC50 ACS Med Chem Lett (2020) 11: 541-549 [PMID:32292562]
ChEMBL Inhibition of TDO (unknown origin) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate incubated for 30 mins microplate spectrophotometry analysis B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2020) 207: 112703-112703 [PMID:32871341]
ChEMBL Inhibition of N-terminal His-tagged human TDO expressed in Escherichia coli expression system B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2019) 182: 111629-111629 [PMID:31445231]
ChEMBL Inhibition of human TDO B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 8303-8332 [PMID:34110158]
ChEMBL Inhibition of human TDO (19 to 388 aa) expressed in Escherichia coli Transetta (DE3) by nanodrop 2000c spectrophotometric analysis B 5.11 pIC50 7770 nM IC50 J Med Chem (2021) 64: 8303-8332 [PMID:34110158]
ChEMBL Inhibition of recombinant human TDO2 expressed in Escherichia coli BL21 (DE3) assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate incubated for 30 mins by methylene blue reagent based concurrent assay B 5.46 pIC50 3430 nM IC50 Bioorg Med Chem (2021) 39: 116160-116160 [PMID:33901770]
ChEMBL Inhibition of recombinant human TDO2 expressed in Escherichia coli BL21 (DE3) assessed as reduction in N-formylkynurenine formation using L-tryptophan as substrate incubated for 30 mins by methylene blue reagent based assay B 5.67 pIC50 2120 nM IC50 Bioorg Med Chem (2021) 39: 116160-116160 [PMID:33901770]
ChEMBL Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs B 6.59 pIC50 260 nM IC50 J Med Chem (2019) 62: 9161-9174 [PMID:31580660]
ChEMBL Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs B 6.59 pIC50 260 nM IC50 Eur J Med Chem (2018) 160: 133-145 [PMID:30321802]
ChEMBL Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs B 6.62 pIC50 242 nM IC50 Eur J Med Chem (2018) 160: 133-145 [PMID:30321802]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]