◎ Sugi Atlas

Atlas / Gene / IDO2

IDO2

gene
On this page

Summary

IDO2 (indoleamine 2,3-dioxygenase 2, HGNC:27269) is a protein-coding gene on chromosome 8p11.21, encoding Indoleamine 2,3-dioxygenase 2 (Q6ZQW0). Catalyzes the first and rate limiting step of the catabolism of the essential amino acid tryptophan along the kynurenine pathway.

Along with the enzymes encoded by the INDO (MIM 147435) and TDO2 (MIM 191070) genes, the enzyme encoded by the INDOL1 gene metabolizes tryptophan in the kynurenine pathway (Ball et al., 2007 [PubMed 17499941]).

Source: NCBI Gene 169355 — RefSeq curated summary.

At a glance

  • GWAS associations: 2
  • Clinical variants (ClinVar): 77 total
  • Druggable target: yes — 2 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_194294

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:27269
Approved symbolIDO2
Nameindoleamine 2,3-dioxygenase 2
Location8p11.21
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000188676
Ensembl biotypeprotein_coding
OMIM612129
Entrez169355

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 protein_coding, 1 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000343295, ENST00000418094, ENST00000502986, ENST00000868807

RefSeq mRNA: 2 — MANE Select: NM_194294 NM_001395206, NM_194294

CCDS: CCDS6114

Canonical transcript exons

ENST00000502986 — 11 exons

ExonStartEnd
ENSE000015048074000532740005378
ENSE000016500663998550839985522
ENSE000035137664001524740016392
ENSE000035299923998265239982770
ENSE000035657883998972139989838
ENSE000035996153994914939949264
ENSE000036217143997906739979186
ENSE000036648553996360839963703
ENSE000036649053998787139987970
ENSE000036714514001356540013713
ENSE000039643823993465139935218

Expression profiles

Bgee: expression breadth broad, 80 present calls, max score 80.38.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0638 / max 28.0212, expressed in 12 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter IDTPM avgSamples expressed
885940.02806
886060.01345
885950.01072
886050.00811
885960.00373

Top tissues by expression

218 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
right lobe of liverUBERON:000111480.38gold quality
liverUBERON:000210774.35gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047373.04gold quality
placentaUBERON:000198771.04gold quality
left lobe of thyroid glandUBERON:000112068.50gold quality
right lobe of thyroid glandUBERON:000111968.48gold quality
thyroid glandUBERON:000204666.61gold quality
vermiform appendixUBERON:000115464.15gold quality
spermCL:000001962.09silver quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099162.08gold quality
endometriumUBERON:000129561.11gold quality
lymph nodeUBERON:000002961.04gold quality
right testisUBERON:000453460.81gold quality
left testisUBERON:000453360.63gold quality
testisUBERON:000047359.04gold quality
caecumUBERON:000115358.94gold quality
skin of hipUBERON:000155454.93gold quality
gall bladderUBERON:000211053.55gold quality
spleenUBERON:000210653.41gold quality
rectumUBERON:000105253.40gold quality
buccal mucosa cellCL:000233653.01gold quality
mucosa of transverse colonUBERON:000499152.48gold quality
upper leg skinUBERON:000426250.64silver quality
sural nerveUBERON:001548850.26gold quality
bone marrow cellCL:000209250.20gold quality
colonic epitheliumUBERON:000039750.18gold quality
tonsilUBERON:000237250.09gold quality
monocyteCL:000057648.92silver quality
small intestine Peyer’s patchUBERON:000345448.48gold quality
skin of abdomenUBERON:000141648.32gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

ExperimentMarker?Max mean expression
E-ANND-3yes5.04

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): PTMA

miRNA regulators (miRDB)

55 targeting IDO2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4673100.0066.641490
HSA-MIR-3667-3P99.9967.171636
HSA-MIR-4482-3P99.9872.503147
HSA-MIR-569699.9872.364487
HSA-MIR-4645-5P99.9865.811284
HSA-MIR-548AN99.9770.912817
HSA-MIR-3065-5P99.9771.563281
HSA-MIR-50799.9770.111915
HSA-MIR-1250-3P99.9670.044038
HSA-MIR-365899.9673.874379
HSA-MIR-55799.9670.011640
HSA-MIR-391099.9571.132227
HSA-MIR-548E-5P99.8972.734486
HSA-MIR-4731-5P99.8967.232537
HSA-MIR-153-5P99.8973.866317
HSA-MIR-579-3P99.8671.663628
HSA-MIR-4728-5P99.8569.394718
HSA-MIR-664B-3P99.8471.653590
HSA-MIR-4799-5P99.8270.602663
HSA-MIR-6785-5P99.8268.684428
HSA-MIR-4659A-3P99.8072.624248
HSA-MIR-4659B-3P99.8072.624248
HSA-MIR-4760-5P99.8069.881619
HSA-MIR-149-3P99.7268.223963
HSA-MIR-4699-3P99.7170.153142
HSA-MIR-6883-5P99.6968.053785
HSA-MIR-806199.6369.441411
HSA-MIR-3942-3P99.5769.032854
HSA-MIR-7159-5P99.5372.122472
HSA-MIR-444199.4966.563216

Literature-anchored findings (GeneRIF, showing 37)

  • This article describes the evolutionary relationships between the INDO and INDOL1 genes. The INDOL1 protein has a distinct expression pattern compared to INDO and both have the ability to catabolise tryptophan. (PMID:17499941)
  • IDO2 encodes a novel IDO-related tryptophan catabolic enzyme that is preferentially inhibited by D-1-methyl-tryptophan (D-1MT). IDO2 may have a distinct role in immune tolerance. Two common human genetic polymorphisms ablate IDO2 enzyme activity. (PMID:17671174)
  • First study to report IDO2 expression in pancreatic ductal adenocarcinoma indicating that IDO2 genetic polymorphisms do not negate interferon-gamma-inducible protein expression. (PMID:19476837)
  • High activity of indoleamine 2,3 dioxygenase enzyme predicts disease severity and case fatality in bacteremic patients. (PMID:19487973)
  • The pro-apoptotic activity of indoleamine 2, 3-dioxygenase is responsible for its transcriptional regulation and the modulation of its pro-apoptotic activity during death receptor activation in melanoma cells. (PMID:19799997)
  • Tryptophan supplementation was able to completely restore hepatitis b virus replication in IFN-gamma- but not IFN-alpha-treated cells, which strongly argues that IDO is the primary mediator of IFN-gamma-elicited antiviral response in human hepatocytes. (PMID:21084489)
  • Data show that IDO2-specific T cells are cytotoxic effector cells that recognize and kill tumor cells. (PMID:21406395)
  • Purification and kinetic characterization of human indoleamine 2,3-dioxygenases 1 and 2 (IDO1 and IDO2) and discovery of selective IDO1 inhibitors. (PMID:21835273)
  • Indoleamine2,3-dioxygenase and tryptophanyl-tRNA synthetase may play critical roles in the immune pathogenesis of chronic kidney disease. (PMID:23651343)
  • The IDO2 is now known to catalyze the first and rate-limiting step in the catabolism of tryptophan along a relative newcomer to the kynurenine pathway field. (PMID:24105077)
  • IDO2 is expressed in both mDCs and plasmacytoid DCs and is not modulated by PGE2. IDO2 expression is constitutively, stably expressed in steady-state conditions and may contribute to the homeostatic tolerogenic capacity of DCs. (PMID:24391212)
  • Multiple-scattering (MS) analysis of EXAFS data on met-indoleamine 2,3-dioxygenase-2 (IDO2) and analysis of XANES have provided the first direct structural information about the axial donor ligands of the iron center for this recently discovered protein. (PMID:24858687)
  • Human indoleamine 2,3-dioxygenase-2 has substrate specificity and inhibition characteristics distinct from those of indoleamine 2,3-dioxygenase-1 (PMID:24875753)
  • These results demonstrate that IDO2 plays a novel role as a negative regulator of IDO1 by competing for heme-binding with IDO1. (PMID:25394548)
  • functional importance of IDO enzymes in human Crohn’s disease (PMID:25541686)
  • High IDO2 expression is associated with cervical cancer. (PMID:27106797)
  • High IDO2 expression is associated with Colorectal Cancer. (PMID:27578919)
  • This study demonstrated that IDO2 rs10109853 and rs4503083 polymorphisms are not associated with MS risk, age at onset and disease progression in Italian MS patients. (PMID:28477703)
  • Data suggest a strong association between the Indoleamine-2,3-Dioxygenase-2 (IDO2) inactivating Y359Stop single nucleotide polymorphism and an increased risk of familial pancreatic cancers when compared with the control group. (PMID:29426021)
  • The results of this study provide genetic support for IDO2 as a contributing factor in PDAC development and argue that IDO2 genotype analysis has the immediate potential to influence the PDAC care decision-making process through stratification of those patients who stand to benefit from adjuvant radiotherapy (PMID:30266763)
  • IDO expression correlates with intra-tumoral neutrophils infiltration and prognosis in the hepatocellular carcinoma patients. (PMID:30843276)
  • Genetic Polymorphisms Affecting IDO1 or IDO2 Activity Differently Associate With Aspergillosis in Humans. (PMID:31134053)
  • Elevated expression of IDO2 is associated with Chemoresistance in breast cancer. (PMID:31844921)
  • Influence of Indoleamine-2,3-Dioxygenase and Its Metabolite Kynurenine on gammadelta T Cell Cytotoxicity against Ductal Pancreatic Adenocarcinoma Cells. (PMID:32384638)
  • Indoleamine 2,3-Dioxygenase 2 Immunohistochemical Expression in Resected Human Non-small Cell Lung Cancer: A Potential New Prognostic Tool. (PMID:32536910)
  • High PD-L1/IDO-2 and PD-L2/IDO-1 Co-Expression Levels Are Associated with Worse Overall Survival in Resected Non-Small Cell Lung Cancer Patients. (PMID:33671892)
  • Methylene blue and ascorbate interfere with the accurate determination of the kinetic properties of IDO2. (PMID:33686747)
  • IDO2 rs10109853 polymorphism affects the susceptibility to multiple myeloma. (PMID:33709342)
  • Investigating the Role of Indoleamine 2,3-Dioxygenase in Acute Myeloid Leukemia: A Systematic Review. (PMID:33777052)
  • Indoleamine 2,3-dioxygenase (IDO)-1 and IDO-2 activity and severe course of COVID-19. (PMID:34859884)
  • Single-nucleotide polymorphisms and activities of indoleamine 2,3-dioxygenase isoforms, IDO1 and IDO2, in tuberculosis patients. (PMID:35045867)
  • Heterozygote Advantage of the Type II Deiodinase Thr92Ala Polymorphism on Intrahospital Mortality of COVID-19. (PMID:35137147)
  • Indoleamine 2,3-dioxygenase 2 immunohistochemical expression in medullary thyroid carcinoma: implications in prognosis and immunomodulatory effects. (PMID:36319978)
  • Regulation of IDO2 by the Aryl Hydrocarbon Receptor (AhR) in Breast Cancer. (PMID:37408267)
  • Prolonged indoleamine 2,3-dioxygenase-2 activity and associated cellular stress in post-acute sequelae of SARS-CoV-2 infection. (PMID:37506544)
  • Membrane Localization and Phosphorylation of Indoleamine 2,3-Dioxygenase 2 (IDO2) in A549 Human Lung Adenocarcinoma Cells: First Steps in Exploring Its Signaling Function. (PMID:38003426)
  • Marked IDO2 expression and activity related to autophagy and apoptosis in brain tissue of fatal tuberculous meningitis. (PMID:38460493)

Cross-species orthologs

2 orthologs

OrganismSymbolGene ID
mus_musculusIdo2ENSMUSG00000031549
rattus_norvegicusIdo2ENSRNOG00000025365

Protein

Protein identifiers

Indoleamine 2,3-dioxygenase 2 — Q6ZQW0 (reviewed: Q6ZQW0)

Alternative names: Indoleamine 2,3-dioxygenase-like protein 1, Indoleamine-pyrrole 2,3-dioxygenase-like protein 1

All UniProt accessions (1): Q6ZQW0

UniProt curated annotations — full annotation on UniProt →

Function. Catalyzes the first and rate limiting step of the catabolism of the essential amino acid tryptophan along the kynurenine pathway. Involved in immune regulation. May not play a significant role in tryptophan-related tumoral resistance.

Tissue specificity. Detected in liver, small intestine, spleen, placenta, thymus, lung, brain, kidney, and colon. Also expressed at low level in testis and thyroid. Not expressed in the majority of human tumor samples (>99%).

Activity regulation. Activity is inhibited by D-1MT (1-methyl-D-tryptophan) and MTH-trp (methylthiohydantoin-DL-tryptophan) but not L-1MT (1-methyl-L-tryptophan).

Cofactor. Binds 1 heme group per subunit.

Pathway. Amino-acid degradation; L-tryptophan degradation via kynurenine pathway; L-kynurenine from L-tryptophan: step 1/2.

Polymorphism. The variant Trp-248 (p.R248W) drastically reduces the enzymatic activity. The Del359-420 variant (p.Y359X) generates a truncated, enzymatically inactive protein. The high prevalence of these polymorphic alleles results in a non-functional IDO2 enzyme in up to 50% of Caucasians.

Miscellaneous. IDO1 and IDO2 are 2 distinct enzymes which catalyze the same reaction. IDO2 affinity for tryptophan is much lower than that of IDO1. 50 % of Caucasians harbor polymorphisms which abolish IDO2 enzymatic activity. IDO2 is expressed in human tumors in an inactive form: tryptophan degradation is entirely provided by IDO1 in these cells. IDO2 may play a role as a negative regulator of IDO1 by competing for heme-binding with IDO1. Low efficiency IDO2 enzymes have been conserved throughout vertebrate evolution, whereas higher efficiency IDO1 enzymes are dispensable in many lower vertebrate lineages. IDO1 may have arisen by gene duplication of a more ancient proto-IDO gene before the divergence of marsupial and eutherian (placental) mammals.

Similarity. Belongs to the indoleamine 2,3-dioxygenase family.

Isoforms (2)

UniProt IDNamesCanonical?
Q6ZQW0-11yes
Q6ZQW0-22

RefSeq proteins (2): NP_001382135, NP_919270* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000898Indolamine_dOaseFamily
IPR037217Trp/Indoleamine_2_3_dOase-likeHomologous_superfamily

Pfam: PF01231

Enzyme classification (BRENDA):

  • EC 1.13.11.11 — tryptophan 2,3-dioxygenase (BRENDA: 16 organisms, 15 substrates, 146 inhibitors, 17 Km, 8 kcat entries)
  • EC 1.13.11.52 — indoleamine 2,3-dioxygenase (BRENDA: 49 organisms, 208 substrates, 831 inhibitors, 203 Km, 109 kcat entries)

Substrate kinetics (BRENDA)

23 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

SubstrateKm (mM)Measurements
L-TRYPTOPHAN0.0007–62.496
D-TRYPTOPHAN0.0019–1627
L-TRYPTOPHAN0.02–1.53113
L-TRP0.02–13312
5-HYDROXY-L-TRYPTOPHAN0.017–0.6810
O20.037–11910
5-FLUORO-DL-TRYPTOPHAN0.006–1006
5-METHYL-DL-TRYPTOPHAN0.088–1.576
6-METHYL-DL-TRYPTOPHAN0.056–3.4575
D-TRP0.3–5.25
6-FLUORO-DL-TRYPTOPHAN0.186–1864
1-METHYL-L-TRYPTOPHAN0.062–0.6963
1-METHYL-D-TRYPTOPHAN0.66–0.7472
5-FLUORO-TRYPTOPHAN0.006–0.362
5-METHOXY-DL-TRYPTOPHAN0.113–0.5472

Catalyzed reactions (Rhea), 1 shown:

  • L-tryptophan + O2 = N-formyl-L-kynurenine (RHEA:24536)

UniProt features (6 total): splice variant 2, sequence variant 2, chain 1, binding site 1

Structure

Experimental structures (PDB)

11 structures.

PDBMethodResolution (Å)
9UYYX-RAY DIFFRACTION2.25
9UZ1X-RAY DIFFRACTION2.35
9UYZX-RAY DIFFRACTION2.45
9UZ0X-RAY DIFFRACTION2.45
9UZ3X-RAY DIFFRACTION2.5
9UZ4X-RAY DIFFRACTION2.5
9UZ5X-RAY DIFFRACTION2.5
21OOX-RAY DIFFRACTION2.55
9UZ2X-RAY DIFFRACTION2.55
21OKX-RAY DIFFRACTION2.6
21OMX-RAY DIFFRACTION2.68

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-Q6ZQW0-F193.250.87

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (1): 347 (proximal binding residue)

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

IDPathway
R-HSA-71240Tryptophan catabolism

MSigDB gene sets: 113 (showing top): GOBP_ALPHA_AMINO_ACID_METABOLIC_PROCESS, REACTOME_TRYPTOPHAN_CATABOLISM, GCAAGGA_MIR502, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_NUCLEOSIDE_PHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_KETONE_METABOLIC_PROCESS, GOBP_ORGANOPHOSPHATE_BIOSYNTHETIC_PROCESS, GOBP_NADPLUS_METABOLIC_PROCESS, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM4, GOBP_AROMATIC_AMINO_ACID_METABOLIC_PROCESS, ACEVEDO_LIVER_TUMOR_VS_NORMAL_ADJACENT_TISSUE_DN, GOBP_ORGANIC_ACID_CATABOLIC_PROCESS, GOBP_INDOLE_CONTAINING_COMPOUND_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_METABOLIC_PROCESS

GO Biological Process (4): immune system process (GO:0002376), obsolete L-tryptophan catabolic process to L-kynurenine (GO:0019441), ‘de novo’ NAD+ biosynthetic process from L-tryptophan (GO:0034354), L-tryptophan catabolic process (GO:0006569)

GO Molecular Function (6): L-tryptophan 2,3-dioxygenase activity (GO:0004833), heme binding (GO:0020037), indoleamine 2,3-dioxygenase activity (GO:0033754), metal ion binding (GO:0046872), oxidoreductase activity (GO:0016491), dioxygenase activity (GO:0051213)

GO Cellular Component (2): cytoplasm (GO:0005737), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-1 pathways:

CategoryPathways
Metabolism of amino acids and derivatives1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen2
cellular anatomical structure2
biological_process1
aromatic amino acid metabolic process1
NAD+ biosynthetic process1
indole-containing compound metabolic process1
L-amino acid metabolic process1
proteinogenic amino acid metabolic process1
aromatic amino acid catabolic process1
indole-containing compound catabolic process1
L-amino acid catabolic process1
proteinogenic amino acid catabolic process1
tetrapyrrole binding1
cation binding1
catalytic activity1
oxidoreductase activity1
intracellular anatomical structure1
cytoplasm1

Protein interactions and networks

STRING

1946 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
IDO2TDO2P48775956
IDO2IFNGP01579870
IDO2FOXP3Q9BZS1832
IDO2CTLA4P16410832
IDO2CD4P01730824
IDO2IL10P22301811
IDO2KMOO15229810
IDO2TNFSF18Q9UNG2797
IDO2KYNUQ16719793
IDO2TNFRSF18Q9Y5U5791
IDO2CD80P33681790
IDO2CD274Q9NZQ7769
IDO2IL2P01585749
IDO2IL17AQ16552749
IDO2TNFRSF9Q07011741

IntAct

2 interactions, top by confidence:

ABTypeScore
IDO2ATF1psi-mi:“MI:0914”(association)0.350

BioGRID (16): DPP8 (Affinity Capture-MS), NRN1 (Affinity Capture-MS), ATF1 (Affinity Capture-MS), ERICH5 (Affinity Capture-MS), ULBP2 (Affinity Capture-MS), EME1 (Affinity Capture-MS), SMARCA1 (Affinity Capture-MS), KLF12 (Affinity Capture-MS), FAM171A2 (Affinity Capture-MS), IDO2 (Two-hybrid), IDO2 (Two-hybrid), ATF1 (Affinity Capture-MS), NRN1 (Affinity Capture-MS), EME1 (Affinity Capture-MS), DPP8 (Affinity Capture-MS)

ESM2 similar proteins: A0A2I2F272, A0A6G9KIF9, A0A8I6ASZ5, D3ZBP4, D3ZND0, F1LV46, F1MH07, O00411, O70576, O75153, P0DUR8, P10937, P14902, P28776, P62044, P70261, Q01433, Q02356, Q08DJ7, Q0CG33, Q15021, Q1LXZ7, Q3SX05, Q3UYV8, Q4R5Q4, Q4R7D0, Q5R5N9, Q6ZQW0, Q7TMC8, Q7Z3D6, Q80TT2, Q8BGB8, Q8BIR2, Q8BKF1, Q8K2Z4, Q8R0V5, Q8R5K4, Q8TDZ2, Q8VDP3, Q99M76

Diamond homologs: A0A2I2F272, A0A6G9KIF9, A0A823AAW6, F1LV46, P0DUR8, P14902, P28776, P47125, P51537, Q0CG33, Q6ZQW0, Q8R0V5, Q9ERD9, Q01966

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

77 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance61
Likely benign4
Benign3

Top pathogenic / likely-pathogenic (0)

SpliceAI

2133 predictions. Top by Δscore:

VariantEffectΔscore
8:39985477:T:TAacceptor_gain1.0000
8:40013708:A:Tdonor_gain1.0000
8:40013709:AAGTG:Adonor_gain1.0000
8:40013711:GTG:Gdonor_gain1.0000
8:40013711:GTGGT:Gdonor_loss1.0000
8:40013712:TG:Tdonor_gain1.0000
8:40013713:GG:Gdonor_gain1.0000
8:40013713:GGT:Gdonor_loss1.0000
8:40013714:G:GGdonor_gain1.0000
8:40013714:G:Tdonor_loss1.0000
8:40013715:TAAG:Tdonor_loss1.0000
8:39963600:A:AGacceptor_gain0.9900
8:39963601:A:Gacceptor_gain0.9900
8:39987868:AAG:Aacceptor_gain0.9900
8:39989834:GCATG:Gdonor_gain0.9900
8:39989837:TGG:Tdonor_loss0.9900
8:39989839:G:GAdonor_loss0.9900
8:39989840:TAAGA:Tdonor_loss0.9900
8:39991083:C:Gdonor_gain0.9900
8:40013560:CTTA:Cacceptor_loss0.9900
8:40013561:TTA:Tacceptor_loss0.9900
8:40013562:TAG:Tacceptor_loss0.9900
8:40013563:A:AGacceptor_gain0.9900
8:40013563:A:Tacceptor_loss0.9900
8:40013563:AGAT:Aacceptor_gain0.9900
8:40013564:G:Aacceptor_loss0.9900
8:40013564:G:GTacceptor_gain0.9900
8:40013564:GATG:Gacceptor_gain0.9900
8:40013710:AGTG:Adonor_gain0.9900
8:40013711:GTGG:Gdonor_gain0.9900

AlphaMissense

2755 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
8:39949244:T:CF40L0.981
8:39949246:T:AF40L0.981
8:39949246:T:GF40L0.981
8:40013656:A:CS284R0.978
8:40013658:C:AS284R0.978
8:40013658:C:GS284R0.978
8:39987920:T:CF180L0.969
8:39987922:T:AF180L0.969
8:39987922:T:GF180L0.969
8:40013644:A:CS280R0.967
8:40013646:T:AS280R0.967
8:40013646:T:GS280R0.967
8:39987946:G:CE188D0.958
8:39987946:G:TE188D0.958
8:39963635:T:AW56R0.956
8:39963635:T:CW56R0.956
8:39987945:A:TE188V0.944
8:39987953:G:CA191P0.943
8:40015252:T:CF305L0.943
8:40015254:T:AF305L0.943
8:40015254:T:GF305L0.943
8:40013566:T:AW254R0.941
8:40013566:T:CW254R0.941
8:39982747:C:AN150K0.938
8:39982747:C:GN150K0.938
8:40015298:T:CF320S0.938
8:39979133:A:CS101R0.937
8:39979135:C:AS101R0.937
8:39979135:C:GS101R0.937
8:40013671:G:CA289P0.933

dbSNP variants (sampled 300 via entrez): RS1000094149 (8:39960055 C>G,T), RS1000103688 (8:39960089 T>G), RS1000104481 (8:40000280 C>T), RS1000107247 (8:39996494 T>C), RS1000152076 (8:40009901 G>A,T), RS1000193241 (8:39954952 C>A), RS1000294856 (8:40012470 A>C,G), RS1000336979 (8:39997730 C>T), RS1000371695 (8:39970671 A>G), RS1000375089 (8:39939377 T>C,G), RS1000379190 (8:40008174 G>A), RS1000442894 (8:39959805 G>A), RS1000474196 (8:39944539 T>C), RS1000574244 (8:39997805 T>C), RS1000623718 (8:39973573 A>G)

Disease associations

OMIM: gene MIM:612129 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

StudyTraitp-value
GCST012310_8Schizophrenia x sex interaction2.000000e-06
GCST012311_27Schizophrenia x sex interaction5.000000e-06

EFO canonical traits (1, from GWAS)

EFO IDTrait name
EFO:0008343sex interaction measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3627587 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 8,329 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL3545369EPACADOSTAT36,082
CHEMBL1475252TENATOPRAZOLE22,247

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: enzyme — 1.13.11.- Dioxygenases

Most potent curated ligand interactions (2 total), top 2:

LigandActionAffinityParameter
example 184 [WO2014186035]Inhibition6.0pIC50
tryptanthrin 5iInhibition5.74pIC50

Binding affinities (BindingDB)

42 measured of 105 human assays (105 total across all organisms); most potent 42 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
1,3-Dichloro-8-nitroindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-Methoxy-9-nitropyrido[3’,4’:4,5]pyrimido[1,2-a]indole-5,11-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-Nitroindolo[2,1-b]quinazolin-12(6H)-oneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-bromo-8-nitroindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-fluoro-8-methylsulfonyl-6-nitroso-5H-indolo[2,1-b]quinazolin-12-oneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
N-(2-aminoethyl)-3-chloro-6-nitroso-12-oxo-5H-indolo[2,1-b]quinazoline-8-carboxamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
N-(3-chloro-6,12-dioxoindolo[2,1-b]quinazolin-8-yl)-3-(3-methyldiazirin-3-yl)propanamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-chloro-6,12-dioxoindolo[2,1-b]quinazoline-8-sulfonamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
tert-butyl N-[2-[(3-chloro-6,12-dioxoindolo[2,1-b]quinazoline-8-carbonyl)amino]ethyl]carbamateIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-benzylsulfanyl-3-chloroindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-fluoro-12-oxo-6H-indolo[2,1-b]quinazoline-8-carboxamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
3-fluoro-8-methylsulfonyl-6H-indolo[2,1-b]quinazolin-12-oneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
N-(1,3-dichloro-6,12-dioxoindolo[2,1-b]quinazolin-8-yl)methanesulfonamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 8-fluoro-3-(1H-imidazol-4-yl)indolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 3-(aminomethyl)-8-fluoroindolo[2,1-b]quinazoline-6,12-dione Hydrochloride SaltIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of benzyl (Z)-((8-fluoro-6-(methoxyimino)-12-oxo-6,12-dihydroindolo[2,1-b]quinazolin-3-yl)methyl)carbamateIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of (Z)—N-((8-fluoro-6-(methoxyimino)-12-oxo-6,12-dihydroindolo[2,1-b]quinazolin-3-yl)methyl)acetamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 1-(aminomethyl)-8-fluoroindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
1,3-difluoro-8-methylsulfonylindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
1,2-difluoro-8-nitroindolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
1,3-difluoro-6,12-dioxoindolo[2,1-b]quinazoline-8-sulfonamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
4-bromo-1-fluoro-6,12-dioxoindolo[2,1-b]quinazoline-8-carbonitrileIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
1,3-difluoro-6,12-dioxoindolo[2,1-b]quinazoline-8-carbonitrileIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-Fluoro-4-((4-fluorobenzyl)amino)indolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
4-chloro-6,12-dioxoindolo[2,1-b]quinazoline-8-sulfonamideIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of (Z)-8-Fluoro-4-((4-fluorophenyl)amino)-6-(hydroxyimino)indolo[2,1-b]quinazolin-12(6H)-oneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-fluoro-4-[(4-fluorophenyl)methoxy]indolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-fluoro-4-(4-fluoroanilino)indolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of (Z)-8-fluoro-6-(methoxyimino)-2-((pyridin-2-ylamino)methyl)indolo[2,1-b]quinazolin-12(6H)-oneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of (Z)-2-((dimethylamino)methyl)-8-fluoro-6-(methoxyimino)indolo[2,1-b]quinazolin-12(6H)-one Trifluoroacetate SaltIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 8-fluoro-2-((pyridin-2-ylamino)methyl)indolo[2,1-b]quinazoline-6,12-dioneIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 1-((8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazolin-2-yl)methyl)guanidineIC5020 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
1-Bromo-8-nitroindolo[2,1-b]quinazoline-6,12-dioneIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
N-(2-aminoethyl)-3-chloro-6-nitroso-12-oxo-5H-indolo[2,1-b]quinazoline-8-carboxamideIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
(6E)-8-fluoro-6-methoxyimino-3-[(4-methylpiperazin-1-yl)methyl]indolo[2,1-b]quinazolin-12-oneIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-(Benzylthio)-4-((4-fluorophenyl)amino)indolo[2,1-b]quinazoline-6,12-dioneIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of (Z)-8-Fluoro-4-((4-fluorophenyl)amino)-6-(methoxyimino)indolo[2,1-b]quinazolin-12(6H)-oneIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
8-benzylsulfanyl-2-[(dimethylamino)methyl]indolo[2,1-b]quinazoline-6,12-dioneIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 8-fluoro-6-hydroxy-6-methyl-12-oxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carbonitrileIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF
Synthesis of 8-fluoro-6,12-dioxo-6,12-dihydroindolo[2,1-b]quinazoline-2-carboxylic AcidIC5065 nMUS-20250171452: TRYPTANTHRIN DERIVATIVES AND USES THEREOF

ChEMBL bioactivities

59 potent at pChembl≥5 of 129 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
6.95IC50112nMCHEMBL5219888
6.87IC50134nMCHEMBL5220224
6.84IC50144nMCHEMBL5091825
6.55IC50280nMCHEMBL4472697
6.51IC50310nMCHEMBL4791168
6.44IC50362nMCHEMBL5085580
6.41IC50387nMCHEMBL5221035
6.35IC50450nMCHEMBL432537
6.35IC50446nMCHEMBL432537
6.31IC50490nMCHEMBL4514196
6.24IC50575nMCHEMBL5221037
6.23IC50590nMCHEMBL4436582
6.20IC50630nMEPACADOSTAT
6.16IC50689nMCHEMBL5082481
6.15IC50710nMEPACADOSTAT
6.14IC50726nMCHEMBL5090441
6.10IC50794nMCHEMBL5092513
6.08IC50830nMCHEMBL5091241
6.06IC50865nMCHEMBL5091415
6.03IC50930nMCHEMBL5091243
6.02IC50958nMCHEMBL5093816
6.02IC50947nMCHEMBL5091590
6.02IC50958nMCHEMBL5084150
6.01Ki970nMCHEMBL432537
5.97IC501081nMCHEMBL5078912
5.93IC501174nMCHEMBL5078101
5.93IC501171nMCHEMBL5088729
5.92IC501200nMCHEMBL1098875
5.91IC501230nMCHEMBL1098875
5.75IC501800nMCHEMBL432537
5.75IC501800nMTENATOPRAZOLE
5.73IC501870nMCHEMBL432537
5.73IC501874nMCHEMBL5084767
5.71Ki1960nMCHEMBL4436480
5.50IC503200nMCHEMBL72165
5.49IC503220nMCHEMBL72165
5.46Ki3500nMCHEMBL1098875
5.46Ki3510nMCHEMBL1098875
5.45IC503580nMCHEMBL4436480
5.42IC503810nMCHEMBL4452150
5.37Ki4320nMCHEMBL4452150
5.30IC505000nMTRYPTANTHRIN
5.30IC505010nMTRYPTANTHRIN
5.25Ki5600nMCHEMBL72165
5.25Ki5620nMCHEMBL72165
5.21Ki6110nMCHEMBL4577825
5.20Ki6320nMCHEMBL4437046
5.12IC507600nMCHEMBL1098875
5.12IC507680nMCHEMBL1098875
5.09IC508200nMCHEMBL3087009

PubChem BioAssay actives

48 with measured affinity, of 277 total; 35 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
N-[[1-[2-[[4-[N’-[(3-bromophenyl)methyl]-N-hydroxycarbamimidoyl]-1,2,5-oxadiazol-3-yl]amino]ethyl]triazol-4-yl]methyl]pyridine-2-carboxamide1916992: Inhibition of human IDO2ic500.1120uM
N-[[1-[2-[[4-[N’-(3-bromo-4-fluorophenyl)-N-hydroxycarbamimidoyl]-1,2,5-oxadiazol-3-yl]amino]ethyl]triazol-4-yl]methyl]-1H-pyrrole-2-carboxamide1916992: Inhibition of human IDO2ic500.1340uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(2-hydroxyethoxymethyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.1440uM
N’-(3-bromo-4-fluorophenyl)-4-[2-[[ethoxy(ethyl)phosphoryl]amino]ethylamino]-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide1609232: Inhibition of N-terminal His-tagged human IDO2 expressed in Escherichia coli expression systemic500.2800uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[3-[[methoxy(methyl)phosphoryl]amino]propylamino]-1,2,5-oxadiazole-3-carboximidamide1728731: Inhibition of N-terminal 6His-tagged recombinant human IDO2 (15 to 420 residues) expressed in Escherichia coli using L-Trp as substrate by UV absorbance methodic500.3100uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(1-hydroxyethyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.3620uM
N-[[1-[2-[[4-[N’-(3-bromo-4-fluorophenyl)-N-hydroxycarbamimidoyl]-1,2,5-oxadiazol-3-yl]amino]ethyl]triazol-4-yl]methyl]pyridine-2-carboxamide1916992: Inhibition of human IDO2ic500.3870uM
8-nitroindolo[2,1-b]quinazoline-6,12-dione1332708: 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 spectrophotometryic500.4500uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[[methoxy(methyl)phosphoryl]amino]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1609232: Inhibition of N-terminal His-tagged human IDO2 expressed in Escherichia coli expression systemic500.4900uM
N-[[1-[2-[[4-[N’-(3-bromophenyl)-N-hydroxycarbamimidoyl]-1,2,5-oxadiazol-3-yl]amino]ethyl]triazol-4-yl]methyl]pyridine-2-carboxamide1916992: Inhibition of human IDO2ic500.5750uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[4-[[methoxy(methyl)phosphoryl]amino]butylamino]-1,2,5-oxadiazole-3-carboximidamide1609232: Inhibition of N-terminal His-tagged human IDO2 expressed in Escherichia coli expression systemic500.5900uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-(sulfamoylamino)ethylamino]-1,2,5-oxadiazole-3-carboximidamide2032194: Inhibition of IDO2 (unknown origin) using D-Trp as substrate incubated for 1 hric500.6300uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(2-hydroxy-4-methylpentan-2-yl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.6890uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(2-hydroxypropan-2-yl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.7260uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(hydroxymethyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.7940uM
N’-(3-bromo-4-fluorophenyl)-4-[2-(4-butyltriazol-1-yl)ethylamino]-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.8300uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(1-hydroxycyclohexyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.8650uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-[1-(2-hydroxyethoxy)ethyl]triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.9300uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(1-hydroxypropyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.9470uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(2-hydroxybutan-2-yl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.9580uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(3-hydroxypropyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic500.9580uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(4-hydroxybutyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic501.0810uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-[2-(2-hydroxyethoxy)propan-2-yl]triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic501.1710uM
N’-(3-bromo-4-fluorophenyl)-N-hydroxy-4-[2-[4-(2-hydroxyethyl)triazol-1-yl]ethylamino]-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic501.1740uM
8-fluoroindolo[2,1-b]quinazoline-6,12-dione1332708: 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 spectrophotometryic501.2000uM
5-methoxy-2-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methylsulfinyl]-1H-imidazo[4,5-b]pyridine1917028: Inhibition of IDO2 (unknown origin)ic501.8000uM
N’-(3-bromo-4-fluorophenyl)-4-[2-(4-tert-butyltriazol-1-yl)ethylamino]-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide1833933: Inhibition of IDO2 (unknown origin) assessed as reduction in kynurenine formation using L-tryptophan as substrate by methylene blue reagent based assayic501.8740uM
8-fluoro-2-(piperazin-1-ylmethyl)indolo[2,1-b]quinazoline-6,12-dione1558441: Uncompetitive inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysiski1.9600uM
8-bromoindolo[2,1-b]quinazoline-6,12-dione1332708: 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 spectrophotometryic503.2000uM
2-[(dimethylamino)methyl]-8-fluoroindolo[2,1-b]quinazoline-6,12-dione1558435: Inhibition of human IDO2 transfected in human U87MG cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated with for 6 hrsic503.8100uM
indolo[2,1-b]quinazoline-6,12-dione1332708: 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 spectrophotometryic505.0000uM
tert-butyl 4-[(8-fluoro-6,12-dioxoindolo[2,1-b]quinazolin-2-yl)methyl]piperazine-1-carboxylate1558441: Uncompetitive inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysiski6.1100uM
8-fluoro-2-[(4-methylpiperazin-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione1558440: Mixed competitive inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysiski6.3200uM
2,8-difluoroindolo[2,1-b]quinazoline-6,12-dione1332708: 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 spectrophotometryic508.2000uM
2-[(4-methylpiperazin-1-yl)methyl]indolo[2,1-b]quinazoline-6,12-dione1558442: Mixed uncompetitive inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysiski8.8500uM

CTD chemical–gene interactions

15 total (human), top 15 by PubMed support.

ChemicalActions (top 5)PubMed papers
Benzo(a)pyreneaffects methylation2
Lipopolysaccharidesincreases expression, affects response to substance, affects cotreatment2
Tetrachlorodibenzodioxindecreases reaction, increases expression2
salinomycindecreases expression1
S-(1,2-dichlorovinyl)cysteineaffects response to substance, increases expression, affects cotreatment1
indeno(1,2,3-cd)pyreneincreases expression1
3’-methoxy-4’-nitroflavonedecreases reaction, increases expression1
abrineincreases expression1
CL 075increases expression1
(+)-JQ1 compounddecreases expression1
Poly I-Cincreases expression1
Valproic Acidincreases methylation1
Antirheumatic Agentsdecreases expression1
Okadaic Aciddecreases expression1
Permethrinincreases expression1

ChEMBL screening assays

46 unique, capped per target: 46 binding

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL3630806BindingInhibition of human IDO2Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway. — J Med Chem

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 81

This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot