MPO

Summary

MPO (myeloperoxidase, HGNC:7218) is a protein-coding gene on chromosome 17q22, encoding Myeloperoxidase (P05164). Part of the host defense system of polymorphonuclear leukocytes.

Myeloperoxidase (MPO) is a heme protein synthesized during myeloid differentiation that constitutes the major component of neutrophil azurophilic granules. Produced as a single chain precursor, myeloperoxidase is subsequently cleaved into a light and heavy chain. The mature myeloperoxidase is a tetramer composed of 2 light chains and 2 heavy chains. This enzyme produces hypohalous acids central to the microbicidal activity of neutrophils.

Source: NCBI Gene 4353 — RefSeq curated summary.

At a glance

• Gene–disease (curated): myeloperoxidase deficiency (Moderate, GenCC)
• GWAS associations: 32
• Clinical variants (ClinVar): 85 total — 4 likely-pathogenic
• Phenotypes (HPO): 14
• Druggable target: yes — 19 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_000250

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:7218
Approved symbol	MPO
Name	myeloperoxidase
Location	17q22
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000005381
Ensembl biotype	protein_coding
OMIM	606989
Entrez	4353

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 2 protein_coding, 2 protein_coding_CDS_not_defined, 2 retained_intron, 1 nonsense_mediated_decay

ENST00000225275, ENST00000577220, ENST00000578493, ENST00000580005, ENST00000581022, ENST00000699291, ENST00000699292

RefSeq mRNA: 1 — MANE Select: NM_000250 NM_000250

CCDS: CCDS11604

Canonical transcript exons

ENST00000225275 — 12 exons

Exon	Start	End
ENSE00000480273	58279008	58279214
ENSE00000480274	58277827	58278145
ENSE00000480276	58273414	58273669
ENSE00000739347	58271655	58271892
ENSE00000739352	58275542	58275702
ENSE00000739356	58279297	58279426
ENSE00000739375	58279523	58279646
ENSE00000739378	58279839	58280014
ENSE00000739393	58280366	58280459
ENSE00001151664	58269855	58270863
ENSE00001151667	58280605	58280935
ENSE00002445423	58272748	58272918

Expression profiles

Bgee: expression breadth ubiquitous, 157 present calls, max score 99.55.

FANTOM5 (CAGE): breadth broad, TPM avg 34.8139 / max 8476.8700, expressed in 296 samples.

FANTOM5 promoters (33 alternative TSS)

Promoter ID	TPM avg	Samples expressed
167226	22.8882	67
167225	6.1396	46
167224	2.3700	32
167206	0.3604	20
167198	0.3227	154
167197	0.2957	127
167223	0.2001	19
167216	0.1870	16
167202	0.1811	15
167192	0.1752	20

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
trabecular bone tissue	UBERON:0002483	99.55	gold quality
bone marrow cell	CL:0002092	99.24	gold quality
bone marrow	UBERON:0002371	98.81	gold quality
bone element	UBERON:0001474	96.61	gold quality
monocyte	CL:0000576	88.14	gold quality
mononuclear cell	CL:0000842	88.03	gold quality
leukocyte	CL:0000738	86.92	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	83.55	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	80.89	gold quality
granulocyte	CL:0000094	80.30	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	77.52	silver quality
spleen	UBERON:0002106	75.99	gold quality
amniotic fluid	UBERON:0000173	74.88	gold quality
blood	UBERON:0000178	74.55	gold quality
right lung	UBERON:0002167	71.54	gold quality
minor salivary gland	UBERON:0001830	69.88	gold quality
saliva-secreting gland	UBERON:0001044	69.57	gold quality
endometrium epithelium	UBERON:0004811	68.42	gold quality
thymus	UBERON:0002370	66.05	silver quality
mouth mucosa	UBERON:0003729	66.01	gold quality
upper lobe of left lung	UBERON:0008952	65.73	gold quality
prefrontal cortex	UBERON:0000451	64.41	gold quality
upper lobe of lung	UBERON:0008948	64.11	gold quality
Brodmann (1909) area 10	UBERON:0013541	63.76	gold quality
gastrocnemius	UBERON:0001388	62.39	gold quality
pancreatic ductal cell	CL:0002079	61.74	silver quality
muscle of leg	UBERON:0001383	61.69	gold quality
nasal cavity mucosa	UBERON:0001826	61.38	gold quality
vena cava	UBERON:0004087	61.33	gold quality
adenohypophysis	UBERON:0002196	60.50	gold quality

Single-cell (SCXA)

Detected in 15 experiment(s), a significant marker in 15.

Experiment	Marker?	Max mean expression
E-MTAB-9801	yes	28866.69
E-MTAB-9067	yes	23589.16
E-GEOD-89232	yes	18532.04
E-GEOD-100618	yes	10251.11
E-CURD-112	yes	9740.02
E-CURD-6	yes	9221.90
E-CURD-122	yes	8671.28
E-MTAB-10432	yes	7989.05
E-HCAD-6	yes	6014.37
E-MTAB-7407	yes	4799.12
E-MTAB-10042	yes	4335.14
E-HCAD-4	yes	4312.68
E-MTAB-8884	yes	3351.29
E-GEOD-76312	yes	3050.07
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPA, CEBPE, CEBPG, FOXC1, HBP1, MYC, MYCN, NR1H3, PITX3, PPARA, PPARG, RARA, RUNX1, RUNX2, RXRA, SP1, SPI1, TAL1, TFDP1, TP53, WT1, ZNF296

miRNA regulators (miRDB)

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

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-12118	100.00	65.88	1270
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-6891-5P	99.98	66.53	1372
HSA-MIR-3173-3P	99.98	66.49	1217
HSA-MIR-95-5P	99.89	72.17	3973
HSA-MIR-6780A-5P	99.88	66.69	2776
HSA-MIR-4694-3P	99.79	69.53	2640
HSA-MIR-1273H-5P	99.77	66.32	2471
HSA-MIR-30B-3P	99.70	65.76	2325
HSA-MIR-3689A-3P	99.70	65.73	2306
HSA-MIR-3689B-3P	99.70	65.71	2311
HSA-MIR-3689C	99.70	65.71	2311
HSA-MIR-6779-5P	99.70	65.76	2363
HSA-MIR-4666B	99.64	68.69	1282
HSA-MIR-4276	99.56	67.66	2514
HSA-MIR-451B	99.55	68.28	1380
HSA-MIR-5683	99.36	68.59	2083
HSA-MIR-183-5P	99.31	72.27	1164
HSA-MIR-7158-5P	99.25	67.95	796
HSA-MIR-877-3P	99.09	68.10	1637
HSA-MIR-224-3P	98.91	68.42	1815
HSA-MIR-522-3P	98.91	68.56	1817
HSA-MIR-887-5P	98.82	65.90	1347
HSA-MIR-4297	98.77	66.95	2013
HSA-MIR-4710	98.61	65.96	1048
HSA-MIR-6827-5P	98.46	64.88	1256
HSA-MIR-6847-5P	97.93	66.74	1808
HSA-MIR-5581-5P	97.91	66.50	965
HSA-MIR-30C-1-3P	97.80	66.36	1499

Literature-anchored findings (GeneRIF, showing 40)

• Binding studies of myeloperoxidase support a model for a single common binding site for halides and thiocyanate as substrates or as inhibitors near the delta-meso carbon of the porphyrin ring in the enzyme. (PMID:11705390)
• The photoprotein pholasin as a luminescence substrate for detection of superoxide anion radicals and myeloperoxidase activity in stimulated neutrophils (PMID:11811524)
• Increased myeloperoxidase and lipid peroxide-modified protein in gynecological malignancies (LOOH-RSA, lipid peroxide-modified protein) (PMID:11813987)
• Neutrophils use MPO to initiate lipid peroxidation in whole plasma through multiple distinct diffusible substrates. Multiple endogenous diffusible substrates for myeloperoxidase in plasma are identified. (PMID:11861298)
• investigation of molecular mechanism of MPO-mediated apoptosis and caspase-3 activation (PMID:11981455)
• up-regulated by the AML1-MTG8 fusion protein, suggesting a role in the granulocytic maturation characteristic of the t(8;21) acute myelogenous leukemia (PMID:11986950)
• A common functional MPO promoter polymorphism (-463 G/A) is associated with increased incidence and clinical aspects of ANCA-associated small vessel vasculitis (PMID:12027420)
• MPO was observed to modulate the vascular signaling and vasodilatory functions of nitric oxide (NO) during acute inflammation (PMID:12089442)
• We confirm that the MPO -463 A variant affords a protective effect against lung cancer risk in smokers, which was strongest for SCLC patients. (PMID:12432558)
• Relative to subjects with the MPO G/G genotype, a significant decreased risk of lung cancer was found for carriers of G/A genotype. (PMID:12496042)
• Myeloperoxidase gene polymorphism does not decrease lung neoplasm susceptibility in caucasians. These findings are in contrast with the earlier studies suggesting a protective effect of carrying the variant A allele. (PMID:12496043)
• Lung cancer risk associated with genetic polymorphism in myeloperoxidase (-463 G/A) in a Chinese population (PMID:12515618)
• These data reveal substantial differences between the two known heme peroxidase superfamilies and reflect the dramatic differences observed in the oxidisability of substrates by the myeloperoxidase redox intermediates compound I and compound II. (PMID:12565898)
• Mediates lipid peroxidation of low-density lipoproteins as modulated by flavonoids. (PMID:12606047)
• Using mass spectrometric method, two products of myeloperoxidase, 5-chlorouracil and 5-bromouracil, were detected in neutrophil-rich human inflammatory tissue; in vitro mechanistic studies were also performed. (PMID:12707270)
• Expression of myeloperoxidase by neutrophils is necessary for their activation by anti-neutrophil cytoplasm autoantibodies against myeloperoxidase. (PMID:12773517)
• Lacrimal fluid peroxidase activity differs in men and women: the gender-related difference accentuates during ageing, probably owing to changing estrogen levels. (PMID:12792137)
• Myeloperoxidase promotor polymorphism is associated with hepatoblastoma (PMID:12800195)
• MPO polymorphism were associated with the extent of brain damage and the functional outcome rather than with the risk of developing brain infarction. (PMID:12818404)
• Myeloperoxidase (MPO) gene variation may modify the extent of advanced atherosclerotic lesions in the human aorta in early middle age. (PMID:12861032)
• In subjects with the high expression genotype of myeloperoxidase, the progression of atherosclerosis was significantly faster in the control group than in the hormone replacement therapy group, whereas in A allele carriers there were no differences (PMID:12915675)
• chemical mechanism behind the bactericidal action of the MPO-H(2)O(2)-Cl(-) system (PMID:12950060)
• in patients with acute coronary syndromes, MPO serum levels powerfully predict an increased risk for subsequent cardiovascular events; MPO may serve as both a marker and mediator of vascular inflammation (PMID:12952835)
• study shows that peroxisome proliferator-activated receptor gamma (PPARgamma) agonists strongly regulate myeloperoxidase gene expression through the Alu element repeats (PMID:14668325)
• These findings provide evidence that myeloperoxidase polymorphism is associated with coronary artery reactivity. (PMID:14730210)
• The heme-containing protein myeloperoxidase is released from stimulated polymorphonuclear leukocytes at sites of inflammation (PMID:14972011)
• Myeloperoxidase polymorphism related to cardiovascular events in coronary artery disease (PMID:15006595)
• The presence of MPO-G/G and A2M-Val/Val genotypes synergistically increased the risk of AD (OR, 25.5; 95% CI, 4.65-139.75). (PMID:15023809)
• Analysis of polymorphism in chronic renal failure patients undergoing hemodialysis. (PMID:15068388)
• the MPO/H2O2/SCN- system may have the potential to play a significant role in the oxidative modification of LDL (PMID:15203186)
• MPO G/G genotype may be one of the genetic factors influencing the progression rate of disability in multiple sclerosis patients. (PMID:15222689)
• Myeloperoxidase was detected in neurons. The increase in neuronal myeloperoxidase expression we observed in Alzheimer disease brains raises the possibility that the enzyme contributes to the oxidative stress implicated in the pathogenesis of the disorder (PMID:15255951)
• MPO appears to be an important modulator of vasomotor function in inflammatory vascular disease (PMID:15304260)
• Insights into mechanisms for inactivating MPO and the novel mode of oxygen binding to the hemoprotein may provide important clues toward understanding the catalytic action of MPO. (PMID:15350145)
• involvement of MPO in the antituberculous, immunological response implies its connection with TNF-alpha and IL-12 activation. (PMID:15379210)
• May represent an important pathway in diabetes complications and a new mechanism in phagocyte- and systemic infection-induced exacerbation of diabetic vascular diseases. (PMID:15504976)
• Mutations of the gene associated with MPO deficiency in Italian patients. (PMID:15507752)
• Mutations of the gene associated with MPO deficiency in Japanese patients. (PMID:15507753)
• Post-translational processing of pro-MPO, MPO secretion and storage, and the role of MPO in signal transduction in granulocytes. (PMID:15507754)
• Myeloperoxidase (MPO)-specific antibodies against neutrophils, anti-neutrophil cytoplasmic antibodies (MPO-ANCA) is involved in the development of vasculitis. (PMID:15507759)

Cross-species orthologs

11 orthologs

Organism	Symbol	Gene ID
danio_rerio	epx	ENSDARG00000012535
mus_musculus	Mpo	ENSMUSG00000009350
rattus_norvegicus	Mpo	ENSRNOG00000008310
drosophila_melanogaster	Pxd	FBGN0004577
drosophila_melanogaster	Pxn	FBGN0011828
drosophila_melanogaster	CG4009	FBGN0038469
drosophila_melanogaster	cysu	FBGN0038511
caenorhabditis_elegans		WBGENE00004256
caenorhabditis_elegans		WBGENE00004257
caenorhabditis_elegans		WBGENE00016700
caenorhabditis_elegans		WBGENE00019613

Paralogs (5): TPO (ENSG00000115705), EPX (ENSG00000121053), PXDN (ENSG00000130508), PXDNL (ENSG00000147485), LPO (ENSG00000167419)

Protein

Protein identifiers

Myeloperoxidase — P05164 (reviewed: P05164)

All UniProt accessions (3): P05164, A0A8V8TPE5, J3QSF7

UniProt curated annotations — full annotation on UniProt →

Function. Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity. Mediates the proteolytic cleavage of alpha-1-microglobulin to form t-alpha-1-microglobulin, which potently inhibits oxidation of low-density lipoprotein particles and limits vascular damage.

Subunit / interactions. Homodimer; disulfide-linked. Each monomer consists of a light and a heavy chain. Found in a complex with CP and LTF; interacts directly with CP, which protects CP antioxidant properties by MPO.

Subcellular location. Lysosome.

Disease relevance. Myeloperoxidase deficiency (MPOD) [MIM:254600] A disorder characterized by decreased myeloperoxidase activity in neutrophils and monocytes that results in disseminated candidiasis. The disease is caused by variants affecting the gene represented in this entry.

Cofactor. Binds 1 Ca(2+) ion per monomer. Binds 1 heme b (iron(II)-protoporphyrin IX) group covalently per monomer.

Similarity. Belongs to the peroxidase family. XPO subfamily.

Isoforms (3)

UniProt ID	Names	Canonical?
P05164-1	H17, B	yes
P05164-2	H14
P05164-3	H7, A

RefSeq proteins (1): NP_000241* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR010255	Haem_peroxidase_sf	Homologous_superfamily
IPR019791	Haem_peroxidase_animal	Family
IPR037120	Haem_peroxidase_sf_animal	Homologous_superfamily

Pfam: PF03098

Enzyme classification (BRENDA):

• EC 1.11.2.2 — myeloperoxidase (BRENDA: 9 organisms, 109 substrates, 246 inhibitors, 35 Km, 33 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
1-ACETYL-4-(METHYLSULFANYL)BENZENE	0.016–0.039	2
1-CHLORO-4-(METHYLSULFANYL)BENZENE	0.027–0.067	2
1-METHOXY-4-(METHYLSULFANYL)BENZENE	0.012–0.03	2
1-METHYL-4-(METHYLSULFANYL)BENZENE	0.032–0.04	2
1-NITRO-4-(METHYLSULFANYL)BENZENE	0.066–0.076	2
3,4-DIHYDROXYPHENYLACETIC ACID	0.52–21.9	2
4-(METHYLSULFANYL)ANILINE	0.057–0.104	2
BENZOTHIOPHENE	0.072–0.081	2
BENZYL METHYL SULFIDE	0.05–0.083	2
CATECHOL	1.84–21.1	2
DOPAMINE	0.64–136.3	2
H2O2	0.03–0.07	2
PHENYL PROPAN-2-YL SULFIDE	0.026–0.041	2
SCN-	0.25–0.29	2
THIOANISOLE	0.018–0.02	2

Catalyzed reactions (Rhea), 1 shown:

• chloride + H2O2 + H(+) = hypochlorous acid + H2O (RHEA:28218)

UniProt features (100 total): helix 28, strand 20, turn 10, binding site 9, sequence variant 8, disulfide bond 7, glycosylation site 6, chain 5, splice variant 2, signal peptide 1, site 1, modified residue 1, sequence conflict 1, active site 1

Structure

Experimental structures (PDB)

49 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
5MFA	X-RAY DIFFRACTION	1.2
5FIW	X-RAY DIFFRACTION	1.7
1D2V	X-RAY DIFFRACTION	1.75
1CXP	X-RAY DIFFRACTION	1.8
1DNU	X-RAY DIFFRACTION	1.85
1D5L	X-RAY DIFFRACTION	1.9
1D7W	X-RAY DIFFRACTION	1.9
1DNW	X-RAY DIFFRACTION	1.9
9QEX	X-RAY DIFFRACTION	1.9
4C1M	X-RAY DIFFRACTION	2
4DL1	X-RAY DIFFRACTION	2
9QE3	X-RAY DIFFRACTION	2.06
6WY7	X-RAY DIFFRACTION	2.09
7NI3	X-RAY DIFFRACTION	2.1
7NI1	X-RAY DIFFRACTION	2.11
7QZR	X-RAY DIFFRACTION	2.18
9QJO	X-RAY DIFFRACTION	2.18
9QGA	X-RAY DIFFRACTION	2.21
6WXZ	X-RAY DIFFRACTION	2.23
1MHL	X-RAY DIFFRACTION	2.25
7LAN	X-RAY DIFFRACTION	2.28
7Z53	X-RAY DIFFRACTION	2.28
6AZP	X-RAY DIFFRACTION	2.29
3ZS0	X-RAY DIFFRACTION	2.3
5WDJ	X-RAY DIFFRACTION	2.4
5UZU	X-RAY DIFFRACTION	2.4
6BMT	X-RAY DIFFRACTION	2.4
9SDS	X-RAY DIFFRACTION	2.49
6WYD	X-RAY DIFFRACTION	2.55
3ZS1	X-RAY DIFFRACTION	2.6

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P05164-F1	89.55	0.76

Functional residue map

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

Catalytic / active sites (2): 405 (transition state stabilizer); 261 (proton acceptor)

Ligand- & substrate-binding residues (9): 336; 338; 340; 408 (covalent); 409 (covalent); 502 (axial binding residue); 260 (covalent); 262; 334

Post-translational modifications (1): 316

Disulfide bonds (7): 167–180, 281–291, 285–309, 319, 387–398, 606–663, 704–730

Glycosylation sites (6): 139, 323, 355, 391, 483, 729

Function

Pathways and Gene Ontology

Reactome pathways

2 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation
R-HSA-8941413	Events associated with phagocytolytic activity of PMN cells

MSigDB gene sets: 270 (showing top): VERHAAK_AML_WITH_NPM1_MUTATED_DN, MODULE_93, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_SECRETORY_GRANULE, GOBP_HYDROGEN_PEROXIDE_CATABOLIC_PROCESS, GOBP_SUPEROXIDE_METABOLIC_PROCESS, GOBP_RESPONSE_TO_FOOD, CHEOK_RESPONSE_TO_HD_MTX_UP, MODULE_16, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, MODULE_118, GOBP_REACTIVE_OXYGEN_SPECIES_BIOSYNTHETIC_PROCESS, GOBP_SMALL_MOLECULE_BIOSYNTHETIC_PROCESS, MODULE_75, GOBP_CELLULAR_RESPONSE_TO_TOXIC_SUBSTANCE

GO Biological Process (16): response to yeast (GO:0001878), hypochlorous acid biosynthetic process (GO:0002149), respiratory burst involved in defense response (GO:0002679), defense response (GO:0006952), response to oxidative stress (GO:0006979), response to mechanical stimulus (GO:0009612), removal of superoxide radicals (GO:0019430), response to food (GO:0032094), response to lipopolysaccharide (GO:0032496), low-density lipoprotein particle remodeling (GO:0034374), defense response to bacterium (GO:0042742), hydrogen peroxide catabolic process (GO:0042744), negative regulation of apoptotic process (GO:0043066), defense response to fungus (GO:0050832), response to gold nanoparticle (GO:1990268), cellular oxidant detoxification (GO:0098869)

GO Molecular Function (7): chromatin binding (GO:0003682), peroxidase activity (GO:0004601), heparin binding (GO:0008201), heme binding (GO:0020037), metal ion binding (GO:0046872), protein binding (GO:0005515), oxidoreductase activity (GO:0016491)

GO Cellular Component (10): extracellular region (GO:0005576), obsolete extracellular space (GO:0005615), nucleus (GO:0005634), nucleoplasm (GO:0005654), lysosome (GO:0005764), secretory granule (GO:0030141), azurophil granule lumen (GO:0035578), azurophil granule (GO:0042582), extracellular exosome (GO:0070062), phagocytic vesicle lumen (GO:0097013)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
Innate Immune System	1
ROS and RNS production in phagocytes	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
defense response	3
response to fungus	2
response to stress	2
binding	2
cellular anatomical structure	2
oxoacid metabolic process	1
small molecule biosynthetic process	1
reactive oxygen species biosynthetic process	1
immune effector process	1
respiratory burst	1
response to external stimulus	1
response to abiotic stimulus	1
superoxide metabolic process	1
cellular response to superoxide	1
cellular oxidant detoxification	1
response to nutrient levels	1
response to chemical	1
response to molecule of bacterial origin	1
response to lipid	1
response to oxygen-containing compound	1
plasma lipoprotein particle remodeling	1
response to bacterium	1
catabolic process	1
hydrogen peroxide metabolic process	1
apoptotic process	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
response to transition metal nanoparticle	1
cellular detoxification	1
antioxidant activity	1
oxidoreductase activity, acting on peroxide as acceptor	1
glycosaminoglycan binding	1
sulfur compound binding	1
tetrapyrrole binding	1
cation binding	1
catalytic activity	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
lytic vacuole	1
endomembrane system	1

Protein interactions and networks

STRING

3240 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
MPO	ELANE	P08246	999
MPO	PRTN3	P15637	998
MPO	CTSG	P08311	997
MPO	LTF	P02788	997
MPO	BPI	P17213	982
MPO	MMP9	P14780	968
MPO	CAMP	P49913	965
MPO	CTSS	P25774	963
MPO	AZU1	P20160	943
MPO	APOA1	P02647	923
MPO	LYZ	P00695	912
MPO	H3-7	Q5TEC6	886
MPO	H3C14	Q71DI3	886
MPO	H3C1	P02295	885
MPO	H3-3A	P06351	885
MPO	H3-4	Q16695	885
MPO	H3-5	Q6NXT2	885

IntAct

81 interactions, top by confidence:

A	B	Type	Score
CALR	MPO	psi-mi:“MI:0407”(direct interaction)	0.580
MPO	CALR	psi-mi:“MI:0915”(physical association)	0.580
CALR	MPO	psi-mi:“MI:2364”(proximity)	0.580
STUB1	MPO	psi-mi:“MI:0915”(physical association)	0.560
MPO	CFP	psi-mi:“MI:0407”(direct interaction)	0.540
FRMD1	A2ML1	psi-mi:“MI:0914”(association)	0.530
ICE2	HP	psi-mi:“MI:0914”(association)	0.530
APCDD1	JCHAIN	psi-mi:“MI:0914”(association)	0.530
EGFL8	MPO	psi-mi:“MI:0914”(association)	0.530
PRRT2	NDUFS4	psi-mi:“MI:0914”(association)	0.530
MPO	CCDC47	psi-mi:“MI:0915”(physical association)	0.400
MPO	HNRNPK	psi-mi:“MI:0915”(physical association)	0.400
MPO	C3	psi-mi:“MI:0915”(physical association)	0.400
MPO	C9	psi-mi:“MI:0915”(physical association)	0.400
MPO	SLC4A1	psi-mi:“MI:0915”(physical association)	0.400
MPO	GYPB	psi-mi:“MI:0915”(physical association)	0.400
MPO	GYPA	psi-mi:“MI:0915”(physical association)	0.400
Dynll1		psi-mi:“MI:0915”(physical association)	0.400
	LECT2	psi-mi:“MI:0915”(physical association)	0.400
CD177	MYO1G	psi-mi:“MI:0914”(association)	0.350
GSK3B	PRSS37	psi-mi:“MI:0914”(association)	0.350
PHF21B	KDM1A	psi-mi:“MI:0914”(association)	0.350
TIFAB	DDX3X	psi-mi:“MI:0914”(association)	0.350
IRAK2	LTF	psi-mi:“MI:0914”(association)	0.350
SRPK1	SNRPGP15	psi-mi:“MI:0914”(association)	0.350
ATG16L1		psi-mi:“MI:0914”(association)	0.350
GOLGA8A	ZNF320	psi-mi:“MI:0914”(association)	0.350

BioGRID (62): MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), MPO (Co-fractionation), ELANE (Co-fractionation), MPO (Co-fractionation), MPO (Co-fractionation), MPO (Co-fractionation), MPO (Affinity Capture-MS), MPO (Affinity Capture-MS), CCDC47 (Proximity Label-MS)

ESM2 similar proteins: A0A1Y9G8H0, A0A452E9Y6, A1A4K5, A1KZ92, A5JUY8, P05164, P07202, P09933, P11247, P11678, P14650, P15396, P22079, P22413, P35419, P43446, P49290, P49340, P57110, P70669, P78562, P80025, Q01603, Q08410, Q13822, Q20616, Q23490, Q2KIY5, Q3TCN2, Q4QQW8, Q5R5M5, Q5SW46, Q64610, Q6DYE8, Q6P9A2, Q801F7, Q8CIY2, Q8HYB7, Q8HZK2, Q8HZK3

Diamond homologs: A0A1Y9G8H0, A0A452E9Y6, A1KZ92, A4IGL7, A5JUY8, A8WQH2, B3A0Q8, G5EG78, H2A0M7, O02768, P05164, P07202, P09933, P11247, P11678, P14650, P22079, P35355, P35419, P49290, P80025, P82600, P90820, Q01603, Q1ENI8, Q20616, Q23490, Q3UQ28, Q5SW46, Q6TMK4, Q7QH73, Q8HYB7, Q8R481, Q92626, Q9VEG6, Q9VZZ4, A2A8L5, A2AJ76, A4IFW2, A4IIW9

SIGNOR signaling

3 interactions.

A	Effect	B	Mechanism
KRT1	“up-regulates quantity”	MPO	binding
MPO	“down-regulates activity”	APOA1	oxidation
MPO	“up-regulates activity”	MPO-ANCA	binding

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	4
Uncertain significance	61
Likely benign	10
Benign	2

Top pathogenic / likely-pathogenic (4)

Variant ID	HGVS	Classification
3351076	NM_000250.2(MPO):c.604dup (p.Glu202fs)	Likely pathogenic
3779889	NM_000250.2(MPO):c.817dup (p.Ala273fs)	Likely pathogenic
3893371	NM_000250.2(MPO):c.760_764del (p.Gln254fs)	Likely pathogenic
4845803	NM_000250.2(MPO):c.1805G>A (p.Trp602Ter)	Likely pathogenic

SpliceAI

1731 predictions. Top by Δscore:

Variant	Effect	Δscore
17:58271674:T:TA	donor_gain	1.0000
17:58271893:C:CC	acceptor_gain	1.0000
17:58271893:C:CG	acceptor_loss	1.0000
17:58271894:T:A	acceptor_loss	1.0000
17:58272743:CTCAC:C	donor_loss	1.0000
17:58272744:TCAC:T	donor_loss	1.0000
17:58272745:CAC:C	donor_loss	1.0000
17:58272747:CCTGG:C	donor_loss	1.0000
17:58272915:CCAC:C	acceptor_gain	1.0000
17:58272916:CAC:C	acceptor_gain	1.0000
17:58272916:CACC:C	acceptor_gain	1.0000
17:58272917:ACCTG:A	acceptor_loss	1.0000
17:58272919:C:CA	acceptor_loss	1.0000
17:58272919:C:CC	acceptor_gain	1.0000
17:58272920:T:A	acceptor_loss	1.0000
17:58273640:C:CT	acceptor_gain	1.0000
17:58275700:CCCCT:C	acceptor_gain	1.0000
17:58275701:CCCT:C	acceptor_gain	1.0000
17:58275702:CCT:C	acceptor_gain	1.0000
17:58275704:T:C	acceptor_gain	1.0000
17:58275704:T:TC	acceptor_gain	1.0000
17:58277821:GCTGA:G	donor_loss	1.0000
17:58277822:CTGA:C	donor_loss	1.0000
17:58277823:TGA:T	donor_loss	1.0000
17:58277826:CCT:C	donor_loss	1.0000
17:58278145:TCTGA:T	acceptor_loss	1.0000
17:58278146:C:CC	acceptor_gain	1.0000
17:58279003:GCCAC:G	donor_loss	1.0000
17:58279004:CCACC:C	donor_loss	1.0000
17:58279005:CACC:C	donor_loss	1.0000

AlphaMissense

4867 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:58272792:A:G	L583P	0.998
17:58275702:C:T	G402E	0.998
17:58277827:C:A	G402W	0.998
17:58279111:T:G	H261P	0.998
17:58279112:G:C	H261D	0.998
17:58272763:C:G	D593H	0.997
17:58272771:C:G	R590P	0.997
17:58272779:G:C	N587K	0.997
17:58272779:G:T	N587K	0.997
17:58272795:T:A	D582V	0.997
17:58272796:C:G	D582H	0.997
17:58272821:A:C	F573L	0.997
17:58272821:A:T	F573L	0.997
17:58272823:A:G	F573L	0.997
17:58273553:G:C	F494L	0.997
17:58273553:G:T	F494L	0.997
17:58273555:A:G	F494L	0.997
17:58275699:T:A	D403V	0.997
17:58275700:C:G	D403H	0.997
17:58278038:G:C	N331K	0.997
17:58278038:G:T	N331K	0.997
17:58279201:G:A	S231F	0.997
17:58272767:G:C	S591R	0.996
17:58272767:G:T	S591R	0.996
17:58272769:T:G	S591R	0.996
17:58272772:G:T	R590S	0.996
17:58272795:T:C	D582G	0.996
17:58272795:T:G	D582A	0.996
17:58275567:C:G	R447P	0.996
17:58275645:C:G	R421P	0.996

dbSNP variants (sampled 300 via entrez): RS1000101468 (17:58280749 G>A,T), RS1000310243 (17:58274648 C>T), RS1000595006 (17:58279459 G>A), RS1001402037 (17:58271024 C>T), RS1001483429 (17:58275005 C>T), RS1001585282 (17:58269384 C>T), RS1001677370 (17:58277024 C>T), RS1001813732 (17:58282341 G>A), RS1002218367 (17:58278551 C>A), RS1002269442 (17:58278258 C>A,T), RS1002396813 (17:58272218 G>A), RS1002450453 (17:58273908 T>C), RS1002882347 (17:58282841 C>T), RS1002946630 (17:58275806 C>T), RS1002964958 (17:58270668 C>G,T)

Disease associations

OMIM: gene MIM:606989 | disease phenotypes: MIM:254600, MIM:104300

GenCC curated gene-disease

Disease	Classification	Inheritance
myeloperoxidase deficiency	Moderate	Autosomal recessive

Mondo (3): myeloperoxidase deficiency (MONDO:0009694), Alzheimer disease type 1 (MONDO:0007088), Alzheimer disease (MONDO:0004975)

Orphanet (3): Myeloperoxidase deficiency (Orphanet:2587), Early-onset autosomal dominant Alzheimer disease (Orphanet:1020), NON RARE IN EUROPE: Alzheimer disease (Orphanet:238616)

HPO phenotypes

14 total (14 of 14 shown, HPO-id order):

HPO	Term
HP:0000006	Autosomal dominant inheritance
HP:0000007	Autosomal recessive inheritance
HP:0000726	Dementia
HP:0001300	Parkinsonism
HP:0001871	Abnormality of blood and blood-forming tissues
HP:0001939	Abnormality of metabolism/homeostasis
HP:0002185	Neurofibrillary tangles
HP:0002423	Long-tract sign
HP:0002511	Alzheimer disease
HP:0002715	Abnormality of the immune system
HP:0003581	Adult onset
HP:0410054	Decreased circulating GABA concentration
HP:6000375	Reduced neutrophil myeloperoxidase activity
HP:6000513	Diminished neutrophil myeloperoxidase activity

GWAS associations

32 associations (top):

Study	Trait	p-value
GCST001980_2	Circulating myeloperoxidase levels (plasma)	4.000000e-09
GCST003265_271	Post bronchodilator FEV1/FVC ratio in COPD	4.000000e-06
GCST004608_125	Granulocyte percentage of myeloid white cells	9.000000e-57
GCST004609_82	Monocyte percentage of white cells	4.000000e-63
GCST004610_105	White blood cell count	9.000000e-13
GCST004613_57	Sum neutrophil eosinophil counts	3.000000e-17
GCST004614_64	Granulocyte count	6.000000e-17
GCST004620_99	Sum basophil neutrophil counts	2.000000e-18
GCST004625_244	Monocyte count	8.000000e-41
GCST004626_147	Myeloid white cell count	4.000000e-17
GCST004629_33	Neutrophil count	2.000000e-18
GCST004633_3	Neutrophil percentage of white cells	2.000000e-15
GCST009597_224	Multiple sclerosis	8.000000e-06
GCST009731_1	Blood protein levels in cardiovascular risk	5.000000e-16
GCST90002379_184	Basophil count	3.000000e-23
GCST90002379_185	Basophil count	3.000000e-30
GCST90002380_3	Basophil percentage of white cells	7.000000e-10
GCST90002380_4	Basophil percentage of white cells	5.000000e-26
GCST90002389_238	Lymphocyte percentage of white cells	1.000000e-12
GCST90002393_527	Monocyte count	5.000000e-12
GCST90002393_528	Monocyte count	2.000000e-09
GCST90002393_529	Monocyte count	9.000000e-50
GCST90002394_406	Monocyte percentage of white cells	2.000000e-31
GCST90002394_407	Monocyte percentage of white cells	3.000000e-10
GCST90002394_408	Monocyte percentage of white cells	3.000000e-17
GCST90002394_409	Monocyte percentage of white cells	7.000000e-71
GCST90002398_305	Neutrophil count	9.000000e-18
GCST90002398_307	Neutrophil count	2.000000e-10
GCST90002399_246	Neutrophil percentage of white cells	5.000000e-30
GCST90002399_247	Neutrophil percentage of white cells	2.000000e-09

EFO canonical traits (12, from GWAS)

EFO ID	Trait name
EFO:0005243	myeloperoxidase measurement
EFO:0004713	FEV/FVC ratio
EFO:0007997	granulocyte percentage of myeloid white cells
EFO:0007989	monocyte percentage of leukocytes
EFO:0004833	neutrophil count
EFO:0004842	eosinophil count
EFO:0007987	granulocyte count
EFO:0005090	basophil count
EFO:0005091	monocyte count
EFO:0007990	neutrophil percentage of leukocytes
EFO:0007992	basophil percentage of leukocytes
EFO:0007993	lymphocyte percentage of leukocytes

MeSH disease descriptors (3)

Descriptor	Name	Tree numbers
D000544	Alzheimer Disease	C10.228.140.380.100; C10.574.945.249; F03.615.400.100
C536594	Alzheimer disease type 1 (supp.)
C562864	Myeloperoxidase Deficiency (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2439 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

19 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,167,862 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1043	DAPSONE	4	64,779
CHEMBL1518	PROPYLTHIOURACIL	4	15,046
CHEMBL276832	HYDRALAZINE	4	23,794
CHEMBL45	MELATONIN	4	56,417
CHEMBL490	PAROXETINE	4	46,410
CHEMBL54976	TRYPTOPHAN	4	549,527
CHEMBL56367	NIMESULIDE	4	25,455
CHEMBL64	ISONIAZID	4	145,319
CHEMBL686	MEFENAMIC ACID	4	61,835
CHEMBL86	METOCLOPRAMIDE	4	37,825
CHEMBL4297594	VERDIPERSTAT	3	140
CHEMBL50	QUERCETIN	3	74,559
CHEMBL1232461	MOLIBRESIB	2	1,538
CHEMBL2105120	FTIVAZIDE	2	118
CHEMBL23588	FLUFENAMIC ACID	2	34,797
CHEMBL267044	LEVOSULPIRIDE	2	4,275
CHEMBL5095218	MITIPERSTAT	2	52
CHEMBL150	KAEMPFEROL	1	25,940
CHEMBL3633460	PF-06282999	1	36

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2333227	MPO		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 1.-.-.- Oxidoreductases

Most potent curated ligand interactions (6 total), top 6:

Ligand	Action	Affinity	Parameter
mitiperstat	Inhibition	9.15	pIC50
compound 28 [PMID: 28671460]	Inhibition	7.36	pIC50
aminopyridine 2	Inhibition	6.8	pIC50
AZD5904	Inhibition	6.7	pIC50
PF-06282999	Inhibition	6.5	pKi
verdiperstat	Inhibition	6.2	pIC50

Binding affinities (BindingDB)

128 measured of 133 human assays (137 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL5181350	IC50	3.6 nM
CHEMBL5197968	IC50	5 nM
1-[2-(1-Aminoethyl)-4-chlorobenzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	7 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
Alternative Preparation	IC50	7 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
US10407422, Example 130	IC50	8 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
1-{2-[(1R)-1-Aminopropyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	8.6 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-{2-[(Cyclobutylamino)methyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	10 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
US10407422, Example 5	IC50	11 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
1-{4-Chloro-2-[(methylamino)methyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	13 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
CHEMBL5200126	IC50	13 nM
1-{2-[(Cyclopentylamino)methyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	14 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-[2-(Aminomethyl)-4-chlorobenzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	15 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-{4-Chloro-2-[1-(methylamino)ethyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	19 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
US10407422, Example 1	IC50	19 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
US10407422, Example 52	IC50	20 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
US10407422, Example 187	IC50	21 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
1-{4-Chloro-2-[(ethylamino)methyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	22 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-{2-[(Propan-2-ylamino)methyl]benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	24 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-(2-{[(Cyclobutylmethyl)amino]methyl}benzyl)-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	29 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
US10407422, Example 34	IC50	30 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
US10407422, Example 53	IC50	32 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
1-[2-(Aminomethyl)-4-(trifluoromethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	40 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
1-{2-[(1S)-1-Aminoethyl]-4-chlorobenzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	42 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
US10407422, Example 185	IC50	45 nM	US-10407422: Triazolopyridine inhibitors of myeloperoxidase
1-{2-[(Methylamino)methyl]-4-(trifluoromethyl)benzyl}-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	49 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
7-{18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13,15,17	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-[(11S)-11-Methyl-18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13,15,17	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-{17-Oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12,14,16	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-(14-fluoro-17-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl)-2H-triazolo[4,5-b]pyridin-5-amine	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-[(3R,4S,6S,10R)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(19),11(21),12,16(20),17-pentaen-10-yl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-[(3R,4S,6S,10S)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(19),11(21),12,16(20),17-pentaen-10-yl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-[(17S)-18-phenyl-16-oxa-2,8,9-triazapentacyclo[16.2.2.11,17.16,9.111,15]pentacosa-6(25),7,11(24),12,14-pentaen-5-yl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
7-[(18S)-19-phenyl-17-oxa-2,8,9-triazapentacyclo[17.2.2.11,18.16,9.112,16]hexacosa-6(26),7,12(25),13,15-pentaen-5-yl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	50 nM	US-10577383: Macrocyclic inhibitors of myeloperoxidase
1-(2-{[(2-Methylpropyl)amino]methyl}benzyl)-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one	IC50	54 nM	US-10016430: 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
7-benzyl-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-chlorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
3-[(5-amino-2H-triazolo[4,5-b]pyridin-7-yl)methyl]-4-fluorobenzonitrile	IC50	55 nM	US-10214527
7-[(2-fluoro-3-methylphenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-benzylphenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-phenylphenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-chloro-2,6-difluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(5-chloro-2-fluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(2-fluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-fluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
3-[(5-amino-2H-triazolo[4,5-b]pyridin-7-yl)methyl]benzonitrile	IC50	55 nM	US-10214527
7-[(2,6-difluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(2,5-difluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(3-chloro-2-fluorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(5-chloro-3-pyridinyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527
7-[(1-benzylindol-4-yl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	IC50	55 nM	US-10214527

ChEMBL bioactivities

936 potent at pChembl≥5 of 966 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	IC50	1	nM	CHEMBL4747269
9.00	IC50	1	nM	CHEMBL4790231
9.00	IC50	1	nM	CHEMBL5639106
8.90	IC50	1.259	nM	CHEMBL5197968
8.85	IC50	1.4	nM	CHEMBL4790231
8.82	IC50	1.5	nM	MITIPERSTAT
8.80	IC50	1.585	nM	MITIPERSTAT
8.70	IC50	2	nM	CHEMBL4763667
8.70	IC50	2	nM	CHEMBL5641842
8.70	IC50	2	nM	CHEMBL5646914
8.70	IC50	2	nM	CHEMBL5646667
8.54	IC50	2.9	nM	CHEMBL4752248
8.52	IC50	3	nM	CHEMBL2347170
8.52	IC50	3	nM	CHEMBL5641725
8.52	IC50	3	nM	CHEMBL5640015
8.44	IC50	3.6	nM	CHEMBL5181350
8.40	IC50	4	nM	CHEMBL2347168
8.34	IC50	4.6	nM	CHEMBL4548537
8.30	IC50	5	nM	CHEMBL2347177
8.30	IC50	5	nM	CHEMBL4068067
8.30	IC50	5	nM	CHEMBL1630742
8.30	IC50	5	nM	CHEMBL4740830
8.30	IC50	5	nM	CHEMBL4861370
8.30	IC50	5	nM	CHEMBL5197968
8.22	IC50	6	nM	CHEMBL2347170
8.22	IC50	6	nM	CHEMBL2347032
8.22	IC50	6	nM	CHEMBL4782307
8.17	IC50	6.7	nM	CHEMBL4453728
8.17	IC50	6.8	nM	CHEMBL4482878
8.15	IC50	7	nM	CHEMBL4851535
8.15	IC50	7	nM	CHEMBL5936050
8.15	IC50	7	nM	MITIPERSTAT
8.15	IC50	7	nM	CHEMBL4482878
8.15	IC50	7	nM	CHEMBL5796857
8.10	IC50	8	nM	CHEMBL2347168
8.10	IC50	8	nM	CHEMBL1630741
8.10	IC50	8	nM	CHEMBL4878307
8.10	IC50	8	nM	CHEMBL5924076
8.10	IC50	8	nM	CHEMBL1630742
8.07	IC50	8.5	nM	CHEMBL4594116
8.07	IC50	8.6	nM	CHEMBL5897801
8.06	IC50	8.7	nM	CHEMBL4482878
8.05	IC50	9	nM	CHEMBL4278946
8.05	IC50	9	nM	CHEMBL5794368
8.03	IC50	9.3	nM	CHEMBL4751166
8.00	IC50	10	nM	CHEMBL2347167
8.00	IC50	10	nM	CHEMBL2347166
8.00	IC50	10	nM	CHEMBL5999011
8.00	IC50	10	nM	CHEMBL5892400
8.00	IC50	10	nM	CHEMBL4482878

PubChem BioAssay actives

481 with measured affinity, of 1163 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
7-[(1R)-1-phenyl-3-[[(1S,3S)-3-phenyl-2,3-dihydro-1H-inden-1-yl]amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0010	uM
7-[(1R)-1-phenyl-3-[(4-phenyl-1-bicyclo[2.2.2]octanyl)amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0010	uM
1-[[2-[(2S,4R)-4-(difluoromethyl)piperidin-2-yl]phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0010	uM
1-[[2-[amino(phenyl)methyl]phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0013	uM
1-[[2-[(1R)-1-aminoethyl]-4-chlorophenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0015	uM
7-[(1R)-1-phenyl-3-[(4-phenylcyclohexyl)amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0020	uM
2-sulfanylidene-1-[[2-[(2R,4S)-4-(trifluoromethyl)piperidin-2-yl]phenyl]methyl]-5H-pyrrolo[3,2-d]pyrimidin-4-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0020	uM
2-sulfanylidene-3-[[2-[(2S,4R)-4-(trifluoromethyl)piperidin-2-yl]phenyl]methyl]-7H-purin-6-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0020	uM
1-[[2-[(2S)-piperidin-2-yl]phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0020	uM
7-[(1R)-1-phenyl-3-[[(1R,4S)-4-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl]amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0029	uM
2-sulfanylidene-3-[[2-[(2R,4R)-4-(trifluoromethyl)piperidin-2-yl]phenyl]methyl]-7H-purin-6-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0030	uM
1-[[2-[(2S)-4,4-difluoropiperidin-2-yl]phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	2144486: Inhibition of human MPO using H2O2 as substrate measured after 15 mins by chemiluminescence based assay	ic50	0.0030	uM
2-[2-(7-fluoro-1H-indol-3-yl)ethylsulfanyl]ethanamine	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0030	uM
3-[[2-[(1R)-1-aminoethyl]-4-chlorophenyl]methyl]-2-sulfanylidene-7H-purin-6-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0036	uM
2-[2-(5-fluoro-1H-indol-3-yl)ethylsulfanyl]ethanamine	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0040	uM
7-[(2,6-dichlorophenyl)methylsulfanyl]-2H-triazolo[4,5-b]pyridin-5-amine	1533019: Inhibition of human PMN leukocytes MPO peroxidation activity using H2O2 as substrate preincubated for 10 mins followed by H2O2 addition and measured for 15 mins by amplex red reagent based assay	ic50	0.0046	uM
2-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-N-hydroxy-4-oxo-1,3-diazinane-5-carboxamide	1802478: Myeloperoxidase Assay from Article 10.1074/jbc.M113.507756: “Potent reversible inhibition of myeloperoxidase by aromatic hydroxamates.”	ic50	0.0050	uM
7-[(3R,4S,6S,10S)-4-benzyl-2-oxa-7,13,14-triazatetracyclo[14.3.1.13,6.111,14]docosa-1(19),11(21),12,16(20),17-pentaen-10-yl]-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0050	uM
7-[(1R)-3-[2-fluoroethyl-(4-phenyl-1-bicyclo[2.2.2]octanyl)amino]-1-phenylpropyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0050	uM
5-(5-fluoro-1H-indol-3-yl)pentan-1-amine	1446226: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins	ic50	0.0050	uM
3-(5-fluoro-1H-indol-3-yl)propyl thiocyanate	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0050	uM
2-[[3,5-bis(trifluoromethyl)phenyl]methylamino]-N-hydroxy-6-oxo-1H-pyrimidine-5-carboxamide	1446226: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins	ic50	0.0050	uM
7-[(1R)-3-[methyl-(4-phenyl-1-bicyclo[2.2.2]octanyl)amino]-1-phenylpropyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0060	uM
4-(7-fluoro-1H-indol-3-yl)butan-1-amine	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0060	uM
7-[(2,6-dichlorophenyl)methoxy]-2H-triazolo[4,5-b]pyridin-5-amine	1533019: Inhibition of human PMN leukocytes MPO peroxidation activity using H2O2 as substrate preincubated for 10 mins followed by H2O2 addition and measured for 15 mins by amplex red reagent based assay	ic50	0.0067	uM
7-[(2-fluorophenyl)methylsulfanyl]-2H-triazolo[4,5-b]pyridin-5-amine	1533018: Inhibition of human PMN leukocytes MPO chlorination activity using H2O2 as substrate preincubated for 10 mins followed by H2O2 addition and measured for 15 mins in presence of NaCl by aminophenyl fluorescein based assay	ic50	0.0068	uM
7-[(17S)-18-phenyl-16-oxa-2,8,9-triazapentacyclo[16.2.2.11,17.16,9.111,15]pentacosa-6(25),7,11(24),12,14-pentaen-5-yl]-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0070	uM
4-(5-fluoro-1H-indol-3-yl)butan-1-amine	1446226: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins	ic50	0.0080	uM
7-(17-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.112,16]pentacosa-1(23),4,6(25),12(24),13,15,19,21-octaen-7-yl)-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0080	uM
7-[[5-(difluoromethyl)-2-phenyltriazol-4-yl]methylsulfanyl]-2H-triazolo[4,5-b]pyridin-5-amine	1533019: Inhibition of human PMN leukocytes MPO peroxidation activity using H2O2 as substrate preincubated for 10 mins followed by H2O2 addition and measured for 15 mins by amplex red reagent based assay	ic50	0.0085	uM
3-[[(2R)-oxolan-2-yl]methyl]-2-sulfanylidene-7H-purin-6-one	1416577: Inhibition of human MPO assessed as reduction in enzyme-mediated chlorination by measuring reduction in HOCl formation preincubated for 10 mins followed by H2O2/NaCl addition and measured at 30 secs time interval for 5 mins by APF dye based fluorescence assay	ic50	0.0090	uM
7-[1-phenyl-3-[(1-phenyl-2-oxabicyclo[2.2.2]octan-4-yl)amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0093	uM
2-[3-(5-fluoro-1H-indol-3-yl)propylamino]ethanol	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0100	uM
2-[2-(5-fluoro-1H-indol-3-yl)ethylamino]ethanol	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0100	uM
N-[3-(5-fluoro-1H-indol-3-yl)propyl]hydroxylamine	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0110	uM
7-[[5-(difluoromethyl)-2-phenyltriazol-4-yl]methoxy]-2H-triazolo[4,5-b]pyridin-5-amine	1533019: Inhibition of human PMN leukocytes MPO peroxidation activity using H2O2 as substrate preincubated for 10 mins followed by H2O2 addition and measured for 15 mins by amplex red reagent based assay	ic50	0.0120	uM
1-[[4-chloro-2-[(1R)-1-(methylamino)ethyl]phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0127	uM
N-benzyl-3-(5-fluoro-1H-indol-3-yl)propan-1-amine	1331722: Inhibition of MPO chlorination activity (unknown origin) assessed as taurine chloramine formation after 5 mins in presence of H2O2/Cl- by HTS method	ic50	0.0130	uM
7-(18-oxa-3,4,10-triazatetracyclo[17.3.1.13,6.113,17]pentacosa-1(23),4,6(25),13(24),14,16,19,21-octaen-7-yl)-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0140	uM
N-ethyl-N-[2-(5-fluoro-1H-indol-3-yl)ethyl]methanesulfonamide	738129: Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay	ic50	0.0140	uM
1-[[2-(aminomethyl)-4-chlorophenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0150	uM
7-[(1R)-1-phenyl-3-[[(1R,3R)-3-phenylcyclopentyl]amino]propyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698296: Inhibition of recombinant human MPO incubated for 10 mins in presence of 120 mM NaCl by aminophenyl fluorescein based assay	ic50	0.0150	uM
1-[[2-(azetidin-1-ylmethyl)phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0151	uM
1-[[4-chloro-2-(methylaminomethyl)phenyl]methyl]-2-sulfanylidene-5H-pyrrolo[3,2-d]pyrimidin-4-one	1875005: Inhibition of MPO (unknown origin) measured after 15 mins in presence of H2O2 by chemiluminescence assay	ic50	0.0159	uM
7-[(3-chlorophenyl)methyl]-2H-triazolo[4,5-b]pyridin-5-amine	1698277: Inhibition of recombinant human MPO incubated for 10 mins in presence of 240 mM NaCl and 10 uM H2O2 by aminophenyl fluorescein based assay	ic50	0.0160	uM
methyl 3-[(5-amino-2H-triazolo[4,5-b]pyridin-7-yl)methyl]benzoate	1698278: Inhibition of recombinant human MPO incubated for 10 mins by amplex red dye based assay	ic50	0.0170	uM
3-[(5-amino-2H-triazolo[4,5-b]pyridin-7-yl)methyl]benzonitrile	1698277: Inhibition of recombinant human MPO incubated for 10 mins in presence of 240 mM NaCl and 10 uM H2O2 by aminophenyl fluorescein based assay	ic50	0.0170	uM
7-(18-oxa-3,4,10-triazatetracyclo[18.3.1.13,6.113,17]hexacosa-1(24),4,6(26),13(25),14,16,20,22-octaen-7-yl)-2H-triazolo[4,5-b]pyridin-5-amine	1753665: Inhibition of MPO (unknown origin) chlorination activity incubated for 10 mins followed by NaCl addition by aminophenyl fluorescein assay	ic50	0.0170	uM
N-[3-(5-fluoro-1H-indol-3-yl)propyl]butan-1-amine	547368: Inhibition of recombinant MPO mediated LDL oxidation using MPO/Cl-/H2O2 system	ic50	0.0170	uM
4-(5-fluoro-1H-indol-3-yl)butanamide	1446226: Inhibition of recombinant MPO (unknown origin) assessed as reduction in taurine chloramine production preincubated with enzyme and taurine followed by H2O2 addition measured after 5 mins	ic50	0.0180	uM

CTD chemical–gene interactions

201 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Hydrogen Peroxide	increases phosphorylation, decreases activity, affects binding, decreases reaction, increases reaction (+10 more)	13
Tetradecanoylphorbol Acetate	decreases reaction, increases secretion, increases expression, increases activity, affects cotreatment (+2 more)	7
hydroquinone	increases cleavage, affects cotreatment, decreases activity, increases reaction, increases metabolic processing (+4 more)	5
Benzene	affects response to substance, increases response to substance, increases metabolic processing	5
Hypochlorous Acid	increases chemical synthesis, increases reaction, increases metabolic processing, affects activity, increases oxidation (+4 more)	5
Tretinoin	decreases expression, increases reaction, decreases reaction, affects cotreatment	5
Glutathione	increases activity, increases reaction, increases oxidation, increases chemical synthesis, decreases abundance (+3 more)	4
4-aminobenzhydrazide	increases oxidation, decreases activity, affects response to substance, decreases reaction, increases chemical synthesis	3
Benzo(a)pyrene	increases methylation, increases mutagenesis, affects response to substance	3
N-Formylmethionine Leucyl-Phenylalanine	increases reaction, decreases reaction, increases secretion, increases activity	3
Sodium Azide	decreases reaction, increases activity, increases reaction, affects cotreatment, increases oxidation (+1 more)	3
chlorodimedone	affects binding, decreases reaction, increases abundance, increases metabolic processing, increases reaction	2
5,5-dimethyl-1-pyrroline-1-oxide	affects cotreatment, increases glutathionylation, increases reaction, increases activity, increases oxidation (+2 more)	2
epigallocatechin gallate	affects cotreatment, decreases reaction, increases expression, increases chemical synthesis, increases metabolic processing	2
Irinotecan	affects cotreatment, increases activity, decreases expression, increases reaction	2
Wortmannin	decreases reaction, increases chemical synthesis, increases phosphorylation, increases secretion, affects cotreatment	2
Arsenic Trioxide	decreases expression, decreases reaction, affects cotreatment	2
Carvedilol	increases secretion, decreases reaction	2
Acetylcysteine	increases oxidation, increases reaction, increases chemical synthesis, affects binding, affects cotreatment	2
Aminoglutethimide	affects cotreatment, increases oxidation, increases metabolic processing, increases expression	2
Chlorine	decreases activity, affects binding, increases oxidation, increases reaction	2
Cisplatin	affects response to substance, decreases expression	2
Indomethacin	increases response to substance, decreases reaction, increases chemical synthesis, increases activity, increases oxidation	2
Lipopolysaccharides	decreases reaction, increases expression	2
Penicillamine	increases oxidation, increases reaction, increases chemical synthesis, decreases secretion	2
Tobacco Smoke Pollution	increases response to substance, decreases expression	2
Valproic Acid	increases methylation, affects expression	2
aristolochic acid I	increases expression	1
4-methoxybenzohydrazide	decreases activity, decreases reaction, increases oxidation	1
GSK484	decreases reaction, increases activity, affects cotreatment	1

ChEMBL screening assays

178 unique, capped per target: 165 binding, 9 functional, 4 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1027367	Binding	Inhibition of MPO activity in TNF-alpha-stimulated human HL60 cells measured enzyme activity per 10'6 cells by spectrophotometrically	Chemical components and its antioxidant properties in vitro: an edible marine brown alga, Ecklonia cava. — Bioorg Med Chem
CHEMBL3636512	ADMET	Drug metabolism assessed as formation of human MPO-mediated PTU-disulfide at 10 uM after 60 mins by LC-MS/MS analysis in presence of H2O2/Cl-	Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases. — J Med Chem
CHEMBL750554	Functional	In vivo agonist efficacy as the maximal lysosomal myeloperoxidase (MPO) release in PMNL assay	Improvements in the minimum binding sequence of C5a: examination of His-67. — J Med Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_B8KQ	Abcam HCT 116 MPO KO	Cancer cell line	Male
CVCL_B9MY	Abcam A-549 MPO KO	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT04520308	PHASE4	UNKNOWN	An Open-label, Single-arm Longitudinal Study With Dupilumab for Patients With Atopic Dermatitis
NCT00009191	PHASE4	COMPLETED	The Depression in Alzheimer’s Disease Study (DIADS)
NCT00009217	PHASE4	COMPLETED	Treatment of Behavioral Symptoms in Alzheimer’s Disease
NCT00018278	PHASE4	COMPLETED	Electrophysiologic Measures of Treatment Response in Alzheimer Disease
NCT00035204	PHASE4	COMPLETED	A Study of the Effects on Sleep, Attention, and Gastrointestinal Tolerance of Galantamine and Donepezil in Patients With Alzheimer’s Disease
NCT00042172	PHASE4	COMPLETED	Treatment for Early Memory Loss
NCT00046358	PHASE4	COMPLETED	The Effect of Short-Term Statins and NSAIDs on Levels of Beta-Amyloid, a Protein Associated With Alzheimer’s Disease
NCT00104442	PHASE4	COMPLETED	Study of the Effects of Current Drug Treatments on Levels of Certain Brain Chemicals in Alzheimer’s Disease
NCT00120874	PHASE4	COMPLETED	Memantine and Comprehensive, Individualized Management of Alzheimer’s Disease and Caregiver Training
NCT00142324	PHASE4	UNKNOWN	CALM-AD
NCT00165724	PHASE4	COMPLETED	Alzheimer’s Disease Long-term Follow-up Study (ALF Study)
NCT00165750	PHASE4	TERMINATED	Correlation Between Regional Brain Volume and Response to Donepezil Treatment in AD Patients
NCT00202124	PHASE4	COMPLETED	Double Blind Study of Trp01 in Patients With Alzheimer’s Disease
NCT00208819	PHASE4	COMPLETED	A Comparison of Two Standard Therapies in the Management of Dementia With Agitation
NCT00216515	PHASE4	COMPLETED	The Efficacy of Galantamine on the Attention and the Frontal Function of the Patients With Dementia of Alzheimer Type
NCT00230568	PHASE4	COMPLETED	EARTH 413: A Study of Aricept in Hispanic Patients With Mild to Moderate Alzheimer’s Disease (AD)
NCT00234637	PHASE4	COMPLETED	Rivastigmine Monotherapy and Combination Therapy With Memantine in Patients With Moderately Severe Alzheimer’s Disease Who Failed to Benefit From Previous Cholinesterase Inhibitor Treatment
NCT00245206	PHASE4	COMPLETED	Side Effects of Newer Antipsychotics in Older Adults
NCT00254033	PHASE4	COMPLETED	Apathy Associated With Alzheimer’s Disease
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