MAOA
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Summary
MAOA (monoamine oxidase A, HGNC:6833) is a protein-coding gene on chromosome Xp11.3, encoding Amine oxidase [flavin-containing] A (P21397). Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and perip…. It is haploinsufficient (ClinGen: sufficient evidence).
This gene is one of two neighboring gene family members that encode mitochondrial enzymes which catalyze the oxidative deamination of amines, such as dopamine, norepinephrine, and serotonin. Mutation of this gene results in Brunner syndrome. This gene has also been associated with a variety of other psychiatric disorders, including antisocial behavior. Alternatively spliced transcript variants encoding multiple isoforms have been observed.
Source: NCBI Gene 4128 — RefSeq curated summary.
At a glance
- Gene–disease (curated): Brunner syndrome (Definitive, ClinGen)
- GWAS associations: 1
- Clinical variants (ClinVar): 334 total — 11 pathogenic, 10 likely-pathogenic
- Phenotypes (HPO): 14
- Druggable target: yes — 130 molecules with ChEMBL bioactivity
- Dosage sensitivity (ClinGen): haploinsufficiency sufficient evidence, triplosensitivity no evidence
- MANE Select transcript:
NM_000240
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:6833 |
| Approved symbol | MAOA |
| Name | monoamine oxidase A |
| Location | Xp11.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000189221 |
| Ensembl biotype | protein_coding |
| OMIM | 309850 |
| Entrez | 4128 |
Gene structure
Transcript identifiers
Ensembl transcripts: 15 — 11 protein_coding, 2 protein_coding_CDS_not_defined, 2 retained_intron
ENST00000338702, ENST00000490604, ENST00000497485, ENST00000542639, ENST00000686683, ENST00000686980, ENST00000688006, ENST00000688859, ENST00000689087, ENST00000693128, ENST00000873971, ENST00000873972, ENST00000967109, ENST00000967110, ENST00000967111
RefSeq mRNA: 2 — MANE Select: NM_000240
NM_000240, NM_001270458
CCDS: CCDS14260, CCDS59163
Canonical transcript exons
ENST00000338702 — 15 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001369566 | 43740681 | 43740738 |
| ENSE00001373498 | 43736227 | 43736280 |
| ENSE00001377890 | 43732699 | 43732795 |
| ENSE00001382812 | 43731694 | 43731853 |
| ENSE00001383783 | 43731241 | 43731390 |
| ENSE00001389556 | 43744367 | 43746817 |
| ENSE00001415055 | 43656299 | 43656414 |
| ENSE00001614970 | 43743794 | 43743905 |
| ENSE00001677475 | 43741950 | 43742047 |
| ENSE00003487993 | 43711872 | 43711976 |
| ENSE00003495252 | 43712705 | 43712796 |
| ENSE00003501661 | 43683513 | 43683607 |
| ENSE00003526715 | 43728173 | 43728314 |
| ENSE00003583432 | 43744109 | 43744171 |
| ENSE00003691177 | 43693291 | 43693428 |
Expression profiles
Bgee: expression breadth ubiquitous, 285 present calls, max score 99.43.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 28.8661 / max 3828.9847, expressed in 1123 samples.
FANTOM5 promoters (8 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 196058 | 28.2360 | 1074 |
| 196057 | 0.3619 | 159 |
| 196056 | 0.1051 | 36 |
| 196055 | 0.0657 | 16 |
| 196067 | 0.0430 | 12 |
| 196068 | 0.0214 | 8 |
| 196066 | 0.0207 | 13 |
| 196059 | 0.0122 | 1 |
Top tissues by expression
295 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| ileal mucosa | UBERON:0000331 | 99.43 | gold quality |
| colonic mucosa | UBERON:0000317 | 98.86 | gold quality |
| mucosa of sigmoid colon | UBERON:0004993 | 98.85 | gold quality |
| right lung | UBERON:0002167 | 98.60 | gold quality |
| jejunal mucosa | UBERON:0000399 | 98.46 | gold quality |
| duodenum | UBERON:0002114 | 98.37 | gold quality |
| rectum | UBERON:0001052 | 98.35 | gold quality |
| parotid gland | UBERON:0001831 | 98.32 | gold quality |
| mucosa of stomach | UBERON:0001199 | 98.28 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 97.97 | gold quality |
| transverse colon | UBERON:0001157 | 97.95 | gold quality |
| lower lobe of lung | UBERON:0008949 | 97.83 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 97.69 | gold quality |
| subcutaneous adipose tissue | UBERON:0002190 | 97.57 | gold quality |
| colonic epithelium | UBERON:0000397 | 97.55 | gold quality |
| adipose tissue | UBERON:0001013 | 97.54 | gold quality |
| small intestine | UBERON:0002108 | 97.54 | gold quality |
| cardiac muscle of right atrium | UBERON:0003379 | 97.32 | gold quality |
| adult mammalian kidney | UBERON:0000082 | 97.19 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 97.12 | gold quality |
| thyroid gland | UBERON:0002046 | 97.12 | gold quality |
| upper lobe of lung | UBERON:0008948 | 97.12 | gold quality |
| intestine | UBERON:0000160 | 97.09 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 97.05 | gold quality |
| large intestine | UBERON:0000059 | 97.04 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 97.04 | gold quality |
| colon | UBERON:0001155 | 96.97 | gold quality |
| nephron tubule | UBERON:0001231 | 96.95 | gold quality |
| synovial joint | UBERON:0002217 | 96.92 | gold quality |
| liver | UBERON:0002107 | 96.74 | gold quality |
Single-cell (SCXA)
Detected in 7 experiment(s), a significant marker in 7.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-GEOD-125970 | yes | 631.07 |
| E-MTAB-10287 | yes | 30.71 |
| E-MTAB-6701 | yes | 16.77 |
| E-MTAB-6678 | yes | 9.29 |
| E-GEOD-130148 | yes | 8.71 |
| E-HCAD-10 | yes | 4.67 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): AR, BMAL1, EGR1, FOXC1, FOXO1, JUN, KLF11, NHLH2, NPAS2, NR3C1, PAX3, SP1, SRY
miRNA regulators (miRDB)
86 targeting MAOA, 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-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-33A-5P | 99.99 | 68.62 | 1055 |
| HSA-MIR-33B-5P | 99.99 | 68.58 | 1062 |
| HSA-MIR-302C-5P | 99.97 | 72.56 | 3642 |
| HSA-MIR-5688 | 99.96 | 73.23 | 4504 |
| HSA-MIR-495-3P | 99.96 | 72.81 | 4197 |
| HSA-MIR-551B-5P | 99.96 | 71.28 | 3493 |
| HSA-MIR-590-3P | 99.96 | 74.34 | 6478 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-205-3P | 99.92 | 69.92 | 3165 |
| HSA-MIR-3919 | 99.87 | 69.45 | 2489 |
| HSA-MIR-5582-3P | 99.86 | 72.48 | 4221 |
| HSA-MIR-1323 | 99.83 | 69.89 | 2471 |
| HSA-MIR-6842-5P | 99.80 | 67.54 | 1587 |
| HSA-MIR-7110-5P | 99.80 | 67.84 | 1712 |
| HSA-MIR-200A-5P | 99.76 | 69.10 | 949 |
| HSA-MIR-200B-5P | 99.76 | 69.05 | 948 |
| HSA-MIR-3680-3P | 99.75 | 72.51 | 3095 |
| HSA-MIR-548O-3P | 99.74 | 69.30 | 2228 |
| HSA-MIR-132-3P | 99.73 | 70.56 | 1424 |
| HSA-MIR-212-3P | 99.73 | 70.65 | 1424 |
| HSA-MIR-1200 | 99.71 | 70.42 | 1838 |
| HSA-MIR-3059-5P | 99.70 | 69.93 | 2491 |
| HSA-MIR-1251-3P | 99.64 | 67.21 | 1408 |
| HSA-MIR-4310 | 99.59 | 68.84 | 2527 |
| HSA-MIR-6752-5P | 99.59 | 67.32 | 1243 |
| HSA-MIR-3136-3P | 99.57 | 66.59 | 781 |
| HSA-MIR-7155-3P | 99.57 | 66.48 | 794 |
| HSA-MIR-105-5P | 99.54 | 69.24 | 2060 |
| HSA-MIR-7853-5P | 99.54 | 69.30 | 2055 |
Functional genomics
ClinGen dosage: haploinsufficiency 3 (sufficient evidence), triplosensitivity 0 (no evidence). ClinGen Gene Dosage Map
Literature-anchored findings (GeneRIF, showing 40)
- Substrates but not inhibitors alter the redox potentials of monoamine oxidases. (PMID:11761322)
- Evidence for positive selection and population structure at the human MAO-A gene. (PMID:11805333)
- Analysis of conserved active site residues in monoamine oxidase A and B and their three-dimensional molecular modeling (PMID:11861643)
- study did not support the involvement of 5-HTTLPR, TPH, MAO-A, or DRD4 polymorphisms in mood disorders (PMID:11992558)
- possible association between the prophylactic efficacy of lithium in mood disorders and the following gene variants: catechol-O-methyltransferase (COMT) G158A, monoamine oxydase A (MAO-A) 30-bp repeat, G-protein beta 3-subunit (Gbeta3) C825T (PMID:11992559)
- possible influence of monoamine oxydase A (MAO-A), catechol-O-methyltransferase (COMT), serotonin receptor 2A (5-HT2A), dopamine receptor D2 (DRD2), and dopamine receptor D4 (DRD4) gene variants on timing of recurrence in mood disorders (PMID:11992560)
- No association exists between genetic variation at the MAOA locus and alcoholism in Chinese Han males in Taiwan. (PMID:11999895)
- a role for the MAO A promoter-region polymorphism in conferring risk for attention deficit hyperactivity disorder (PMID:12140786)
- Role of genotype in the cycle of violence in maltreated children: Maltreated children with a genotype conferring high levels of MAOA expression were less likely to develop antisocial problems (PMID:12161658)
- MAO-A promoter polymorphism is associated with Moclobemide response in depressed patients. (PMID:12163988)
- Single nucleotide polymorphism in smokers (PMID:12360111)
- spectrum and redox properties are altered by inhibitors (PMID:12445480)
- Case control analysis of the VNTR showed an association with a subgroup of children with comorbid conduct problems. (PMID:12497620)
- These findings suggest that the three-repeat allele of the MAOAuVNTR 30-bp polymorphism is not associated with impulsive and aggressive personality traits. (PMID:12554604)
- Investigation of possible ssociation of a T941G single nucleotide polymorphism with generalized anxiety disorder, panic disorder, or major depression showed an association with gneralized anxiety disorder only. (PMID:12555227)
- Comparison of male alcoholics to male normal controls for the frequencies of two-loci and three-loci haplotypes was statistically significant (PMID:12555234)
- MAO-A polymorphisms are associated with smoking behaviour (PMID:12563176)
- Mao-A gene promoter allele was found in panic disorder. (PMID:12607224)
- genotyped 16 subjects for the DRD4 and MAOA genes who had been scanned during the Attention Network Test (PMID:12773616)
- study shows that the monoamine oxidase A structure is “more flexible” than that of monoamine oxidase B and that clorgyline and pargyline inactivation increase structural stability of both enzymes (PMID:12777388)
- There was a weak association of MAOA in neuroticism only in males. The er was no significant interaction between COMT and MAOA. (PMID:12815746)
- In a study of 129 Chinese Han males neither antisocial alcoholism nor antisocial personality disorder is found to be associated with genetic variants of the MAO-A gene. (PMID:12824808)
- This study showed that the genetic polymorphism of MAOA-VNTR might affect the incidence of nausea induced by SSRIs. (PMID:12886034)
- Functional MAOA-uVNTR alleles may act as a genetic modifier of the severity of autism in males. (PMID:12919132)
- It is proposed that the FAD binding site in MAO A is quite similar to that in MAO B. Structural information in this review is used to explain previous studies on flavin analog incorporation into either MAO B or into MAO A. (PMID:14697881)
- polymorphism is associated with aggression in children (PMID:15024395)
- association between the monoamine oxidase A (MAO-A) gene and obesity. (PMID:15034227)
- lower expression of the MAOA variable number tandem repeat polymorphism is related to a history of early abuse and may sensitize males, but not females, to the effects of early abuse experiences on impulsive traits in adulthood (PMID:15150530)
- There was no evidence of epistatic interaction between MAOA, MOAB, and COMT genes on Overt aggression scale scores. (PMID:15211623)
- our results do not confirm the hypothesis that there is a simple correlation between single gene polymorphisms in monoamine oxidase A and personality traits measurement (PMID:15292674)
- These data suggest that the EcoRV and uVNTR polymorphisms may be involved in the pathogenesis of major depression and associated with insomnia in depressed patients. (PMID:15486489)
- evidence in support of interaction between the MAOA and serotonin transporter (SERT) genes in 114 anorexia nervosa nuclear families (patient with AN plus biological parents) (PMID:15523490)
- monoamine oxidase A has a stable tyrosyl radical (PMID:15556933)
- MAOA gene variation may modulate the expression of some clinical aspects of severe mood disorders. (PMID:15564894)
- High-activity MAOA promoter gene polymorphisms, as in aging, are a risk factor for telomeric shortening. (PMID:15722955)
- This study findings further support the notion that allelic variation of MAOA activity contributes modestly to the balance of hyper- (impulsive-aggressive) and hyporeactive (anxious-depressive) traits. (PMID:15870836)
- Monoamine oxidase A polymorphism could play a role in susceptibility to alcoholism, which may differ across sexes. (PMID:15900229)
- This study findings suggest that the MAOA-uVNTR may be involved in the pathogenesis of major depressive disorder and the antidepressant therapeutic mechanisms in Chinese population, and that there may be a gender effect in this association. (PMID:15956990)
- present study strongly supports the notion that carrying the 3-repeat allele of the MAO-A-gene promoter increases the risk of male adolescent criminal behavior, when interacting with psychosocial factors. (PMID:16125147)
- important component of the active site structure of hMAO A is the loop conformation of residues 210-216, which differs from that of hMAO B and rat MAO A (PMID:16129825)
Cross-species orthologs
11 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| mus_musculus | Maoa | ENSMUSG00000025037 |
| rattus_norvegicus | Maoa | ENSRNOG00000002848 |
| drosophila_melanogaster | CG10561 | FBGN0002036 |
| drosophila_melanogaster | CG7737 | FBGN0033584 |
| drosophila_melanogaster | CG5653 | FBGN0035943 |
| drosophila_melanogaster | CG7460 | FBGN0036749 |
| drosophila_melanogaster | CG6034 | FBGN0036750 |
| drosophila_melanogaster | CG8032 | FBGN0037606 |
| drosophila_melanogaster | shps | FBGN0286199 |
| caenorhabditis_elegans | spr-5 | WBGENE00005010 |
| caenorhabditis_elegans | WBGENE00011615 |
Paralogs (7): KDM1A (ENSG00000004487), MAOB (ENSG00000069535), SMOX (ENSG00000088826), IL4I1 (ENSG00000104951), PPOX (ENSG00000143224), PAOX (ENSG00000148832), KDM1B (ENSG00000165097)
Protein
Protein identifiers
Amine oxidase [flavin-containing] A — P21397 (reviewed: P21397)
Alternative names: Monoamine oxidase type A
All UniProt accessions (4): A0A8I5KP93, A0A8I5KUC3, P21397, Q53YE7
UniProt curated annotations — full annotation on UniProt →
Function. Catalyzes the oxidative deamination of primary and some secondary amine such as neurotransmitters, with concomitant reduction of oxygen to hydrogen peroxide and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. Preferentially oxidizes serotonin. Also catalyzes the oxidative deamination of kynuramine to 3-(2-aminophenyl)-3-oxopropanal that can spontaneously condense to 4-hydroxyquinoline.
Subunit / interactions. Monomer, homo- or heterodimer (containing two subunits of similar size). Each subunit contains a covalently bound flavin. Enzymatically active as monomer.
Subcellular location. Mitochondrion outer membrane.
Tissue specificity. Heart, liver, duodenum, blood vessels and kidney.
Disease relevance. Brunner syndrome (BRNRS) [MIM:300615] A form of X-linked non-dysmorphic mild intellectual disability. Male patients are affected by borderline intellectual deficit and exhibit abnormal behavior, including disturbed regulation of impulsive aggression. Obligate female carriers have normal intelligence and behavior. The disease is caused by variants affecting the gene represented in this entry.
Polymorphism. A polymorphism 1.2 kb upstream of the MAOA coding sequences consists of a 30-bp repeated sequence present in 3, 3.5, 4, or 5 copies. The polymorphism affect transcriptional activity of the MAOA gene promoter. Alleles with 3.5 or 4 copies of the repeat sequence are transcribed 2 to 10 times more efficiently than those with 3 or 5 copies of the repeat.
Similarity. Belongs to the flavin monoamine oxidase family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| P21397-1 | 1 | yes |
| P21397-2 | 2 |
RefSeq proteins (2): NP_000231, NP_001257387 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR001613 | Flavin_amine_oxidase | Family |
| IPR002937 | Amino_oxidase | Domain |
| IPR036188 | FAD/NAD-bd_sf | Homologous_superfamily |
| IPR050703 | Flavin_MAO | Family |
Pfam: PF01593
Enzyme classification (BRENDA):
- EC 1.4.3.4 — monoamine oxidase (BRENDA: 65 organisms, 330 substrates, 1539 inhibitors, 310 Km, 144 kcat entries)
Substrate kinetics (BRENDA)
66 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| BENZYLAMINE | 0.0109–82 | 43 |
| KYNURAMINE | 0.0161–5.123 | 27 |
| SEROTONIN | 0.069–4.7 | 26 |
| 2-PHENYLETHYLAMINE | 0.016–86 | 25 |
| PHENYLETHYLAMINE | 0.0004–6.34 | 18 |
| TRYPTAMINE | 0.0185–5.1 | 12 |
| TYRAMINE | 0.018–6.14 | 12 |
| 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE | 0.033–0.797 | 8 |
| 4-TYRAMINE | 0.83–5.5 | 6 |
| 4-[(1R)-2-AMINO-1-HYDROXYETHYL]BENZENE-1,2-DIOL | 0.57–3.5 | 6 |
| DOPAMINE | 0.088–4.71 | 6 |
| N-METHYLHISTAMINE | 0.29–7.5 | 6 |
| O2 | 0.0093–0.33 | 5 |
| P-NITROPHENYLETHYLAMINE | 0.005–0.22 | 5 |
| (S)-1,2,3,4-TETRAHYDRO-1-METHYLISOQUINOLINE | 1.12–1.96 | 4 |
Catalyzed reactions (Rhea), 10 shown:
- a primary methyl amine + O2 + H2O = an aldehyde + H2O2 + NH4(+) (RHEA:16153)
- 2-phenylethylamine + O2 + H2O = 2-phenylacetaldehyde + H2O2 + NH4(+) (RHEA:25265)
- a secondary aliphatic amine + O2 + H2O = a primary amine + an aldehyde + H2O2 (RHEA:26414)
- dopamine + O2 + H2O = 3,4-dihydroxyphenylacetaldehyde + H2O2 + NH4(+) (RHEA:27946)
- tyramine + O2 + H2O = (4-hydroxyphenyl)acetaldehyde + H2O2 + NH4(+) (RHEA:30591)
- (R)-adrenaline + O2 + H2O = (R)-3,4-dihydroxymandelaldehyde + methylamine + H2O2 (RHEA:51168)
- tryptamine + O2 + H2O = indole-3-acetaldehyde + H2O2 + NH4(+) (RHEA:59416)
- kynuramine + O2 + H2O = 3-(2-aminophenyl)-3-oxopropanal + H2O2 + NH4(+) (RHEA:59596)
- serotonin + O2 + H2O = (5-hydroxyindol-3-yl)acetaldehyde + H2O2 + NH4(+) (RHEA:69072)
- (R)-noradrenaline + O2 + H2O = (R)-3,4-dihydroxymandelaldehyde + H2O2 + NH4(+) (RHEA:69076)
UniProt features (79 total): strand 26, helix 24, mutagenesis site 8, sequence variant 5, turn 4, modified residue 3, topological domain 2, site 2, chain 1, splice variant 1, transmembrane region 1, sequence conflict 1, region of interest 1
Structure
Experimental structures (PDB)
4 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 2Z5Y | X-RAY DIFFRACTION | 2.17 |
| 2Z5X | X-RAY DIFFRACTION | 2.2 |
| 2BXR | X-RAY DIFFRACTION | 3 |
| 2BXS | X-RAY DIFFRACTION | 3.15 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-P21397-F1 | 97.09 | 0.97 |
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): 335 (important for substrate specificity); 374 (important for catalytic activity)
Post-translational modifications (3): 1, 383, 406
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 165 | no loss of activity. |
| 266 | no loss of activity. |
| 306 | no loss of activity. |
| 321 | no loss of activity. |
| 323 | no loss of activity. |
| 374 | complete loss of activity. |
| 398 | no loss of activity. |
| 406 | complete loss of activity. |
Function
Pathways and Gene Ontology
Reactome pathways
23 pathways
| ID | Pathway |
|---|---|
| R-HSA-141333 | Biogenic amines are oxidatively deaminated to aldehydes by MAOA and MAOB |
| R-HSA-181430 | Norepinephrine Neurotransmitter Release Cycle |
| R-HSA-379397 | Enzymatic degradation of dopamine by COMT |
| R-HSA-379398 | Enzymatic degradation of Dopamine by monoamine oxidase |
| R-HSA-379401 | Dopamine clearance from the synaptic cleft |
| R-HSA-380612 | Metabolism of serotonin |
| R-HSA-5579012 | Defective MAOA causes BRUNS |
| R-HSA-6785807 | Interleukin-4 and Interleukin-13 signaling |
| R-HSA-112310 | Neurotransmitter release cycle |
| R-HSA-112311 | Neurotransmitter clearance |
| R-HSA-112315 | Transmission across Chemical Synapses |
| R-HSA-112316 | Neuronal System |
| R-HSA-1280215 | Cytokine Signaling in Immune system |
| R-HSA-140179 | Amine Oxidase reactions |
| R-HSA-1430728 | Metabolism |
| R-HSA-1643685 | Disease |
| R-HSA-168256 | Immune System |
| R-HSA-211859 | Biological oxidations |
| R-HSA-211945 | Phase I - Functionalization of compounds |
| R-HSA-380615 | Serotonin clearance from the synaptic cleft |
| R-HSA-449147 | Signaling by Interleukins |
| R-HSA-5579029 | Metabolic disorders of biological oxidation enzymes |
| R-HSA-5668914 | Diseases of metabolism |
MSigDB gene sets: 346 (showing top):
GOBP_PHENOL_CONTAINING_COMPOUND_METABOLIC_PROCESS, MODULE_93, KOBAYASHI_EGFR_SIGNALING_24HR_UP, REACTOME_BIOLOGICAL_OXIDATIONS, GRUETZMANN_PANCREATIC_CANCER_DN, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOZGIT_ESR1_TARGETS_DN, MODULE_563, MODULE_445, GAUSSMANN_MLL_AF4_FUSION_TARGETS_A_UP, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, SABATES_COLORECTAL_ADENOMA_SIZE_DN, BROWNE_HCMV_INFECTION_16HR_UP, SARRIO_EPITHELIAL_MESENCHYMAL_TRANSITION_DN, CHX10_01
GO Biological Process (5): biogenic amine metabolic process (GO:0006576), positive regulation of signal transduction (GO:0009967), dopamine catabolic process (GO:0042420), serotonin catabolic process (GO:0042429), catecholamine metabolic process (GO:0006584)
GO Molecular Function (5): primary methylamine oxidase activity (GO:0008131), flavin adenine dinucleotide binding (GO:0050660), monoamine oxidase activity (GO:0097621), protein binding (GO:0005515), oxidoreductase activity (GO:0016491)
GO Cellular Component (4): mitochondrion (GO:0005739), mitochondrial outer membrane (GO:0005741), cytosol (GO:0005829), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-13 pathways:
| Category | Pathways |
|---|---|
| Dopamine clearance from the synaptic cleft | 2 |
| Neurotransmitter clearance | 2 |
| Transmission across Chemical Synapses | 2 |
| Amine Oxidase reactions | 1 |
| Neurotransmitter release cycle | 1 |
| Serotonin clearance from the synaptic cleft | 1 |
| Metabolic disorders of biological oxidation enzymes | 1 |
| Signaling by Interleukins | 1 |
| Neuronal System | 1 |
| Immune System | 1 |
| Phase I - Functionalization of compounds | 1 |
| Metabolism | 1 |
| Biological oxidations | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| oxidoreductase activity, acting on the CH-NH2 group of donors, oxygen as acceptor | 2 |
| cytoplasm | 2 |
| cellular anatomical structure | 2 |
| amine metabolic process | 1 |
| signal transduction | 1 |
| regulation of signal transduction | 1 |
| positive regulation of cell communication | 1 |
| positive regulation of signaling | 1 |
| positive regulation of response to stimulus | 1 |
| dopamine metabolic process | 1 |
| catecholamine catabolic process | 1 |
| phenol-containing compound catabolic process | 1 |
| serotonin metabolic process | 1 |
| indole-containing compound catabolic process | 1 |
| primary amino compound catabolic process | 1 |
| biogenic amine metabolic process | 1 |
| catechol-containing compound metabolic process | 1 |
| nucleotide binding | 1 |
| anion binding | 1 |
| binding | 1 |
| catalytic activity | 1 |
| intracellular membrane-bounded organelle | 1 |
| mitochondrial membrane | 1 |
| organelle outer membrane | 1 |
Protein interactions and networks
STRING
3226 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| MAOA | COMT | P21964 | 964 |
| MAOA | SLC6A4 | P31645 | 943 |
| MAOA | TOMT | Q8WZ04 | 894 |
| MAOA | DRD4 | P21917 | 893 |
| MAOA | SLC6A3 | Q01959 | 890 |
| MAOA | DBH | P09172 | 877 |
| MAOA | DDC | P20711 | 864 |
| MAOA | HTR1A | P08908 | 862 |
| MAOA | AOC2 | O75106 | 798 |
| MAOA | SLC18A2 | Q05940 | 793 |
| MAOA | HTR2A | P28223 | 787 |
| MAOA | TH | P07101 | 786 |
| MAOA | ALDH2 | P05091 | 781 |
| MAOA | BCHE | P06276 | 745 |
| MAOA | ACHE | P22303 | 745 |
IntAct
31 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MAOA | MAOB | psi-mi:“MI:0915”(physical association) | 0.670 |
| MAOA | MAOB | psi-mi:“MI:0914”(association) | 0.670 |
| ARL4C | RGS12 | psi-mi:“MI:0914”(association) | 0.640 |
| ASPH | STXBP3 | psi-mi:“MI:0914”(association) | 0.640 |
| CDK5RAP3 | PLD2 | psi-mi:“MI:0914”(association) | 0.530 |
| CENPH | PSMD11 | psi-mi:“MI:0914”(association) | 0.530 |
| LPAR1 | TMEM223 | psi-mi:“MI:0914”(association) | 0.530 |
| PAEP | PROS1 | psi-mi:“MI:0914”(association) | 0.530 |
| NDRG1 | MAOA | psi-mi:“MI:0915”(physical association) | 0.400 |
| MAOA | psi-mi:“MI:0915”(physical association) | 0.400 | |
| APBB1 | SSPOP | psi-mi:“MI:0914”(association) | 0.350 |
| COQ9 | NDUFS8 | psi-mi:“MI:0914”(association) | 0.350 |
| COQ9 | ACOT7 | psi-mi:“MI:0914”(association) | 0.350 |
| MAPT | SHTN1 | psi-mi:“MI:0914”(association) | 0.350 |
| WNT2B | PGRMC2 | psi-mi:“MI:0914”(association) | 0.350 |
| MTCH2 | IPO5 | psi-mi:“MI:0914”(association) | 0.350 |
| ARMC6 | DDX39A | psi-mi:“MI:0914”(association) | 0.350 |
| CHRNA3 | ENTPD6 | psi-mi:“MI:0914”(association) | 0.350 |
| GDPD5 | TMEM120B | psi-mi:“MI:0914”(association) | 0.350 |
| HPN | DDX39A | psi-mi:“MI:0914”(association) | 0.350 |
| MAGEA8 | B4GALT5 | psi-mi:“MI:0914”(association) | 0.350 |
| PACC1 | IPO5 | psi-mi:“MI:0914”(association) | 0.350 |
| SAAL1 | TMEM223 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC39A14 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| SLC7A1 | ESYT2 | psi-mi:“MI:0914”(association) | 0.350 |
| A2M | TPP1 | psi-mi:“MI:0403”(colocalization) | 0.350 |
| CDH5 | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.270 |
BioGRID (25): MAOA (Affinity Capture-MS), MAOB (Affinity Capture-MS), MIEF1 (Affinity Capture-MS), MAOA (Affinity Capture-RNA), MAOA (Affinity Capture-MS), MAOB (Proximity Label-MS), MAOA (Proximity Label-MS), MAOA (Proximity Label-MS), MAOA (Affinity Capture-MS), MAOA (Affinity Capture-MS), MAOA (Proximity Label-MS), MAOB (Affinity Capture-MS), MIEF1 (Affinity Capture-MS), MAOA (Affinity Capture-MS), MAOA (Proximity Label-MS)
ESM2 similar proteins: A0A0P0XM10, A0A2U8QPE6, A6MFL0, A8QL51, A8QL52, A8QL58, B0VXW0, B5AR80, B5U6Y8, G8XQX1, J7H670, O64411, P0C2D5, P0DO52, P19643, P21396, P21397, P21398, P23623, P27338, P49253, P54982, P56560, P57681, P58027, P58028, P81382, P81383, P86810, Q0J290, Q4JHE1, Q4JHE2, Q4JHE3, Q5NU32, Q5R748, Q5RE60, Q5RE98, Q64133, Q6NSN2, Q6PLK3
Diamond homologs: A0A024BTN9, A0A2U8QPE6, A2XDA1, A6MFL0, A8QL51, A8QL52, A8QL58, B0VXW0, B5AR80, B5U6Y8, C0HJE7, C3VEP9, C3VEQ0, F8S0Z5, G8XQX1, J7H670, K9N7B7, O09046, O49901, O93364, P0C2D5, P0CC17, P0DI84, P0DPS2, P19643, P21397, P26294, P27338, P28553, P28554, P29273, P40974, P49086, P56560, P56742, P58027, P58028, P74306, P80093, P81382
SIGNOR signaling
9 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| MAOA | “down-regulates quantity” | 3-methoxytyramine | “chemical modification” |
| MAOA | “down-regulates quantity” | dopamine | “chemical modification” |
| MAOA | “up-regulates quantity” | 3,4-dihydroxyphenylacetaldehyde | “chemical modification” |
| MAOA | “down-regulates quantity” | serotonin | “chemical modification” |
| MAOA | “up-regulates quantity” | (R)-adrenaline | “chemical modification” |
| MAOA | “up-regulates quantity” | (R)-noradrenaline | “chemical modification” |
| NHLH2 | “up-regulates quantity by expression” | MAOA | “transcriptional regulation” |
| Phenelzine | “down-regulates activity” | MAOA | “chemical inhibition” |
| moclobemide | “down-regulates activity” | MAOA | “chemical inhibition” |
Disease & clinical
Clinical variants and AI predictions
ClinVar
334 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 11 |
| Likely pathogenic | 10 |
| Uncertain significance | 131 |
| Likely benign | 71 |
| Benign | 11 |
Top pathogenic / likely-pathogenic (21)
| Variant ID | HGVS | Classification |
|---|---|---|
| 1071006 | NC_000023.10:g.(?43515570)(43603780_?)del | Pathogenic |
| 1074868 | NM_000240.4(MAOA):c.1214del (p.Gly405fs) | Pathogenic |
| 139432 | NM_000240.4(MAOA):c.797G>T (p.Cys266Phe) | Pathogenic |
| 146001 | GRCh38/hg38 Xp11.3(chrX:43640608-44123496)x2 | Pathogenic |
| 208352 | NM_000240.4(MAOA):c.749_750insT (p.Ser251fs) | Pathogenic |
| 2422624 | NC_000023.10:g.(?43515590)(43817891_?)del | Pathogenic |
| 3237494 | NM_000240.4(MAOA):c.290_303del (p.Leu97fs) | Pathogenic |
| 451098 | NM_000240.4(MAOA):c.1263-2A>G | Pathogenic |
| 4624227 | NM_000240.4(MAOA):c.1183A>T (p.Lys395Ter) | Pathogenic |
| 685032 | GRCh37/hg19 Xp11.4-11.3(chrX:42165435-43684005)x0 | Pathogenic |
| 9967 | NM_000240.4(MAOA):c.886C>T (p.Gln296Ter) | Pathogenic |
| 2571364 | NM_000240.4(MAOA):c.166del (p.Arg56fs) | Likely pathogenic |
| 3256735 | NM_000240.4(MAOA):c.1180G>C (p.Glu394Gln) | Likely pathogenic |
| 3600474 | NM_000240.4(MAOA):c.11_12del (p.Gln4fs) | Likely pathogenic |
| 3659338 | NM_000240.4(MAOA):c.73+1G>C | Likely pathogenic |
| 4051008 | NM_000240.4(MAOA):c.83del (p.Ala28fs) | Likely pathogenic |
| 4074827 | NM_000240.4(MAOA):c.796-1G>T | Likely pathogenic |
| 4082335 | NM_000240.4(MAOA):c.1420C>T (p.Gln474Ter) | Likely pathogenic |
| 431096 | NM_000240.4(MAOA):c.730G>A (p.Val244Ile) | Likely pathogenic |
| 4820104 | NM_000240.4(MAOA):c.1075del (p.Asp359fs) | Likely pathogenic |
| 992787 | NM_000240.4(MAOA):c.233dup (p.Leu78fs) | Likely pathogenic |
SpliceAI
2081 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| X:43656410:TTCAG:T | donor_loss | 1.0000 |
| X:43656411:TCAG:T | donor_loss | 1.0000 |
| X:43656415:G:A | donor_loss | 1.0000 |
| X:43656416:T:G | donor_loss | 1.0000 |
| X:43657964:TGGA:T | donor_gain | 1.0000 |
| X:43657965:GGAG:G | donor_gain | 1.0000 |
| X:43657968:GA:G | donor_gain | 1.0000 |
| X:43657970:G:GG | donor_gain | 1.0000 |
| X:43657980:G:GT | donor_gain | 1.0000 |
| X:43683507:CTTTA:C | acceptor_loss | 1.0000 |
| X:43683508:TTTA:T | acceptor_loss | 1.0000 |
| X:43683509:TTA:T | acceptor_loss | 1.0000 |
| X:43683511:A:AG | acceptor_gain | 1.0000 |
| X:43683511:A:G | acceptor_loss | 1.0000 |
| X:43683511:AG:A | acceptor_gain | 1.0000 |
| X:43683512:G:GA | acceptor_gain | 1.0000 |
| X:43683512:GG:G | acceptor_gain | 1.0000 |
| X:43683512:GGA:G | acceptor_gain | 1.0000 |
| X:43683512:GGACT:G | acceptor_gain | 1.0000 |
| X:43683604:AAGGG:A | donor_loss | 1.0000 |
| X:43683605:AGGG:A | donor_loss | 1.0000 |
| X:43683606:GG:G | donor_gain | 1.0000 |
| X:43683607:GG:G | donor_gain | 1.0000 |
| X:43683607:GGTA:G | donor_loss | 1.0000 |
| X:43683608:G:GG | donor_gain | 1.0000 |
| X:43683608:GTAA:G | donor_loss | 1.0000 |
| X:43683609:T:TC | donor_loss | 1.0000 |
| X:43693286:TGCAG:T | acceptor_loss | 1.0000 |
| X:43693288:CAGAA:C | acceptor_loss | 1.0000 |
| X:43693289:A:AG | acceptor_gain | 1.0000 |
AlphaMissense
3451 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| X:43731245:G:C | R217P | 0.999 |
| X:43731841:T:A | W315R | 0.999 |
| X:43731841:T:C | W315R | 0.999 |
| X:43741974:T:A | W397R | 0.999 |
| X:43741974:T:C | W397R | 0.999 |
| X:43683592:A:C | R51S | 0.998 |
| X:43683592:A:T | R51S | 0.998 |
| X:43731813:G:C | K305N | 0.998 |
| X:43731813:G:T | K305N | 0.998 |
| X:43741976:G:C | W397C | 0.998 |
| X:43741976:G:T | W397C | 0.998 |
| X:43742003:C:G | C406W | 0.998 |
| X:43743852:T:A | W441R | 0.998 |
| X:43743852:T:C | W441R | 0.998 |
| X:43743892:G:C | R454P | 0.998 |
| X:43683591:G:C | R51T | 0.997 |
| X:43728238:C:T | S190F | 0.997 |
| X:43728314:G:C | Q215H | 0.997 |
| X:43728314:G:T | Q215H | 0.997 |
| X:43731326:T:A | V244D | 0.997 |
| X:43731811:A:G | K305E | 0.997 |
| X:43732794:G:C | G351R | 0.997 |
| X:43743829:C:A | A433E | 0.997 |
| X:43743859:G:A | G443D | 0.997 |
| X:43743882:G:C | A451P | 0.997 |
| X:43693324:G:C | A68P | 0.996 |
| X:43731843:G:C | W315C | 0.996 |
| X:43731843:G:T | W315C | 0.996 |
| X:43732795:G:A | G351D | 0.996 |
| X:43736228:T:C | F352L | 0.996 |
dbSNP variants (sampled 300 via entrez): RS1000048725 (X:43678067 A>G), RS1000068610 (X:43679327 G>A), RS1000105013 (X:43677222 C>T), RS1000215290 (X:43672042 C>G,T), RS1000373411 (X:43659534 C>G), RS1000379370 (X:43686516 A>C), RS1000405150 (X:43743282 A>G), RS1000406951 (X:43697930 C>G,T), RS1000411376 (X:43696856 G>A,T), RS1000427405 (X:43660022 T>A), RS1000527827 (X:43714638 G>A), RS1000557465 (X:43740939 C>T), RS1000710225 (X:43662209 A>G), RS1000712526 (X:43672398 AT>A), RS1000763950 (X:43663098 T>G)
Disease associations
OMIM: gene MIM:309850 | disease phenotypes: MIM:300615
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| Brunner syndrome | Definitive | X-linked |
ClinGen Gene-Disease Validity (1)
Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.
| Disease | Classification | Inheritance |
|---|---|---|
| Brunner syndrome | Definitive | XL |
Mondo (3): Brunner syndrome (MONDO:0010379), intellectual disability (MONDO:0001071), antisocial behavior, susceptibility to (MONDO:0800413)
Orphanet (2): Monoamine oxidase A deficiency (Orphanet:3057), NON RARE IN EUROPE: Unexplained intellectual disability (Orphanet:319658)
HPO phenotypes
14 total (14 of 14 shown, HPO-id order):
| HPO | Term |
|---|---|
| HP:0000708 | Atypical behavior |
| HP:0000717 | Autism |
| HP:0000718 | Aggressive behavior |
| HP:0000744 | Low frustration tolerance |
| HP:0001249 | Intellectual disability |
| HP:0001270 | Motor delay |
| HP:0001419 | X-linked recessive inheritance |
| HP:0002014 | Diarrhea |
| HP:0002315 | Headache |
| HP:0030186 | Kinetic tremor |
| HP:0031284 | Flushing |
| HP:0100543 | Cognitive impairment |
| HP:0100710 | Impulsivity |
| HP:0100716 | Self-injurious behavior |
GWAS associations
1 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST000349_8 | Smoking behavior | 7.000000e-06 |
EFO canonical traits (1, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004318 | smoking behavior |
MeSH disease descriptors (2)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008607 | Intellectual Disability | C10.597.606.360; C23.888.592.604.646; F01.700.687; F03.625.539 |
| C563156 | Brunner Syndrome (supp.) |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (2): CHEMBL1951 (SINGLE PROTEIN), CHEMBL2095205 (PROTEIN FAMILY)
Molecules with ChEMBL bioactivity
130 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 512,950 (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 |
|---|---|---|---|
| CHEMBL104 | CLOTRIMAZOLE | 4 | 56,325 |
| CHEMBL1070 | NABUMETONE | 4 | 55,063 |
| CHEMBL1079604 | METAXALONE | 4 | 5,021 |
| CHEMBL1089 | PHENELZINE | 4 | 18,793 |
| CHEMBL1112 | ARIPIPRAZOLE | 4 | 24,205 |
| CHEMBL1171837 | PONATINIB | 4 | 8,955 |
| CHEMBL1179047 | CHLOROPROCAINE | 4 | 52,577 |
| CHEMBL119 | TRIMETREXATE | 4 | 57,002 |
| CHEMBL1196 | PROPARACAINE | 4 | 12,973 |
| CHEMBL1200624 | ETHYNODIOL DIACETATE | 4 | 5,941 |
| CHEMBL1200904 | SELEGILINE HYDROCHLORIDE | 4 | 5,084 |
| CHEMBL1201142 | RASAGILINE MESYLATE | 4 | 716 |
| CHEMBL1201303 | PYRVINIUM | 4 | 1,797 |
| CHEMBL1206 | ETHOPROPAZINE | 4 | 15,984 |
| CHEMBL121 | ROSIGLITAZONE | 4 | 58,849 |
| CHEMBL1257051 | TEDIZOLID | 4 | 1,778 |
| CHEMBL126 | LINEZOLID | 4 | 27,339 |
| CHEMBL12713 | SERTINDOLE | 4 | 8,984 |
| CHEMBL1336 | SORAFENIB | 4 | 86,060 |
| CHEMBL1401 | NITAZOXANIDE | 4 | 9,504 |
| CHEMBL1448 | NICLOSAMIDE | 4 | |
| CHEMBL1475 | TRIOXSALEN | 4 | |
| CHEMBL1520 | VARDENAFIL | 4 | |
| CHEMBL1626223 | PYRANTEL | 4 | |
| CHEMBL169901 | DEBRISOQUIN | 4 | |
| CHEMBL18116 | TOLOXATONE | 4 | |
| CHEMBL1909286 | PHENOXYPROPAZINE | 4 | |
| CHEMBL191083 | METHYLENE BLUE CATION | 4 | |
| CHEMBL193 | NIFEDIPINE | 4 | |
| CHEMBL1946170 | REGORAFENIB | 4 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
2 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs1137070 | MAOA | 0.00 | 0 | ||
| rs979605 | MAOA | 0.00 | 0 |
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Catecholamine turnover
Most potent curated ligand interactions (9 total), top 9:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| moclobemide | Inhibition | 8.3 | pKi |
| harmaline | Inhibition | 7.48 | pIC50 |
| phenelzine | Irreversible inhibition | 7.33 | pKi |
| acacetin | Inhibition | 7.23 | pKi |
| CR4056 | Inhibition | 6.69 | pIC50 |
| bifemelane | Inhibition | 5.38 | pKi |
| tranylcypromine | Inhibition | 4.7 | pIC50 |
| linezolid | Inhibition | 4.34 | pIC50 |
| selegiline | Inhibition | 4.17 | pKi |
Binding affinities (BindingDB)
456 measured of 1162 human assays (1168 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| 1,4-Bis(2-pentanoylimino-5-(2-methoxy-2-oxoethylidene)-4-oxo-thiazolidin-3-yl)benzene (5a) | IC50 | 1 nM | |
| 3,4-dichloro-N-(1H-pyrrolo[3,2-b]pyridin-5-yl)benzamide | IC50 | 1.13 nM | US-9738640: Substituted benzamide derivatives as in vitro MAO-B inhibitors |
| tert-butyl N-[1-[3-[2-[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]ethynyl]azetidine-1-carbonyl]cyclopropyl]-N-methylcarbamate | IC50 | 2.3 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 2-[4-[2-[5-(4-acetylpiperazin-1-yl)-2-pyridinyl]ethyl]phenyl]acetohydrazide | IC50 | 3.2 nM | US-9603833: Benzene or thiophene derivative and use thereof as VAP-1 inhibitor |
| N-[4-[7-[2-[1-(cyclobutanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 4 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| CLG | IC50 | 4.5 nM | |
| N-[4-[7-[2-[1-(cyclopropanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 5 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(3-hydroxy-3-methylcyclobutanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 5 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(2,2-difluorocyclopropanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 5 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| tert-butyl N-[1-[3-[2-[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]ethynyl]azetidine-1-carbonyl]cyclopropyl]carbamate | IC50 | 5 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(3,3-difluorocyclobutanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 6 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(3-methyloxetane-3-carbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 6 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(1-methylcyclopropanecarbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 6 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| tert-butyl N-[1-[3-[2-[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]ethynyl]azetidine-1-carbonyl]cyclobutyl]carbamate | IC50 | 6 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(cyclopropanecarbonyl)piperidin-4-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 6.5 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[4-oxo-7-[2-(3-propan-2-ylimidazol-4-yl)ethynyl]chromen-3-yl]phenyl]methanesulfonamide | IC50 | 7 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 2-[4-[2-(2-piperazin-1-yl-4-pyridinyl)ethyl]phenyl]acetohydrazide | IC50 | 7.3 nM | US-9603833: Benzene or thiophene derivative and use thereof as VAP-1 inhibitor |
| [3-(2,3-Dichloro-phenoxy)-propyl]-methyl-prop-2-ynyl-amine (clorgyline) | IC50 | 7.7 nM | US-20250382276: COMPOUND, METHOD OF PREPARATION, COMPOSITION, AND USES THEREOF |
| N-[4-[7-[2-[1-(3-methoxypropanoyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 8 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1k | IC50 | 8.6 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1g | IC50 | 8.8 nM | |
| tert-butyl 3-[2-[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]ethynyl]azetidine-1-carboxylate | IC50 | 9 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[4-oxo-7-[2-(2-oxo-1H-pyridin-4-yl)ethynyl]chromen-3-yl]phenyl]methanesulfonamide | IC50 | 9 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| cyclopentyl 3-[2-[3-[4-(methanesulfonamido)phenyl]-4-oxochromen-7-yl]ethynyl]azetidine-1-carboxylate | IC50 | 9 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 1,2-Bis(2-(2-chlorobenzoylimino)-5-(2-methoxy-2-oxoethylidene)-4-oxo-thiazolidin-3-yl)benzene (3e) | IC50 | 9 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1a | IC50 | 9 nM | |
| 2-[4-[2-(6-piperazin-1-yl-2-pyridinyl)ethyl]phenyl]acetohydrazide | IC50 | 9.8 nM | US-9603833: Benzene or thiophene derivative and use thereof as VAP-1 inhibitor |
| 7-[(4-Cyanobenzyl)oxy]-3,4-dihydronaphthalen-1(2H)-one (4m) | IC50 | 10 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1m | IC50 | 10 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1e | IC50 | 10 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1j | IC50 | 10 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 3c | IC50 | 10 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 3d | IC50 | 10 nM | |
| 4-chloro-3-fluoro-N-(1H-pyrrolo[3,2-b]pyridin-5-yl)benzamide | IC50 | 10.9 nM | US-9738640: Substituted benzamide derivatives as in vitro MAO-B inhibitors |
| 7-[(4-Fluorobenzyl)oxy]-3,4-dihydronaphthalen-1(2H)-one (4e) | IC50 | 12 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 2i | IC50 | 14 nM | |
| N-[4-[7-[2-(2,3-dimethylimidazol-4-yl)ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 15 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(2-hydroxyacetyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 15 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(2-hydroxypropanoyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 15 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-[1-(2-hydroxy-2-methylpropanoyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 16 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[4-oxo-7-(2-pyridin-3-ylethynyl)chromen-3-yl]phenyl]methanesulfonamide | IC50 | 21 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 2-chloro-6-methyl-N-[[4-(2-oxo-1H-pyridin-4-yl)phenyl]methyl]benzamide | IC50 | 23 nM | US-9000015: Compounds for the treatment of addiction |
| 2,6-dichloro-N-[[4-(5-fluoro-2-oxo-1H-pyridin-4-yl)phenyl]methyl]benzamide | IC50 | 25 nM | US-9000015: Compounds for the treatment of addiction |
| 7-[(3-Cyanobenzyl)oxy]-3,4-dihydronaphthalen-1(2H)-one (4l) | IC50 | 26 nM | |
| 4,5-Dihydro-(1H)-pyrazole derivative, 1f | IC50 | 28 nM | |
| 7-[(4-Chlorobenzyl)oxy]-3,4-dihydronaphthalen-1(2H)-one (4g) | IC50 | 33 nM | |
| 7-[(4-Bromobenzyl)oxy]-3,4-dihydronaphthalen-1(2H)-one (4i) | IC50 | 34 nM | |
| N-[4-[7-[2-[1-(1-methylpiperidine-4-carbonyl)azetidin-3-yl]ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 35 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| N-[4-[7-[2-(oxan-4-yl)ethynyl]-4-oxochromen-3-yl]phenyl]methanesulfonamide | IC50 | 43 nM | US-8673966: ALDH-2 inhibitors in the treatment of addiction |
| 3,4-difluoro-N-(1H-pyrrolo[3,2-b]pyridin-5-yl)benzamide | IC50 | 46.1 nM | US-9738640: Substituted benzamide derivatives as in vitro MAO-B inhibitors |
ChEMBL bioactivities
2623 potent at pChembl≥5 of 4490 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 10.85 | Ki | 0.014 | nM | CHEMBL5271774 |
| 10.00 | IC50 | 0.1 | nM | CHEMBL209413 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5269241 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5283319 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5276967 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5272518 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5291452 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5280524 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5272772 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5271570 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5268306 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5273835 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5284012 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5275680 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5290358 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5284128 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5282135 |
| 10.00 | Ki | 0.1 | nM | CHEMBL5270226 |
| 9.57 | IC50 | 0.27 | nM | CHEMBL1929421 |
| 9.52 | Ki | 0.3 | nM | CLORGILINE |
| 9.52 | IC50 | 0.3 | nM | CHEMBL1929421 |
| 9.46 | Ki | 0.346 | nM | CHEMBL5270286 |
| 9.41 | IC50 | 0.389 | nM | CHEMBL3319256 |
| 9.40 | IC50 | 0.4 | nM | CHEMBL5178014 |
| 9.32 | Ki | 0.48 | nM | CHEMBL4104691 |
| 9.30 | Ki | 0.5 | nM | MOCLOBEMIDE |
| 9.30 | IC50 | 0.5 | nM | CLORGILINE |
| 9.21 | IC50 | 0.61 | nM | CLORGILINE |
| 9.18 | IC50 | 0.6607 | nM | CHEMBL4061639 |
| 9.15 | IC50 | 0.7 | nM | CHEMBL1256153 |
| 9.14 | IC50 | 0.72 | nM | CHEMBL3415804 |
| 9.08 | IC50 | 0.83 | nM | CHEMBL1651055 |
| 9.07 | IC50 | 0.85 | nM | CHEMBL3415795 |
| 9.05 | Ki | 0.8913 | nM | CHEMBL14640 |
| 9.00 | IC50 | 1 | nM | CHEMBL3415817 |
| 9.00 | IC50 | 1 | nM | CLORGILINE |
| 9.00 | Ki | 1 | nM | CHEMBL4748517 |
| 9.00 | Ki | 1 | nM | CHEMBL4787516 |
| 9.00 | Ki | 1 | nM | CHEMBL4761363 |
| 9.00 | Ki | 1 | nM | CHEMBL4757953 |
| 9.00 | Ki | 1 | nM | CHEMBL4787184 |
| 9.00 | Ki | 1 | nM | CHEMBL4762228 |
| 9.00 | IC50 | 1 | nM | HARMINE |
| 9.00 | Ki | 1 | nM | HARMINE |
| 8.97 | IC50 | 1.06 | nM | CLORGILINE |
| 8.96 | IC50 | 1.1 | nM | CLORGILINE |
| 8.92 | IC50 | 1.2 | nM | CLORGILINE |
| 8.89 | IC50 | 1.29 | nM | CHEMBL1482039 |
| 8.85 | IC50 | 1.4 | nM | CHEMBL3415783 |
| 8.84 | IC50 | 1.445 | nM | CHEMBL3319257 |
PubChem BioAssay actives
1242 with measured affinity, of 6100 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 |
|---|---|---|---|---|
| 2-[2-(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)-2-oxoethyl]propanedinitrile | 1930190: Inhibition of human MAO-A | ki | <0.0001 | uM |
| N-ethyl-3-(4-fluorophenyl)-5-phenyl-3,4-dihydropyrazole-2-carbothioamide | 1961157: Inhibition of human MAO-A by spectrofluorimetric analysis | ki | 0.0001 | uM |
| 8-methoxy-3-[3-(trifluoromethyl)phenyl]indeno[1,2-c]pyridazin-5-one | 266327: Inhibition of MAO-B in baboon liver mitochondria | ic50 | 0.0001 | uM |
| 3-(4-fluorophenyl)-N,5-diphenyl-3,4-dihydropyrazole-2-carbothioamide | 1961157: Inhibition of human MAO-A by spectrofluorimetric analysis | ki | 0.0001 | uM |
| N-[4-chloro-3-[3-[methyl(prop-2-ynyl)amino]propoxy]phenyl]-N’-hydroxydecanediamide | 1900906: Inhibition of MAO-A (unknown origin) expressed in mouse GL26 cells using 14C 5-hydroxytryptamine as substrate pre-incubated for 20 mins followed by substrate addition measured after 20 mins by liquid scintillation spectroscopy | ic50 | 0.0001 | uM |
| 2-amino-5-(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)furan-3-carbonitrile | 1930190: Inhibition of human MAO-A | ki | 0.0003 | uM |
| 4-[[4-chloro-3-[3-[methyl(prop-2-ynyl)amino]propoxy]anilino]methyl]-N-hydroxybenzamide | 1900906: Inhibition of MAO-A (unknown origin) expressed in mouse GL26 cells using 14C 5-hydroxytryptamine as substrate pre-incubated for 20 mins followed by substrate addition measured after 20 mins by liquid scintillation spectroscopy | ic50 | 0.0004 | uM |
| 2-(furan-3-yl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0007 | uM |
| 2-(4-bromophenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;hydrochloride | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0008 | uM |
| 11-methoxy-16-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2,4,6,9(17),10,12,14-octaen-8-one | 629007: Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay | ic50 | 0.0008 | uM |
| 2-(phenoxymethyl)-4,5-dihydro-1H-imidazole | 223245: Displacement of [3H]idazoxan from imidazoline receptor I-2 binding sites in rabbit kidney membrane | ki | 0.0009 | uM |
| methyl (2Z)-2-[3-[4-[(5Z)-5-(2-methoxy-2-oxoethylidene)-4-oxo-2-pentanoylimino-1,3-thiazolidin-3-yl]phenyl]-4-oxo-2-pentanoylimino-1,3-thiazolidin-5-ylidene]acetate | 1802510: In-vitro Monoamine Oxidase Inhibition Assay from Article 10.1016/j.bioorg.2016.11.004: “Symmetrical aryl linked bis-iminothiazolidinones as new chemical entities for the inhibition of monoamine oxidases: Synthesis, in vitro biological evaluation and molecular modelling analysis.” | ic50 | 0.0010 | uM |
| 2-(3,4-dichlorophenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0010 | uM |
| 3-[2-[3-(2-chlorophenyl)-5-(4-methoxyphenyl)-3,4-dihydropyrazol-2-yl]-2-oxoethyl]-1,3-benzoxazol-2-one | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| N-[(E)-[(E)-3-(2-chlorophenyl)-1-(4-methoxyphenyl)prop-2-enylidene]amino]-2-(2-oxo-1,3-benzoxazol-3-yl)acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| N-[(E)-[(E)-3-(3-methoxyphenyl)-1-phenylprop-2-enylidene]amino]-2-(2-oxo-1,3-benzoxazol-3-yl)acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| 2-(5-chloro-2-oxo-1,3-benzoxazol-3-yl)-N-[(E)-[(E)-3-(2-chlorophenyl)-1-(2-methoxyphenyl)prop-2-enylidene]amino]acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| 2-(5-chloro-2-oxo-1,3-benzoxazol-3-yl)-N-[(E)-[(E)-3-(2-methoxyphenyl)-1-phenylprop-2-enylidene]amino]acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| N-[(E)-[(E)-1,3-diphenylprop-2-enylidene]amino]-2-(2-oxo-1,3-benzoxazol-3-yl)acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0010 | uM |
| 2-[3-[(4-fluorophenoxy)methyl]phenyl]-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0014 | uM |
| 2-(3-benzyl-2-oxoquinoxalin-1-yl)-N-[(E)-1-(4-hydroxyphenyl)ethylideneamino]acetamide | 1859162: Inhibition of MAO-A (unknown origin) | ic50 | 0.0016 | uM |
| 2-[3-[(3-fluorophenyl)methoxy]phenyl]-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0019 | uM |
| 1-[5-(4-hydroxyphenyl)-3-(2-methoxyphenyl)-3,4-dihydropyrazol-2-yl]ethanone | 125552: Binding affinity was evaluated against human monoamino oxidase A | ki | 0.0020 | uM |
| 2-[2-(1,3-benzodioxol-5-yl)-4-oxo-1,2-dihydroquinazolin-3-yl]acetohydrazide | 1871551: Inhibition of MAO-A (unknown origin) | ic50 | 0.0021 | uM |
| 2-(3,4-difluorophenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0023 | uM |
| 4-[(E)-N-[(3-benzylquinoxalin-2-yl)amino]-C-methylcarbonimidoyl]phenol | 516368: Inhibition of MAOA by spectrophotometry | ic50 | 0.0028 | uM |
| 1-[(E)-[4-(3,4-dimethyl-5,5-dioxopyrazolo[4,3-c][1,2]benzothiazin-2-yl)phenyl]methylideneamino]-3-(4-methylphenyl)thiourea | 1506641: Inhibition of human MAOA pre-incubated for 10 mins before p-tyramine substrate addition and measured after 10 mins by amplex red reagent-based microplate fluorescence reader analysis | ic50 | 0.0030 | uM |
| trans-(1R,2S)-2-(3,4-difluorophenyl)-N-[[1-(4-phenylphenyl)triazol-4-yl]methyl]cyclopropan-1-amine;hydrochloride | 2086565: Inhibition of MAO-A (unknown origin) assessed as luminescent signal by MAO-Glo-assay | ic50 | 0.0032 | uM |
| N-methyl-N-prop-2-ynyl-2-thiophen-2-ylprop-2-en-1-amine;hydrochloride | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0034 | uM |
| 4-[(E)-[(3-benzylquinoxalin-2-yl)hydrazinylidene]methyl]phenol | 516368: Inhibition of MAOA by spectrophotometry | ic50 | 0.0034 | uM |
| 2-(4-fluorophenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;hydrochloride | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0037 | uM |
| 2-(4-chlorophenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0039 | uM |
| 3-chloro-2-(4-methoxyphenyl)-1H-indole-5,6-dicarbonitrile | 1192163: Inhibition of human recombinant MAO-A assessed as kynuramine oxidation to 4-hydroxyquinoline formation by spectrofluorometric analysis | ic50 | 0.0040 | uM |
| 1-[5-(2,4-dihydroxyphenyl)-3-(2-methoxyphenyl)-3,4-dihydropyrazol-2-yl]ethanone | 125552: Binding affinity was evaluated against human monoamino oxidase A | ki | 0.0040 | uM |
| phenyl 5-(2-hydroxyphenyl)-3-(4-methylphenyl)-3,4-dihydropyrazole-2-carboxylate | 776657: Competitive inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 insect cells using p-tyramine as substrate by Lineweaver-Burk plot analysis | ki | 0.0040 | uM |
| N-[(E)-[(E)-3-(2-chlorophenyl)-1-(2-methoxyphenyl)prop-2-enylidene]amino]-2-(2-oxo-1,3-benzoxazol-3-yl)acetamide | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0040 | uM |
| 5-chloro-3-[2-[5-(4-methoxyphenyl)-3-phenyl-3,4-dihydropyrazol-2-yl]-2-oxoethyl]-1,3-benzoxazol-2-one | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0040 | uM |
| 3-[2-[3-(4-methylphenyl)-5-phenyl-3,4-dihydropyrazol-2-yl]-2-oxoethyl]-1,3-benzoxazol-2-one | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0040 | uM |
| 11-[5-[4-(2-fluorophenyl)piperazin-1-yl]pentoxy]-16-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2,4,6,9(17),10,12,14-octaen-8-one | 1857198: Inhibition of MAO-A (unknown origin) using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by Amplex red fluorescence based microplate reader assay | ic50 | 0.0040 | uM |
| (E)-3-[4-[[4-chloro-3-[3-[methyl(prop-2-ynyl)amino]propoxy]anilino]methyl]phenyl]-N-hydroxyprop-2-enamide | 1900906: Inhibition of MAO-A (unknown origin) expressed in mouse GL26 cells using 14C 5-hydroxytryptamine as substrate pre-incubated for 20 mins followed by substrate addition measured after 20 mins by liquid scintillation spectroscopy | ic50 | 0.0040 | uM |
| 2-(4-chloro-3-methylphenyl)-N-methyl-N-prop-2-ynylprop-2-en-1-amine;oxalic acid | 1199579: Inhibition of human recombinant MAO-A expressed in Sf9 cells using 5-hydroxytryptamine substrate assessed as hydrogen peroxide production after 1 hr by fluorescence assay | ic50 | 0.0041 | uM |
| 4-(2,4-difluorophenyl)-N-[(E)-(4-morpholin-4-ylphenyl)methylideneamino]-1,3-thiazol-2-amine | 1351087: Reversible-competitive inhibition of human MAO-A using varying levels of tyramine as substrate after 30 mins by Lineweaver-Burk plot | ki | 0.0044 | uM |
| (5R)-5-(methoxymethyl)-3-pyrrol-1-yl-1,3-oxazolidin-2-one | 1940943: Inhibition of recombinant human MAO-A using kynuramine as substrate incubated for 20 mins by spectrophotometry analysis | ki | 0.0049 | uM |
| 3-[2-[3-(3-methoxyphenyl)-5-phenyl-3,4-dihydropyrazol-2-yl]-2-oxoethyl]-5-methyl-1,3-benzoxazol-2-one | 1708793: Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | ki | 0.0050 | uM |
| 11-[3-[4-(2-fluorophenyl)piperazin-1-yl]propoxy]-16-azatetracyclo[7.7.1.02,7.013,17]heptadeca-1(16),2,4,6,9(17),10,12,14-octaen-8-one | 1857198: Inhibition of MAO-A (unknown origin) using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by Amplex red fluorescence based microplate reader assay | ic50 | 0.0050 | uM |
| N’-[2-(3-benzyl-2-oxoquinoxalin-1-yl)acetyl]-4-methylbenzohydrazide | 1767577: Inhibition of MAO-A (unknown origin) by multi-well spectrophotometry | ic50 | 0.0053 | uM |
| N-methyl-N-(1H-pyrrol-2-ylmethyl)prop-2-yn-1-amine | 1940942: Inhibition of MAO-A (unknown origin) | ki | 0.0054 | uM |
| 1-[[2-(3-benzyl-2-oxoquinoxalin-1-yl)acetyl]amino]-3-phenylthiourea | 1767577: Inhibition of MAO-A (unknown origin) by multi-well spectrophotometry | ic50 | 0.0054 | uM |
| 5-[(Z)-(6-bromoindol-3-ylidene)methyl]-2-imino-1,3-dimethylimidazol-4-ol | 672470: Inhibition of human recombinant MAO-A using kynuramine as substrate preincubated with compound for 15 mins measured after 20 mins by fluorometric analysis | ic50 | 0.0056 | uM |
| 2-[(1R,2R)-2-phenylcyclopropyl]-4,5-dihydro-1H-imidazole | 223249: Displacement of [3H]idazoxan from imidazoline receptor I-2 of rabbit kidney membranes | ki | 0.0060 | uM |
CTD chemical–gene interactions
149 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, increases expression, affects expression, increases methylation | 9 |
| Estradiol | decreases expression, affects cotreatment, increases expression | 6 |
| Serotonin | increases abundance, increases metabolic processing, decreases reaction, increases degradation, decreases amination | 5 |
| Ro 41-1049 | decreases activity, affects binding | 4 |
| Clorgyline | increases degradation, decreases activity, decreases reaction | 4 |
| Acetaminophen | decreases expression | 3 |
| Benzo(a)pyrene | affects methylation, decreases expression, increases methylation | 3 |
| Cisplatin | affects expression, affects cotreatment, increases expression, decreases reaction | 3 |
| Dexamethasone | increases expression, decreases reaction | 3 |
| Progesterone | affects cotreatment, increases expression | 3 |
| Tetrachlorodibenzodioxin | decreases expression, increases expression | 3 |
| Tobacco Smoke Pollution | decreases expression, affects expression, decreases activity | 3 |
| Aflatoxin B1 | decreases expression, decreases methylation, increases methylation | 3 |
| Cadmium Chloride | decreases expression, increases abundance, increases expression | 3 |
| bisphenol A | affects cotreatment, increases methylation, increases expression | 2 |
| sodium arsenite | decreases expression, increases expression | 2 |
| sarpogrelate | decreases reaction, increases expression | 2 |
| entinostat | increases expression, affects cotreatment | 2 |
| bisphenol S | increases expression, affects cotreatment, decreases methylation | 2 |
| Arsenic Trioxide | increases expression | 2 |
| Troglitazone | decreases activity, increases expression | 2 |
| Air Pollutants | decreases expression, increases abundance | 2 |
| Carbamazepine | affects expression, increases expression | 2 |
| Diethylstilbestrol | increases expression | 2 |
| Disulfiram | affects binding, decreases expression, decreases reaction, increases metabolic processing | 2 |
| Phenylmercuric Acetate | affects cotreatment, decreases expression | 2 |
| Zeranol | increases expression | 2 |
| Thapsigargin | decreases expression | 2 |
| beta-Naphthoflavone | decreases expression | 2 |
| Moclobemide | decreases amination, decreases reaction, decreases activity | 2 |
ChEMBL screening assays
1269 unique, capped per target: 1213 binding, 36 admet, 14 toxicity, 6 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1003726 | Binding | Inhibition of human recombinant MAO-A assessed as hydrogen peroxide production | Chalcones: a valid scaffold for monoamine oxidases inhibitors. — J Med Chem |
| CHEMBL2327762 | ADMET | Inhibition of human MAO-A assessed as residual activity at 10 uM | Synthesis and antibacterial activities of new piperidine substituted (5R)-[1,2,3]triazolylmethyl and (5R)-[(4-F-[1,2,3]triazolyl)methyl] oxazolidinones. — Bioorg Med Chem Lett |
| CHEMBL5049165 | Toxicity | Inhibition of human recombinant MAO-A expressed in supersomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate by spectrofluorimetric analysis | Probing Fluorinated Motifs onto Dual AChE-MAO B Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Early-ADME Studies. — J Med Chem |
Cellosaurus cell lines
3 cell lines: 2 cancer cell line, 1 transformed cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_D7GW | Ubigene HEK293T MAOA KO | Transformed cell line | Female |
| CVCL_SW27 | HAP1 MAOA (-) 1 | Cancer cell line | Male |
| CVCL_SW28 | HAP1 MAOA (-) 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
197 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT05657860 | PHASE4 | COMPLETED | Guanfacine Extended Release for the Reduction of Aggression and Self-injurious Behavior Associated With Prader-Willi Syndrome |
| NCT05744479 | PHASE4 | RECRUITING | Metformin for Antipsychotic-induced Weight Gain in Adults With Intellectual Disability |
| NCT06107829 | PHASE4 | WITHDRAWN | Valbenazine Treatment of Tardive Dyskinesia in Adults With Intellectual/Developmental Disabilities |
| NCT06997198 | PHASE4 | NOT_YET_RECRUITING | Deutetrabenazine Treatment for Tardive Dyskinesia in Intellectual/Developmental Disabilities |
| NCT02270736 | PHASE3 | COMPLETED | Clinical Study to Investigate the Efficacy and Safety of NT 201 Compared to Placebo in the Treatment of Chronic Troublesome Drooling Associated With Neurological Disorders and/or Intellectual Disability |
| NCT02304302 | PHASE2 | COMPLETED | Down Syndrome Memantine Follow-up Study |
| NCT03862950 | PHASE2 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome (Met) |
| NCT04529226 | PHASE2 | UNKNOWN | Study to Compare Clozapine vs Treatment as Usual in People With Intellectual Disability & Treatment-resistant Psychosis |
| NCT04821856 | PHASE2 | COMPLETED | Evaluation of the Effectiveness of Cannabidiol in Treating Severe Behavioural Problems in Children and Adolescents With Intellectual Disability |
| NCT05273320 | PHASE1 | COMPLETED | Clinical Trial of Nabilone for Aggression in Adults With Intellectual and Developmental Disabilities |
| NCT05301361 | PHASE1 | ENROLLING_BY_INVITATION | Sensitivity of the NIH Toolbox to Stimulant Treatment in Intellectual Disabilities |
| NCT06016764 | PHASE1 | COMPLETED | Use of MRI and cTBS for Catatonia in Autism |
| NCT06586827 | PHASE1 | COMPLETED | Impact of Competency-Based Training and Technical Assistance Employment Outcomes of Individuals With ID/DD |
| NCT07531940 | PHASE1 | NOT_YET_RECRUITING | Escalating Doses of Memantine in Down Syndrome (MEDS-123) |
| NCT03479476 | PHASE2/PHASE3 | COMPLETED | A Trial of Metformin in Individuals With Fragile X Syndrome |
| NCT02616796 | PHASE1/PHASE2 | COMPLETED | Effects of Social Gaze Training on Brain and Behavior in Fragile X Syndrome |
| NCT06860672 | EARLY_PHASE1 | RECRUITING | Clinical Trial of the Dual Vector Base Editor for the Treatment of the CHD3-R1025W Mutation |
| NCT00597948 | Not specified | COMPLETED | Healthy Lifestyles for People With Intellectual Disabilities |
| NCT01087320 | Not specified | RECRUITING | Genome Medical Sequencing for Gene Discovery |
| NCT01652963 | Not specified | UNKNOWN | Picture-based Computerised Assessment and Training of Cognitive Behaviour Therapy Skills |
| NCT01695395 | Not specified | COMPLETED | Mental Health Care Provision for Adults With Intellectual Disability and a Mental Disorder |
| NCT01867554 | Not specified | COMPLETED | Research and Characterization of New Genes Involved in Intellectual Disability |
| NCT01915381 | Not specified | COMPLETED | Improving Adherence Healthy Lifestyle With a Smartphone Application Based on Adults With Intellectual Disabilities |
| NCT01988623 | Not specified | COMPLETED | Pivotal Response Treatment for Individuals With Intellectual Disabilities |
| NCT02099773 | Not specified | COMPLETED | Support Staff-client Interactions With Augmentative and Alternative Communication |
| NCT02136849 | Not specified | COMPLETED | Inter-regional Project of the Great Western Exploration Approach for Exome Molecular Causes Severe Intellectual Disability Isolated or Syndromic |
| NCT02225041 | Not specified | COMPLETED | Sedation Strategy and Cognitive Outcome After Critical Illness in Early Childhood |
| NCT02414438 | Not specified | COMPLETED | Establishing the Clinical Utility of First StepDx PLUS and NextStepDx PLUS Study |
| NCT02451761 | Not specified | COMPLETED | Apparently Balanced Chromosomal Translocation/ Next-generation Sequencing/ Intellectual Disability |
| NCT02461420 | Not specified | ACTIVE_NOT_RECRUITING | Mapping the Genotype, Phenotype, and Natural History of Phelan-McDermid Syndrome |
| NCT02461459 | Not specified | ACTIVE_NOT_RECRUITING | Autism Spectrum Disorder (ASD) and Intellectual Disability (ID) Determinants in Tuberous Sclerosis Complex (TSC) |
| NCT02486081 | Not specified | COMPLETED | Development and Application-Smart Football for Movement Evaluation and Training in the Special Education Population |
| NCT02504502 | Not specified | COMPLETED | Enhancing Genomic Laboratory Reports to Enhance Communication and Empower Patients |
| NCT02513277 | Not specified | COMPLETED | Diabetes Screening & Prevention for People With Learning (Intellectual) Disabilities:STOP Diabetes Study |
| NCT02561754 | Not specified | COMPLETED | Weight Management for Adolescents With IDD |
| NCT02591446 | Not specified | COMPLETED | Transcranial Magnetic Stimulation Studies in Autism Spectrum Disorders |
| NCT02714868 | Not specified | COMPLETED | Evaluation of Project TEAM (Teens Making Environmental and Activity Modifications) |
| NCT02721394 | Not specified | UNKNOWN | FCT With Young Children With ID in the UK: A Feasibility Project V.1 |
| NCT02746614 | Not specified | COMPLETED | Psychomotor Therapy Effects in Adaptive Behavior and Motor Proficiency in Intellectual Disability |
| NCT02836405 | Not specified | COMPLETED | TMS for the Investigation of Brain Plasticity in Autism Spectrum Disorders |
Related Atlas pages
- Associated diseases: Brunner syndrome
- Targeted by drugs: Linezolid, Moclobemide, Phenelzine, Selegiline, Tranylcypromine
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): antisocial behavior, susceptibility to, Brunner syndrome