INMT

Summary

INMT (indolethylamine N-methyltransferase, HGNC:6069) is a protein-coding gene on chromosome 7p14.3, encoding Indolethylamine N-methyltransferase (O95050). Functions as a thioether S-methyltransferase and is active with a variety of thioethers and the corresponding selenium and tellurium compounds, including 3-methylthiopropionaldehyde, dimethyl selenide, dimethyl telluride, 2-methylthioethylamine, 2-methylthioethanol, methyl-n-pro….

N-methylation of endogenous and xenobiotic compounds is a major method by which they are degraded. This gene encodes an enzyme that N-methylates indoles such as tryptamine. Alternative splicing results in multiple transcript variants. Read-through transcription also exists between this gene and the downstream MINDY4 (aka FAM188B) gene. In rodents and other mammals such as cetartiodactyla this gene is in the opposite orientation compared to its orientation in human and other primates and this gene appears to have been lost in carnivora and chiroptera.

Source: NCBI Gene 11185 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 58 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_006774

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:6069
Approved symbol	INMT
Name	indolethylamine N-methyltransferase
Location	7p14.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000241644
Ensembl biotype	protein_coding
OMIM	604854
Entrez	11185

Gene structure

Transcript identifiers

Ensembl transcripts: 4 — 2 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000013222, ENST00000409539, ENST00000461246, ENST00000484180

RefSeq mRNA: 2 — MANE Select: NM_006774 NM_001199219, NM_006774

CCDS: CCDS5430, CCDS56479

Canonical transcript exons

ENST00000013222 — 3 exons

Exon	Start	End
ENSE00000832209	30752135	30752304
ENSE00001310197	30755422	30757602
ENSE00003655533	30753731	30753938

Expression profiles

Bgee: expression breadth ubiquitous, 188 present calls, max score 98.74.

FANTOM5 (CAGE): breadth broad, TPM avg 3.3746 / max 433.1743, expressed in 294 samples.

FANTOM5 promoters (1 alternative TSS)

Promoter ID	TPM avg	Samples expressed
78003	3.3746	294

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lung	UBERON:0002167	98.74	gold quality
upper lobe of left lung	UBERON:0008952	98.24	gold quality
upper lobe of lung	UBERON:0008948	97.43	gold quality
right coronary artery	UBERON:0001625	97.29	gold quality
left coronary artery	UBERON:0001626	96.40	gold quality
coronary artery	UBERON:0001621	96.38	gold quality
cardiac muscle of right atrium	UBERON:0003379	96.22	silver quality
right atrium auricular region	UBERON:0006631	95.01	gold quality
lung	UBERON:0002048	95.00	gold quality
cardiac atrium	UBERON:0002081	94.94	gold quality
apex of heart	UBERON:0002098	94.01	gold quality
right adrenal gland	UBERON:0001233	93.82	gold quality
right adrenal gland cortex	UBERON:0035827	93.52	gold quality
left adrenal gland cortex	UBERON:0035825	93.48	gold quality
left adrenal gland	UBERON:0001234	93.32	gold quality
adrenal cortex	UBERON:0001235	93.11	gold quality
ascending aorta	UBERON:0001496	93.09	gold quality
thoracic aorta	UBERON:0001515	93.03	gold quality
left uterine tube	UBERON:0001303	92.37	gold quality
lower esophagus muscularis layer	UBERON:0035833	92.00	gold quality
lower esophagus	UBERON:0013473	91.92	gold quality
saphenous vein	UBERON:0007318	91.85	gold quality
adrenal gland	UBERON:0002369	91.67	gold quality
peritoneum	UBERON:0002358	91.66	gold quality
omental fat pad	UBERON:0010414	91.66	gold quality
aorta	UBERON:0000947	91.37	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	91.28	gold quality
descending thoracic aorta	UBERON:0002345	90.65	gold quality
adipose tissue of abdominal region	UBERON:0007808	90.42	gold quality
popliteal artery	UBERON:0002250	90.19	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-HCAD-9	yes	1384.62
E-GEOD-75367	yes	102.43
E-GEOD-134144	yes	31.56
E-MTAB-10137	no	559.52
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

53 targeting INMT, 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-7110-3P	100.00	73.18	2486
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-302C-5P	99.97	72.56	3642
HSA-MIR-4487	99.96	64.58	1252
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-205-3P	99.92	69.92	3165
HSA-MIR-613	99.91	71.50	1710
HSA-MIR-4760-5P	99.80	69.88	1619
HSA-MIR-6817-3P	99.79	68.35	2126
HSA-MIR-4729	99.69	72.18	4233
HSA-MIR-6762-3P	99.66	66.94	1188
HSA-MIR-10393-5P	99.65	68.01	1368
HSA-MIR-1827	99.63	68.57	3265
HSA-MIR-8061	99.63	69.44	1411
HSA-MIR-24-3P	99.59	69.97	1934
HSA-MIR-203A-3P	99.49	70.56	2806
HSA-MIR-372-5P	99.41	69.11	2299
HSA-MIR-410-3P	99.27	69.98	2457
HSA-MIR-296-3P	99.21	66.56	474
HSA-MIR-4426	99.17	66.74	1949
HSA-MIR-7160-5P	99.11	67.17	2207
HSA-MIR-3160-3P	99.07	64.78	955
HSA-MIR-12125	98.59	67.54	1044
HSA-MIR-5581-3P	98.55	70.31	1161

Literature-anchored findings (GeneRIF, showing 5)

• study suggests that rs77743549 of INMT may be associated with the risk for Hirschsprung’s disease (PMID:26183064)
• genome-wide association studies in populations in Argentina/Bangladeshi: Three SNPs in INMT (rs6970396, rs1061644, rs4270015) are associated with production of trimethylselenonium (TMSe); urinary Se excretion is up-regulated in TMSe-producing women. (PMID:26537946)
• analysis of 254C and 254F variants of hINMT reveals differences in methylation of tryptamine, dimethylsulfide and dimethylselenide (PMID:31310642)
• Targeting INMT and interrupting its methylation pathway for the treatment of castration resistant prostate cancer. (PMID:34587977)
• Differential molecular mechanisms of substrate recognition by selenium methyltransferases, INMT and TPMT, in selenium detoxification and excretion. (PMID:38159853)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	zgc:64002	ENSDARG00000086998
mus_musculus	Inmt	ENSMUSG00000003477
rattus_norvegicus	Inmt	ENSRNOG00000011250
caenorhabditis_elegans		WBGENE00011573
caenorhabditis_elegans		WBGENE00015124
caenorhabditis_elegans		WBGENE00018340

Paralogs (2): PNMT (ENSG00000141744), NNMT (ENSG00000166741)

Protein

Protein identifiers

Indolethylamine N-methyltransferase — O95050 (reviewed: O95050)

Alternative names: Aromatic alkylamine N-methyltransferase, Thioether S-methyltransferase

All UniProt accessions (1): O95050

UniProt curated annotations — full annotation on UniProt →

Function. Functions as a thioether S-methyltransferase and is active with a variety of thioethers and the corresponding selenium and tellurium compounds, including 3-methylthiopropionaldehyde, dimethyl selenide, dimethyl telluride, 2-methylthioethylamine, 2-methylthioethanol, methyl-n-propyl sulfide and diethyl sulfide. Plays an important role in the detoxification of selenium compounds. Catalyzes the N-methylation of tryptamine and structurally related compounds.

Subunit / interactions. Monomer.

Subcellular location. Cytoplasm.

Tissue specificity. Widely expressed. The highest levels were in thyroid, adrenal gland, adult and fetal lung. Intermediate levels in heart, placenta, skeletal muscle, testis, small intestine, pancreas, stomach, spinal cord, lymph node and trachea. Very low levels in adult and fetal kidney and liver, in adult spleen, thymus, ovary, colon and bone marrow. Not expressed in peripheral blood leukocytes and brain.

Similarity. Belongs to the class I-like SAM-binding methyltransferase superfamily. NNMT/PNMT/TEMT family.

Isoforms (2)

UniProt ID	Names	Canonical?
O95050-1	1	yes
O95050-2	2

RefSeq proteins (2): NP_001186148, NP_006765* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000940	NNMT_TEMT_trans	Family
IPR025820	NNMT/PNMT/TEMT_CS	Conserved_site
IPR029063	SAM-dependent_MTases_sf	Homologous_superfamily
IPR053384	SAM-dep_methyltransferase	Family

Pfam: PF01234

Catalyzed reactions (Rhea), 4 shown:

• dimethyl sulfide + S-adenosyl-L-methionine = trimethylsulfonium + S-adenosyl-L-homocysteine (RHEA:19613)
• a primary amine + S-adenosyl-L-methionine = a methylated primary amine + S-adenosyl-L-homocysteine + H(+) (RHEA:23136)
• a secondary amine + S-adenosyl-L-methionine = a methylated secondary amine + S-adenosyl-L-homocysteine + H(+) (RHEA:53924)
• a tertiary amine + S-adenosyl-L-methionine = a methylated tertiary amine + S-adenosyl-L-homocysteine + H(+) (RHEA:53928)

UniProt features (44 total): helix 12, strand 10, binding site 8, sequence variant 7, modified residue 2, turn 2, chain 1, splice variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
2A14	X-RAY DIFFRACTION	1.7

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O95050-F1	97.14	0.96

Functional residue map

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

Ligand- & substrate-binding residues (8): 20; 25; 63; 69; 85–87; 90; 142–143; 163

Post-translational modifications (2): 96, 13

Function

Pathways and Gene Ontology

Reactome pathways

4 pathways

ID	Pathway
R-HSA-2408552	Methylation of MeSeH for excretion
R-HSA-1430728	Metabolism
R-HSA-2408522	Selenoamino acid metabolism
R-HSA-71291	Metabolism of amino acids and derivatives

MSigDB gene sets: 112 (showing top): GSE45365_NK_CELL_VS_BCELL_DN, YAO_HOXA10_TARGETS_VIA_PROGESTERONE_UP, YAO_TEMPORAL_RESPONSE_TO_PROGESTERONE_CLUSTER_1, FERREIRA_EWINGS_SARCOMA_UNSTABLE_VS_STABLE_DN, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM4, ACEVEDO_LIVER_TUMOR_VS_NORMAL_ADJACENT_TISSUE_DN, INGRAM_SHH_TARGETS_UP, HFH8_01, ICHIBA_GRAFT_VERSUS_HOST_DISEASE_35D_DN, HFH3_01, JECHLINGER_EPITHELIAL_TO_MESENCHYMAL_TRANSITION_DN, LEE_AGING_NEOCORTEX_DN, GOBP_RESPONSE_TO_TOXIC_SUBSTANCE, MODULE_48, GOBP_METHYLATION

GO Biological Process (3): amine metabolic process (GO:0009308), response to toxic substance (GO:0009636), methylation (GO:0032259)

GO Molecular Function (7): thioether S-methyltransferase activity (GO:0004790), N-methyltransferase activity (GO:0008170), amine N-methyltransferase activity (GO:0030748), protein binding (GO:0005515), methyltransferase activity (GO:0008168), S-adenosylmethionine-dependent methyltransferase activity (GO:0008757), transferase activity (GO:0016740)

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

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Selenoamino acid metabolism	1
Metabolism of amino acids and derivatives	1
Metabolism	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
metabolic process	2
S-adenosylmethionine-dependent methyltransferase activity	2
methyltransferase activity	2
cellular anatomical structure	2
response to chemical	1
S-methyltransferase activity	1
binding	1
transferase activity, transferring one-carbon groups	1
catalytic activity	1
cytoplasm	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

568 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
INMT	AOX1	Q06278	587
INMT	MINDY4	Q4G0A6	577
INMT	MAOB	P27338	519
INMT	ALDH2	P05091	475
INMT	DDC	P20711	453
INMT	IDO2	Q6ZQW0	427
INMT	MKI67	P46013	407
INMT	AOC3	Q16853	406
INMT	GPRIN2	O60269	404
INMT	OBSCN	Q5VST9	395
INMT	TFAP2A	P05549	380
INMT	COL4A3	Q01955	369
INMT	NMT1	P30419	365
INMT	TIPARP	Q7Z3E1	365
INMT	C2orf74	A8MZ97	357

IntAct

9 interactions, top by confidence:

A	B	Type	Score
KLHL12	INMT	psi-mi:“MI:0915”(physical association)	0.720
INMT	KLHL12	psi-mi:“MI:0915”(physical association)	0.720
INMT	LNX2	psi-mi:“MI:0915”(physical association)	0.490
INMT	KLHL12	psi-mi:“MI:0915”(physical association)	0.000

BioGRID (5): KLHL12 (Two-hybrid), LNX2 (Two-hybrid), INMT (Synthetic Lethality), INMT (Two-hybrid), INMT (Affinity Capture-RNA)

ESM2 similar proteins: A0A1W2PQ27, A0A1W2PQ64, A0A1W2PQC6, A0A1W2PQD8, A0A1W2PQJ5, A0A1W2PR75, A2AV36, A4QN59, A6QQV6, D4A1F2, F1RA39, G5E8F4, J9SQF3, O00142, O42868, O55239, O95050, O95932, O97972, P0CR76, P0CR77, P10938, P40261, P40936, P53538, Q01841, Q22453, Q32LP9, Q4R7D0, Q566Y1, Q5M9G7, Q5RFR7, Q5U4E8, Q5XG58, Q62160, Q6C195, Q6CQ61, Q6DE00, Q6FMU7, Q6PCI6

Diamond homologs: A0A5F8AH41, O55239, O95050, O97972, P10937, P10938, P11086, P40261, P40935, P40936, Q06AU9, Q06AV1, Q5RFR7

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	46
Likely benign	5
Benign	7

Top pathogenic / likely-pathogenic (0)

SpliceAI

462 predictions. Top by Δscore:

Variant	Effect	Δscore
7:30752303:TGGTG:T	donor_loss	1.0000
7:30752305:G:C	donor_loss	1.0000
7:30752305:G:GG	donor_gain	1.0000
7:30753726:CACAG:C	acceptor_loss	1.0000
7:30753729:A:AG	acceptor_gain	1.0000
7:30753729:AGG:A	acceptor_loss	1.0000
7:30753730:G:GG	acceptor_gain	1.0000
7:30753730:GGA:G	acceptor_gain	1.0000
7:30753928:G:GT	donor_gain	1.0000
7:30753935:ACAG:A	donor_loss	1.0000
7:30753936:CAG:C	donor_loss	1.0000
7:30753940:T:A	donor_loss	1.0000
7:30755420:A:AG	acceptor_gain	1.0000
7:30755421:G:GA	acceptor_gain	1.0000
7:30752264:G:GT	donor_gain	0.9900
7:30752278:A:T	donor_gain	0.9900
7:30752303:TG:T	donor_gain	0.9900
7:30752304:GG:G	donor_gain	0.9900
7:30753729:AG:A	acceptor_gain	0.9900
7:30753729:AGGAG:A	acceptor_gain	0.9900
7:30753730:GG:G	acceptor_gain	0.9900
7:30753730:GGAGG:G	acceptor_gain	0.9900
7:30753916:GCCT:G	donor_gain	0.9900
7:30755420:AGC:A	acceptor_gain	0.9900
7:30755421:G:GG	acceptor_gain	0.9900
7:30755421:GC:G	acceptor_gain	0.9900
7:30755421:GCG:G	acceptor_gain	0.9900
7:30755421:GCGGC:G	acceptor_gain	0.9900
7:30755717:G:GT	donor_gain	0.9900
7:30755857:G:GT	donor_gain	0.9900

AlphaMissense

1706 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:30753808:T:C	F78L	0.987
7:30753810:C:A	F78L	0.987
7:30753810:C:G	F78L	0.987
7:30755690:T:C	F211L	0.987
7:30755692:T:A	F211L	0.987
7:30755692:T:G	F211L	0.987
7:30753895:T:A	W107R	0.986
7:30753895:T:C	W107R	0.986
7:30753865:T:A	W97R	0.985
7:30753865:T:C	W97R	0.985
7:30752193:T:C	F15L	0.983
7:30752195:C:A	F15L	0.983
7:30752195:C:G	F15L	0.983
7:30752295:T:C	F49L	0.979
7:30752297:C:A	F49L	0.979
7:30752297:C:G	F49L	0.979
7:30755619:T:A	L187H	0.973
7:30753797:C:A	A74D	0.972
7:30753897:G:C	W107C	0.972
7:30753897:G:T	W107C	0.972
7:30752268:T:C	F40L	0.971
7:30752270:T:A	F40L	0.971
7:30752270:T:G	F40L	0.971
7:30755536:T:G	C159W	0.970
7:30755829:C:A	A257D	0.970
7:30755640:T:A	V194E	0.968
7:30753764:G:A	G63D	0.967
7:30753764:G:T	G63V	0.967
7:30753846:C:A	N90K	0.966
7:30753846:C:G	N90K	0.966

dbSNP variants (sampled 300 via entrez): RS1000196075 (7:30754432 C>T), RS1000432477 (7:30757828 G>C,T), RS1000890203 (7:30751847 C>G,T), RS1000898158 (7:30753412 G>T), RS1001945304 (7:30752811 G>T), RS1002199352 (7:30756828 G>C), RS1002290337 (7:30753038 G>C), RS1002601499 (7:30750399 A>G), RS1002619536 (7:30752307 G>A,T), RS1002650577 (7:30752640 G>A), RS1002930931 (7:30755816 T>C), RS1002953989 (7:30757743 C>T), RS1003156712 (7:30757431 G>A,T), RS1003678482 (7:30753995 T>C), RS1004234704 (7:30756493 C>T)

Disease associations

OMIM: gene MIM:604854 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): prostate cancer (MONDO:0008315)

Orphanet (1): Familial prostate cancer (Orphanet:1331)

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST001432_2	Nephrolithiasis	2.000000e-14
GCST002726_46	Glucose homeostasis traits	6.000000e-06
GCST007833_8	Urolithiasis	5.000000e-10

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0006832	disposition index measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D011471	Prostatic Neoplasms	C04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2131 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 2,165 (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
CHEMBL1214186	SINEFUNGIN	2	2,165

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

ChEMBL bioactivities

17 potent at pChembl≥5 of 36 total, top 17 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.10	IC50	800	nM	CHEMBL3228343
6.00	IC50	1000	nM	CHEMBL3228332
5.70	Ki	2000	nM	S-ADENOSYLHOMOCYSTEINE
5.66	IC50	2200	nM	CHEMBL3228352
5.58	IC50	2600	nM	CHEMBL3228354
5.55	IC50	2800	nM	CHEMBL3228372
5.48	IC50	3300	nM	CHEMBL3228261
5.47	IC50	3400	nM	CHEMBL4591248
5.43	IC50	3700	nM	CHEMBL3228381
5.40	IC50	4000	nM	CHEMBL3228385
5.40	IC50	4000	nM	SINEFUNGIN
5.37	IC50	4300	nM	CHEMBL3228371
5.22	IC50	6000	nM	CHEMBL3228345
5.19	IC50	6400	nM	CHEMBL3228361
5.17	IC50	6700	nM	CHEMBL3228364
5.10	IC50	7900	nM	CHEMBL3228400
5.00	IC50	9900	nM	CHEMBL3228382

PubChem BioAssay actives

17 with measured affinity, of 112 total; 17 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
(E)-but-2-enedioic acid;2,3,5,6,7,8-hexahydroimidazo[1,2-a]pyridine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	0.8000	uM
(E)-but-2-enedioic acid;3,5,6,7-tetrahydro-2H-pyrrolo[1,2-a]imidazole	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	1.0000	uM
(2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid	91847: Inhibitory constant towards indole N-methyl-transferase	ki	2.0000	uM
3-methyl-1,3-thiazolidin-2-imine;hydroiodide	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	2.2000	uM
(E)-but-2-enedioic acid;3-ethyl-1,3-thiazolidin-2-imine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	2.6000	uM
1-ethylpyrrolidin-2-imine;oxalic acid	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	2.8000	uM
(E)-but-2-enedioic acid;3,4,6,7,8,9-hexahydro-2H-pyrido[1,2-a]pyrimidine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	3.3000	uM
(2S,5S)-2-amino-5-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]-7-(3-carbamoylphenyl)hept-6-ynoic acid	1616806: Inhibition of wild type human INMT expressed in Escherichia coli using tryptamine as substrate in presence of SAM incubated for 30 mins by MTase-Glo assay	ic50	3.4000	uM
3-methyl-1,3-thiazinan-2-imine;hydrobromide	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	3.7000	uM
(2S,5S)-2,5-diamino-6-[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]hexanoic acid	1885879: Inhibition of N-terminal 6His-tagged full length human recombinant INMT (1 to 263 residues) expressed in Escherichia coli BL21 (DE3) cells using S-(5’-Adenosyl)-L-methionine chloride dihydrochloride and 9H-pyrido[3,4-b]indole as substrate incubated for 2.5 hrs by MTase-Glo assay	ic50	4.0000	uM
3-methyl-6H-1,3-thiazin-2-imine;hydrate;hydrochloride	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	4.0000	uM
1-methylpyrrolidin-2-imine;hydroiodide	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	4.3000	uM
(E)-but-2-enedioic acid;3,5,6,8-tetrahydro-2H-imidazo[2,1-c][1,4]thiazine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	6.0000	uM
(E)-but-2-enedioic acid;2-imino-N-methyl-1,3-thiazolidin-3-amine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	6.4000	uM
3-methyl-1,3-thiazol-2-imine;hydroiodide	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	6.7000	uM
(E)-but-2-enedioic acid;1-methyl-2,3-dihydropyridin-6-imine	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	7.9000	uM
3-ethyl-1,3-thiazinan-2-imine;hydrobromide	1123843: Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	ic50	9.9000	uM

CTD chemical–gene interactions

14 total (human), top 14 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression	3
Nickel	decreases expression	2
bisphenol A	decreases expression	1
triadimefon	decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
Benzo(a)pyrene	increases methylation, affects methylation	1
Dexamethasone	increases expression	1
Phenylmercuric Acetate	affects cotreatment, decreases expression	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	increases expression	1
Tungsten Compounds	decreases expression	1
Antirheumatic Agents	increases expression	1
Cadmium Chloride	decreases expression	1
Okadaic Acid	decreases expression	1

ChEMBL screening assays

41 unique, capped per target: 38 binding, 3 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3231054	Binding	Inhibition of human lung INMT using N-methyltryptamine as substrate after 60 to 90 mins by liquid scintillation counting in presence of S-methyl-[14C]adenosylmethionine	Cyclic amidine inhibitors of indolamine N-methyltransferase. — J Med Chem
CHEMBL4416335	ADMET	Inhibition of wild type human INMT expressed in Escherichia coli at 10 uM using tryptamine as substrate in presence of SAM incubated for 30 mins by MTase-Glo assay relative to control	High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). — J Med Chem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00029224	PHASE4	COMPLETED	Treatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997	PHASE4	COMPLETED	Open-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609	PHASE4	COMPLETED	The Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623	PHASE4	SUSPENDED	The Plenaxis® Experience Study
NCT00106392	PHASE4	COMPLETED	A Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029	PHASE4	UNKNOWN	MR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485	PHASE4	COMPLETED	Angelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219	PHASE4	COMPLETED	Zoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271	PHASE4	COMPLETED	Effect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146	PHASE4	COMPLETED	Study to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554	PHASE4	COMPLETED	Open-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098	PHASE4	COMPLETED	Docetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696	PHASE4	COMPLETED	Casodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139	PHASE4	COMPLETED	Effect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765	PHASE4	COMPLETED	Effects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690	PHASE4	COMPLETED	Evaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708	PHASE4	COMPLETED	Local Anesthesia for Prostate Biopsy
NCT00526331	PHASE4	COMPLETED	Evaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213	PHASE4	COMPLETED	Compare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330	PHASE4	TERMINATED	Dissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966	PHASE4	COMPLETED	Radical Prostatectomy and Perioperative Fluid Therapy
NCT00805701	PHASE4	COMPLETED	Study Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027	PHASE4	COMPLETED	Effect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269	PHASE4	UNKNOWN	Can Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277	PHASE4	COMPLETED	Study of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800	PHASE4	COMPLETED	Does Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199	PHASE4	COMPLETED	Global Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226	PHASE4	COMPLETED	Evaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563	PHASE4	COMPLETED	Randomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905	PHASE4	COMPLETED	Study to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672	PHASE4	COMPLETED	3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143	PHASE4	TERMINATED	Prospective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742	PHASE4	UNKNOWN	Comparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563	PHASE4	COMPLETED	Hydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874	PHASE4	COMPLETED	Efficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472	PHASE4	TERMINATED	Firmagon (Degarelix) Intermittent Therapy
NCT01547416	PHASE4	COMPLETED	The Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544	PHASE4	COMPLETED	The Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749	PHASE4	UNKNOWN	Evaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635	PHASE4	COMPLETED	Study of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer