NTMT1

Summary

NTMT1 (N-terminal Xaa-Pro-Lys N-methyltransferase 1, HGNC:23373) is a protein-coding gene on chromosome 9q34.11, encoding N-terminal Xaa-Pro-Lys N-methyltransferase 1 (Q9BV86). Distributive alpha-N-methyltransferase that methylates the N-terminus of target proteins containing the N-terminal motif [Ala/Gly/Pro/Ser]-Pro-Lys when the initiator Met is cleaved.

The METTL11A gene encodes an N-terminal methyltransferase for the RAN (MIM 601179) guanine nucleotide exchange factor regulator of chromosome condensation 1 (RCC1; MIM 179710). METTL11A enzyme alpha-N-methylates other protein targets such as SET (MIM 600960) and RB (MIM 180200).

Source: NCBI Gene 28989 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 28 total
• Phenotypes (HPO): 1
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_014064

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23373
Approved symbol	NTMT1
Name	N-terminal Xaa-Pro-Lys N-methyltransferase 1
Location	9q34.11
Locus type	gene with protein product
Status	Approved
Aliases	AD-003, HOMT1A, NRMT1, NRMT
Ensembl gene	ENSG00000148335
Ensembl biotype	protein_coding
OMIM	613560
Entrez	28989

Gene structure

Transcript identifiers

Ensembl transcripts: 24 — 22 protein_coding, 1 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000372480, ENST00000372481, ENST00000372483, ENST00000372486, ENST00000459968, ENST00000481189, ENST00000482347, ENST00000486391, ENST00000611055, ENST00000613644, ENST00000617943, ENST00000900249, ENST00000900251, ENST00000900252, ENST00000900253, ENST00000900254, ENST00000900255, ENST00000900256, ENST00000935935, ENST00000935936, ENST00000935937, ENST00000949698, ENST00000949699, ENST00000949700

RefSeq mRNA: 9 — MANE Select: NM_014064 NM_001286796, NM_001286797, NM_001286798, NM_001286799, NM_001286800, NM_001286801, NM_001286802, NM_001286803, NM_014064

CCDS: CCDS35160, CCDS69682, CCDS75918

Canonical transcript exons

ENST00000372483 — 4 exons

Exon	Start	End
ENSE00001457923	129632650	129632865
ENSE00001887244	129626163	129626295
ENSE00003656407	129634054	129634306
ENSE00003904160	129635208	129636135

Expression profiles

Bgee: expression breadth ubiquitous, 252 present calls, max score 97.17.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 31.1356 / max 192.0113, expressed in 1822 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
98940	30.6861	1821
98941	0.2903	70
98939	0.0712	32
98938	0.0625	28
98942	0.0255	7

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
left testis	UBERON:0004533	97.17	gold quality
right testis	UBERON:0004534	97.07	gold quality
left ventricle myocardium	UBERON:0006566	96.52	gold quality
gastrocnemius	UBERON:0001388	95.90	gold quality
right adrenal gland	UBERON:0001233	95.60	gold quality
left adrenal gland	UBERON:0001234	95.54	gold quality
testis	UBERON:0000473	95.39	gold quality
muscle of leg	UBERON:0001383	95.17	gold quality
left adrenal gland cortex	UBERON:0035825	94.95	gold quality
hindlimb stylopod muscle	UBERON:0004252	94.93	gold quality
heart left ventricle	UBERON:0002084	94.92	gold quality
apex of heart	UBERON:0002098	94.89	gold quality
right adrenal gland cortex	UBERON:0035827	94.75	gold quality
cardiac ventricle	UBERON:0002082	94.68	gold quality
cardiac muscle of right atrium	UBERON:0003379	94.64	gold quality
adrenal cortex	UBERON:0001235	94.03	gold quality
adrenal gland	UBERON:0002369	93.91	gold quality
quadriceps femoris	UBERON:0001377	93.89	gold quality
myocardium	UBERON:0002349	93.81	gold quality
right atrium auricular region	UBERON:0006631	93.76	gold quality
vastus lateralis	UBERON:0001379	93.60	gold quality
cardiac atrium	UBERON:0002081	93.57	gold quality
skeletal muscle tissue	UBERON:0001134	93.52	gold quality
stromal cell of endometrium	CL:0002255	93.35	gold quality
prefrontal cortex	UBERON:0000451	93.18	gold quality
heart	UBERON:0000948	93.14	gold quality
tibialis anterior	UBERON:0001385	93.04	gold quality
deltoid	UBERON:0001476	92.96	gold quality
muscle tissue	UBERON:0002385	92.81	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	92.11	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

11 targeting NTMT1, 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-3065-3P	99.87	70.25	1407
HSA-MIR-10394-5P	99.65	66.83	1852
HSA-MIR-1205	99.65	66.76	1826
HSA-MIR-6727-3P	99.49	65.92	1333
HSA-MIR-6871-3P	99.43	68.85	741
HSA-MIR-4722-3P	99.35	65.22	1099
HSA-MIR-4763-5P	98.75	63.89	854
HSA-MIR-4733-3P	98.35	65.20	994
HSA-MIR-939-5P	97.10	65.80	1579
HSA-MIR-1343-5P	96.48	66.06	1506
HSA-MIR-203A-5P	96.33	65.03	714

Literature-anchored findings (GeneRIF, showing 14)

• discovery of the first alpha-N-methyltransferase, which we named N-terminal RCC1 methyltransferase (NRMT). (PMID:20668449)
• Peptide methylation assays and substrate immunoprecipitations demonstrate that the canonical M-X-P-K methylation motif is not the only one recognized by NRMT. (PMID:22769851)
• Concurrent expression of NRMT1 and NRMT2 accelerates the production of trimethylation, and we propose that NRMT2 activates NRMT1 by priming its substrates for trimethylation. (PMID:24090352)
• kinetic mechanism of NTMT1 (PMID:25771539)
• These studies position the NRMT1 knockout mouse as a useful new system for studying the effects of genomic instability and defective DNA damage repair on organismal and tissue-specific aging. (PMID:25843235)
• NRMT1 adopts a core methyltransferase fold that resembles DOT1L and PRMT but not SET domain family histone methyltransferases. (PMID:26543159)
• CENP-A undergoes alpha-amino trimethylation by the enzyme NRMT in vivo. (PMID:28266506)
• NRMT1 mutants N209I (endometrial cancer) and P211S (lung cancer) alter its catalytic activity and decrease N-terminal trimethylation. (PMID:28556566)
• The NRMT2 expression activates NRMT1 activity, not through priming, but by increasing its stability and substrate affinity. (PMID:30151928)
• Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues. (PMID:32605369)
• Modulation of N-terminal methyltransferase 1 by an N(6)-methyladenosine-based epitranscriptomic mechanism. (PMID:33561748)
• Methyltransferase-like protein 11A promotes migration of cervical cancer cells via up-regulating ELK3. (PMID:34450313)
• Age-related neurodegeneration and cognitive impairments of NRMT1 knockout mice are preceded by misregulation of RB and abnormal neural stem cell development. (PMID:34711807)
• Pan-cancer analysis reveals the pro-oncogenic role of N6-methyladenosine (m6A)-regulated NTMT1 in head and neck squamous cell carcinoma. (PMID:38014887)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	ntmt1	ENSDARG00000022399
mus_musculus	Ntmt1	ENSMUSG00000026857
rattus_norvegicus	Ntmt1	ENSRNOG00000024809
drosophila_melanogaster	Ntmt	FBGN0033457
caenorhabditis_elegans	homt-1	WBGENE00022277

Paralogs (1): NTMT2 (ENSG00000203740)

Protein

Protein identifiers

N-terminal Xaa-Pro-Lys N-methyltransferase 1 — Q9BV86 (reviewed: Q9BV86)

Alternative names: Alpha N-terminal protein methyltransferase 1A, Methyltransferase-like protein 11A, N-terminal RCC1 methyltransferase, X-Pro-Lys N-terminal protein methyltransferase 1A

All UniProt accessions (4): Q9BV86, S4R338, S4R344, S4R3J7

UniProt curated annotations — full annotation on UniProt →

Function. Distributive alpha-N-methyltransferase that methylates the N-terminus of target proteins containing the N-terminal motif [Ala/Gly/Pro/Ser]-Pro-Lys when the initiator Met is cleaved. Specifically catalyzes mono-, di- or tri-methylation of the exposed alpha-amino group of the Ala, Gly or Ser residue in the [Ala/Gly/Ser]-Pro-Lys motif and mono- or di-methylation of Pro in the Pro-Pro-Lys motif. Some of the substrates may be primed by NTMT2-mediated monomethylation. Catalyzes the trimethylation of the N-terminal Gly in CENPA (after removal of Met-1). Responsible for the N-terminal methylation of KLHL31, MYL2, MYL3, RB1, RCC1, RPL23A and SET. Required during mitosis for normal bipolar spindle formation and chromosome segregation via its action on RCC1.

Subcellular location. Nucleus.

Similarity. Belongs to the methyltransferase superfamily. NTM1 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9BV86-1	1	yes
Q9BV86-2	2

RefSeq proteins (9): NP_001273725, NP_001273726, NP_001273727, NP_001273728, NP_001273729, NP_001273730, NP_001273731, NP_001273732, NP_054783* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR008576	MeTrfase_NTM1	Family
IPR029063	SAM-dependent_MTases_sf	Homologous_superfamily

Pfam: PF05891

Enzyme classification (BRENDA):

• EC 2.1.1.244 — protein N-terminal methyltransferase (BRENDA: 5 organisms, 114 substrates, 37 inhibitors, 30 Km, 20 kcat entries)

Substrate kinetics (BRENDA)

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

Substrate	Km (mM)	Measurements
N-TERMINAL-SPKRIA-[RCC1]	0.0032–0.263	3
SSKRAKAKTTKKRP	0.0044–0.0156	3
N-TERMINAL-SPKRIAKRRSPP	0.0031–0.0049	2
N-TERMINAL-[RCC1]	0.002–0.0021	2
SPKRIAKRRSPPADA	0.0009–0.0011	2
(E)-HEX-2-EN-5-YNYL-S-ADENOSYL-L-METHIONINE	0.0014	1
APKRQSPLPP	0.002	1
APKRVVQLSL	0.0031	1
N-TERMINAL-DIMETHYL-SPKRIAKRRS	0.0043	1
N-TERMINAL-LPKRIA	0.0054	1
N-TERMINAL-METHYL-SPKRIAKRRS	0.0014	1
N-TERMINAL-PPKRIA	0.0003	1
N-TERMINAL-RPKRIA	0.004	1
N-TERMINAL-SPKRIAKRR	0.0014	1
N-TERMINAL-SPKRIAKRRS	0.0009	1

Catalyzed reactions (Rhea), 3 shown:

• N-terminal L-alanyl-L-prolyl-L-lysyl-[protein] + 3 S-adenosyl-L-methionine = N-terminal N,N,N-trimethyl-L-alanyl-L-prolyl-L-lysyl-[protein] + 3 S-adenosyl-L-homocysteine + 3 H(+) (RHEA:54712)
• N-terminal L-seryl-L-prolyl-L-lysyl-[protein] + 3 S-adenosyl-L-methionine = N-terminal N,N,N-trimethyl-L-seryl-L-prolyl-L-lysyl-[protein] + 3 S-adenosyl-L-homocysteine + 3 H(+) (RHEA:54724)
• N-terminal L-prolyl-L-prolyl-L-lysyl-[protein] + 2 S-adenosyl-L-methionine = N-terminal N,N-dimethyl-L-prolyl-L-prolyl-L-lysyl-[protein] + 2 S-adenosyl-L-homocysteine + 2 H(+) (RHEA:54736)

UniProt features (55 total): mutagenesis site 16, helix 12, strand 9, binding site 5, turn 4, sequence conflict 3, chain 2, modified residue 2, initiator methionine 1, splice variant 1

Structure

Experimental structures (PDB)

18 structures.

PDB	Method	Resolution (Å)
5CVD	X-RAY DIFFRACTION	1.3
6WJ7	X-RAY DIFFRACTION	1.42
5E1D	X-RAY DIFFRACTION	1.45
6DTN	X-RAY DIFFRACTION	1.48
6KDQ	X-RAY DIFFRACTION	1.5
5CVE	X-RAY DIFFRACTION	1.5
6PVB	X-RAY DIFFRACTION	1.5
5E1B	X-RAY DIFFRACTION	1.65
6WH8	X-RAY DIFFRACTION	1.73
2EX4	X-RAY DIFFRACTION	1.75
5E1M	X-RAY DIFFRACTION	1.75
5E2A	X-RAY DIFFRACTION	1.75
6PVA	X-RAY DIFFRACTION	1.84
5E2B	X-RAY DIFFRACTION	1.95
5E1O	X-RAY DIFFRACTION	2
7K3D	X-RAY DIFFRACTION	2.34
7SS1	X-RAY DIFFRACTION	2.4
7U1M	X-RAY DIFFRACTION	3.17

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9BV86-F1	97.56	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.

Ligand- & substrate-binding residues (5): 69; 74; 91–93; 119–120; 135

Post-translational modifications (2): 1, 2

Mutagenesis-validated functional residues (16):

Position	Phenotype
19	decreased methyltransferase activity with cenpa.
19	reduced methyltransferase activity with cenpa.
20	nearly abolishes methyltransferase activity with cenpa.
136	strongly reduces methyltransferase activity with cenpa.
167	does not affect methyltransferase activity.
167	abolishes methyltransferase activity with cenpa.
168	decreased methyltransferase activity.
168	loss of methyltransferase activity.
177	induces a slight decrease in methyltransferase activity.
177	induces a strong decrease in methyltransferase activity.
177	strongly reduces methyltransferase activity with cenpa.
180	induces a decrease in methyltransferase activity.
180	induces a strong decrease in methyltransferase activity.
180	reduced methyltransferase activity with cenpa.
182	induces a slight decrease in methyltransferase activity.
182	induces a strong decrease in methyltransferase activity.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 93 (showing top): GOBP_PEPTIDYL_SERINE_MODIFICATION, TGACCTY_ERR1_Q2, E4F1_Q6, HIF1_Q3, GOBP_PEPTIDYL_PROLINE_MODIFICATION, GOBP_CHROMATIN_REMODELING, GOBP_METHYLATION, TGACCTTG_SF1_Q6, GOBP_N_TERMINAL_PROTEIN_AMINO_ACID_MODIFICATION, SANSOM_APC_MYC_TARGETS, SANSOM_APC_TARGETS_REQUIRE_MYC, GOBP_CELL_CYCLE_PROCESS, GOMF_PROTEIN_METHYLTRANSFERASE_ACTIVITY, GOMF_S_ADENOSYLMETHIONINE_DEPENDENT_METHYLTRANSFERASE_ACTIVITY, GOBP_SPINDLE_ORGANIZATION

GO Biological Process (9): spindle organization (GO:0007051), chromosome segregation (GO:0007059), N-terminal peptidyl-glycine methylation (GO:0018013), N-terminal peptidyl-proline dimethylation (GO:0018016), N-terminal peptidyl-serine dimethylation (GO:0035572), N-terminal peptidyl-serine trimethylation (GO:0035573), chromatin remodeling (GO:0006338), N-terminal protein amino acid methylation (GO:0006480), methylation (GO:0032259)

GO Molecular Function (6): protein methyltransferase activity (GO:0008276), histone methyltransferase activity (GO:0042054), N-terminal protein N-methyltransferase activity (GO:0071885), protein binding (GO:0005515), methyltransferase activity (GO:0008168), transferase activity (GO:0016740)

GO Cellular Component (4): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
cell cycle process	2
N-terminal peptidyl-serine methylation	2
protein methyltransferase activity	2
microtubule cytoskeleton organization	1
N-terminal protein amino acid methylation	1
peptidyl-glycine modification	1
N-terminal peptidyl-proline methylation	1
chromatin organization	1
protein methylation	1
N-terminal protein amino acid modification	1
metabolic process	1
methyltransferase activity	1
catalytic activity, acting on a protein	1
histone modifying activity	1
S-adenosylmethionine-dependent methyltransferase activity	1
binding	1
transferase activity, transferring one-carbon groups	1
catalytic activity	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
intracellular anatomical structure	1
cytoplasm	1

Protein interactions and networks

STRING

1298 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
NTMT1	KLHL31	Q9H511	882
NTMT1	RCC1	P18754	878
NTMT1	RPL23A	P29316	807
NTMT1	RABIF	P47224	625
NTMT1	METTL17	Q9H7H0	606
NTMT1	RANBP1	P43487	596
NTMT1	EEF1AKMT2	Q5JPI9	590
NTMT1	METTL9	Q9H1A3	567
NTMT1	METTL27	Q8N6F8	539
NTMT1	METTL21A	Q8WXB1	537
NTMT1	CENPA	P49450	532
NTMT1	H2BC21	Q16778	527
NTMT1	DDB2	Q92466	515
NTMT1	PARP3	Q9Y6F1	504
NTMT1	METTL18	O95568	496

IntAct

41 interactions, top by confidence:

A	B	Type	Score
NTMT1	RCC1	psi-mi:“MI:0213”(methylation reaction)	0.560
NTMT1	RCC1	psi-mi:“MI:0407”(direct interaction)	0.560
GLYR1	NTMT1	psi-mi:“MI:0915”(physical association)	0.560
CCL5	C4A	psi-mi:“MI:0914”(association)	0.530
DRG1	LRRC41	psi-mi:“MI:0914”(association)	0.530
NTMT1	RB1	psi-mi:“MI:0213”(methylation reaction)	0.440
NTMT1	SET	psi-mi:“MI:0213”(methylation reaction)	0.440
NTMT1	RBMX	psi-mi:“MI:0915”(physical association)	0.400
Rcc1	WDR46	psi-mi:“MI:0914”(association)	0.350
LRRK2		psi-mi:“MI:0914”(association)	0.350
VAMP4	NBAS	psi-mi:“MI:0914”(association)	0.350
DENR	ATG13	psi-mi:“MI:0914”(association)	0.350
TIRAP	DHPS	psi-mi:“MI:0914”(association)	0.350
DRG1	LRRC41	psi-mi:“MI:0914”(association)	0.350
PRKCE	PRPSAP2	psi-mi:“MI:0914”(association)	0.350
DRG1	RPS3A	psi-mi:“MI:0914”(association)	0.350
HNRNPCL2	SMCHD1	psi-mi:“MI:0914”(association)	0.350
SNAP91	GMNN	psi-mi:“MI:0914”(association)	0.350
DRG1	ACTA2	psi-mi:“MI:0914”(association)	0.350
VCY	WDR45B	psi-mi:“MI:0914”(association)	0.350
VRK2	TMEM192	psi-mi:“MI:0914”(association)	0.350
DNAJB6	SCAMP1	psi-mi:“MI:0914”(association)	0.350
SMYD3	GYG2	psi-mi:“MI:0914”(association)	0.350

BioGRID (71): DDB2 (Biochemical Activity), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Co-fractionation), NTMT1 (Co-fractionation), NTMT1 (Co-fractionation), NTMT1 (Co-fractionation), NTMT1 (Reconstituted Complex), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS), NTMT1 (Affinity Capture-MS)

ESM2 similar proteins: A2APY7, A3KP37, A7YW45, B2GV71, M1BYJ7, O08691, O08701, O14744, O46504, O80543, P20373, P41819, P49900, P78540, P78697, Q1JPL4, Q2LZ79, Q337B8, Q3KRD0, Q4G064, Q4R5M3, Q4V7R3, Q58DL1, Q5R698, Q5RBS1, Q5TEU4, Q66KM2, Q66L51, Q6AY46, Q6BSY5, Q6C7H6, Q6FKY3, Q6NUA1, Q6NYF0, Q6PI48, Q6YXZ7, Q75C90, Q7SYK1, Q7T0W5, Q80XC2

Diamond homologs: A2XMJ1, A8WVR2, B1H2P7, B2RXM4, B8JM82, D2H163, D3ZVR1, O13748, P38340, Q10CT5, Q2T9N3, Q4KL94, Q4KLE6, Q55DH6, Q5BJX0, Q5PP70, Q5VVY1, Q6NN40, Q6NWX7, Q8R2U4, Q9BV86, Q9N4D9, Q23552, Q89XU2, Q9M571

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	14
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2325 predictions. Top by Δscore:

Variant	Effect	Δscore
9:129613420:T:TA	donor_gain	1.0000
9:129613477:T:TA	donor_gain	1.0000
9:129613513:T:A	donor_gain	1.0000
9:129613598:C:CC	acceptor_gain	1.0000
9:129620065:A:AC	donor_gain	1.0000
9:129620066:C:CC	donor_gain	1.0000
9:129632841:G:GT	donor_gain	1.0000
9:129632841:G:T	donor_gain	1.0000
9:129632864:GG:G	donor_gain	1.0000
9:129632865:GG:G	donor_gain	1.0000
9:129634053:GGAA:G	acceptor_gain	1.0000
9:129634184:TTC:T	donor_gain	1.0000
9:129634296:G:GG	donor_gain	1.0000
9:129634300:GTGA:G	donor_gain	1.0000
9:129634301:TGAT:T	donor_gain	1.0000
9:129634303:A:AG	donor_gain	1.0000
9:129634303:A:G	donor_gain	1.0000
9:129634303:ATAG:A	donor_loss	1.0000
9:129634304:TAGG:T	donor_loss	1.0000
9:129634305:AGGT:A	donor_loss	1.0000
9:129634306:GG:G	donor_loss	1.0000
9:129634307:G:T	donor_loss	1.0000
9:129634308:T:A	donor_loss	1.0000
9:129635203:CCCA:C	acceptor_loss	1.0000
9:129635204:CCA:C	acceptor_loss	1.0000
9:129635205:CA:C	acceptor_loss	1.0000
9:129635206:A:AG	acceptor_gain	1.0000
9:129635206:AG:A	acceptor_gain	1.0000
9:129635207:G:GT	acceptor_gain	1.0000
9:129635207:GG:G	acceptor_gain	1.0000

AlphaMissense

1485 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
9:129634109:G:A	G73E	0.999
9:129634297:T:A	W136R	0.999
9:129634297:T:C	W136R	0.999
9:129635289:A:T	K166I	0.999
9:129635290:A:C	K166N	0.999
9:129635290:A:T	K166N	0.999
9:129632837:C:T	S45F	0.998
9:129634108:G:T	G73W	0.998
9:129634109:G:T	G73V	0.998
9:129634112:G:C	R74T	0.998
9:129634112:G:T	R74M	0.998
9:129634113:G:C	R74S	0.998
9:129634113:G:T	R74S	0.998
9:129634288:T:A	W133R	0.998
9:129634288:T:C	W133R	0.998
9:129634299:G:C	W136C	0.998
9:129634299:G:T	W136C	0.998
9:129634085:C:A	A65D	0.997
9:129635214:T:C	L141P	0.997
9:129635296:C:A	N168K	0.997
9:129635296:C:G	N168K	0.997
9:129634095:T:G	C68W	0.996
9:129634097:G:A	G69E	0.996
9:129634103:G:A	G71D	0.996
9:129634108:G:A	G73R	0.996
9:129634108:G:C	G73R	0.996
9:129635291:G:C	D167H	0.996
9:129635292:A:C	D167A	0.996
9:129635292:A:T	D167V	0.996
9:129635336:A:C	S182R	0.996

dbSNP variants (sampled 300 via entrez): RS1000035606 (9:129635170 G>A,C,T), RS1000043386 (9:129608086 G>A), RS1000132120 (9:129629356 G>A), RS1000259437 (9:129625360 G>A), RS1000319099 (9:129619251 A>G,T), RS1000412158 (9:129628259 A>T), RS1000636716 (9:129636227 CAAA>C,CA,CAA,CAAAA,CAAAAA), RS1000769129 (9:129631098 CTCTG>C), RS1000800168 (9:129630856 C>T), RS1000859678 (9:129621294 C>G), RS1000889691 (9:129614956 A>G), RS1001009480 (9:129609967 CTG>C), RS1001146750 (9:129609604 G>T), RS1001261290 (9:129615195 G>A,T), RS1001322600 (9:129620438 G>A,C)

Disease associations

OMIM: gene MIM:613560 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): dystonic disorder (MONDO:0003441)

Orphanet (0):

HPO phenotypes

1 total (1 of 1 shown, HPO-id order):

HPO	Term
HP:0001332	Dystonia

GWAS associations

0 associations (top):

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D020821	Dystonic Disorders	C10.228.662.300

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL4523442 (SINGLE PROTEIN), CHEMBL5291694 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 76 (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
CHEMBL4297611	VENGLUSTAT	3	76

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

Binding affinities (BindingDB)

38 measured of 48 human assays (48 total across all organisms); most potent 38 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(S)-((S)-6-amino-1-(((S)-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	40 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-hydroxyphenyl)acetyl]pyrrolidine-2-carboxamide	IC50	54 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-(((2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	60 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-((2-(2-amino-2-oxoethoxy)ethyl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	65 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-N-((6S,9S,12S,15S,18S,21S,24S)-1,28-diamino-6-carbamoyl-9,12,15,18,21-pentakis(3-guanidinopropyl)-1-imino-8,11,14,17,20,23-hexaoxo-2,7,10,13,16,19,22-heptaazaoctacosan-24-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	68 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-(((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	79 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-6-amino-1-((2-(2-amino-2-oxoethoxy)ethyl)amino)-1-oxohexan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	86 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-(((S)-1-amino-1-oxopent-4-yn-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	90 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-(((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)pyrrolidine-2-carboxamide	IC50	95 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-6-amino-1-((3-carbamoylphenyl)amino)-1-oxohexan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	100 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-((2-(2-amino-2-oxoethoxy)ethyl)amino)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(3,4-dihydroxyphenyl)acetyl)pyrrolidine-2-carboxamide	IC50	110 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-1-(2-(1H-indol-4-yl)acetyl)-N-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)pyrrolidine-2-carboxamide	IC50	160 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(2-(4-hydroxyphenyl)acetyl)-L-prolyl-L-lysyl-L-arginylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L-glutaminyl-L-arginyl-L-arginyl-L-arginine	IC50	230 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1,6-diamino-1-oxohexan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	320 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	400 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)(methyl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	590 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-1-oxopent-4-yn-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	670 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	840 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-1-oxopropan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	960 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	960 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(quinolin-8-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1200 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-1-(((1H-benzo[d]imidazol-2-yl)methyl)amino)-6-amino-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1300 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(4-fluoronaphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1400 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(4-(hydroxymethyl)phenyl)acetyl)pyrrolidine-2-carboxamide	IC50	1500 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-((2-(2-amino-2-oxoethoxy)ethyl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1560 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(4-bromonaphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1600 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1620 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	1630 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-phenethylpyrrolidine-2-carboxamide	IC50	1770 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-((E)-3-(4-hydroxyphenyl)acryloyl)pyrrolidine-2-carboxamide	IC50	2500 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-1,6-diamino-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	2800 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-((2-amino-2-oxoethyl)amino)-1-oxohexan-2-yl)-1-(2-(naphthalen-1-yl)acetyl)pyrrolidine-2-carboxamide	IC50	3130 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(benzo[d][1,3]dioxol-5-yl)acetyl)pyrrolidine-2-carboxamide	IC50	5000 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(4S)-5-amino-4-[[(2S)-6-amino-2-[[(2S)-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-5-oxopentanoic acid	IC50	5760 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-6-amino-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-1-oxohexan-2-yl)-1-(2-(4-nitrophenyl)acetyl)pyrrolidine-2-carboxamide	IC50	8960 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-1-(((1H-benzo[d]imidazol-2-yl)methyl)amino)-6-amino-1-oxohexan-2-yl)-1-(2-(4-hydroxyphenyl)acetyl)pyrrolidine-2-carboxamide	IC50	10000 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(2-chloroacetyl)-L-prolyl-L-prolyl-L-lysyl-L-arginine	IC50	16000 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof
(S)-((S)-1-(((S)-1-amino-5-guanidino-1-oxopentan-2-yl)amino)-5-guanidino-1-oxopentan-2-yl)-1-(2-(4-hydroxyphenyl)acetyl)pyrrolidine-2-carboxamide	IC50	20700 nM	US-12479887: Inhibitors for protein n-terminal methyltransferase and uses thereof

ChEMBL bioactivities

134 potent at pChembl≥5 of 159 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.89	Ki	0.13	nM	CHEMBL4647584
9.31	Ki	0.49	nM	CHEMBL4647584
9.21	Ki	0.62	nM	CHEMBL4647584
9.14	Ki	0.73	nM	CHEMBL4647584
9.11	Ki	0.78	nM	CHEMBL4647726
8.89	Ki	1.3	nM	CHEMBL4647726
8.62	Ki	2.4	nM	CHEMBL4647726
8.61	Kd	2.47	nM	CHEMBL4647584
8.60	Ki	2.5	nM	CHEMBL4647726
8.31	Ki	4.9	nM	CHEMBL4645959
8.27	Ki	5.4	nM	CHEMBL4645959
8.17	Ki	6.8	nM	CHEMBL4645959
8.09	Ki	8.2	nM	CHEMBL4645959
8.08	Kd	8.28	nM	CHEMBL5403284
7.82	Ki	15	nM	CHEMBL4647584
7.57	IC50	27	nM	CHEMBL5403284
7.49	Kd	32.5	nM	VENGLUSTAT
7.46	IC50	35	nM	CHEMBL4518093
7.43	Kd	36.9	nM	CHEMBL5403284
7.41	Ki	39	nM	CHEMBL4518093
7.39	Ki	41	nM	CHEMBL4647726
7.39	Kd	41	nM	CHEMBL4647726
7.33	Kd	46.7	nM	CHEMBL4645959
7.27	IC50	54	nM	CHEMBL4787034
7.09	IC50	82	nM	CHEMBL4647584
7.08	IC50	84	nM	CHEMBL4635903
7.00	Ki	99	nM	CHEMBL4645959
7.00	IC50	100	nM	CHEMBL4744916
7.00	IC50	100	nM	CHEMBL4757419
7.00	IC50	100	nM	CHEMBL4787034
6.99	Ki	103	nM	CHEMBL4475410
6.96	IC50	110	nM	CHEMBL5402262
6.92	Ki	121	nM	CHEMBL4575245
6.89	IC50	130	nM	CHEMBL4647726
6.89	IC50	130	nM	CHEMBL4761806
6.80	IC50	158	nM	CHEMBL4518093
6.80	Kd	160	nM	VENGLUSTAT
6.70	IC50	200	nM	CHEMBL4636288
6.70	IC50	200	nM	CHEMBL4787034
6.70	IC50	200	nM	CHEMBL4777235
6.64	IC50	230	nM	CHEMBL4777235
6.58	IC50	260	nM	CHEMBL4645959
6.52	Kd	300	nM	CHEMBL4787034
6.52	IC50	300	nM	VENGLUSTAT
6.52	IC50	300	nM	CHEMBL5427360
6.52	IC50	300	nM	CHEMBL5402262
6.51	Kd	310	nM	CHEMBL4647584
6.50	IC50	320	nM	CHEMBL4633108
6.47	IC50	340	nM	CHEMBL4740501
6.47	IC50	340	nM	CHEMBL4796649

PubChem BioAssay actives

136 with measured affinity, of 331 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
(2S)-2-amino-4-[4-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]butyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660881: Time dependent inhibition of NTMT1 (unknown origin) pre-incubated for 120 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay based Morrison’s quadratic equation analysis	ki	0.0001	uM
(2S)-2-amino-4-[3-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660879: Time dependent inhibition of NTMT1 (unknown origin) pre-incubated for 60 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay based Morrison’s quadratic equation analysis	ki	0.0008	uM
(2S)-2-amino-4-[2-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]ethyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660880: Time dependent inhibition of NTMT1 (unknown origin) pre-incubated for 90 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay based Morrison’s quadratic equation analysis	ki	0.0049	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-fluoro-3-hydroxyphenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1966366: Binding affinity to N-terminal 6-his tagged TEV fused full length human NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-Codonplus(DE3)-RIL cells assessed as dissociation constant in the presence of SAM by isothermal titration calorimetry	kd	0.0083	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-fluorophenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1864739: Binding affinity to NTMT1 (unknown origin) assessed as dissociation constant in presence of SAM by isothermal titration calorimetry analysis	kd	0.0325	uM
(2S)-2-amino-4-[3-[(2S)-2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1593491: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells preincubated for 10 mins in presence of SAM followed by GPKRIA addition and measured after 20 mins by MALDI TOF-MS analysis	ic50	0.0350	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-hydroxyphenyl)acetyl]pyrrolidine-2-carboxamide	1721183: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells pre-incubated for 10 mins in presence of SAM and SAHH before RCC1-6 addition and measured after 15 mins by fluorescence based SAHH-coupled assay	ic50	0.0540	uM
(2S)-2-amino-4-[4-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]butyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660875: Inhibition of NTMT1 (unknown origin) pre-incubated for 10 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay	ic50	0.0840	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.1000	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-hydroxyphenyl)acetyl]pyrrolidine-2-carboxamide	1721195: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells assessed as Me3RCC1 level at 50 uM pre-incubated for 10 mins before RCC1 substrate addition and measured after 15 mins by Western blot analysis relative to control	ic50	0.1000	uM
(2S)-2-amino-4-[3-[(2S)-2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1593486: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using GPKRIA as substrate preincubated for 10 mins in presence of SAM followed by substrate addition by fluorescence assay	ki	0.1030	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-chloro-3-hydroxyphenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1966359: Inhibition of N-terminal 6-his tagged TEV fused full length human NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-Codonplus(DE3)-RIL cells using GPKRIA peptide as substrate preincubated with compound for 10 mins followed by substrate addition and measured immediately by SAHH-coupled fluorescence analysis	ic50	0.1100	uM
(2S)-2-amino-4-[3-[(2S)-2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1593486: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using GPKRIA as substrate preincubated for 10 mins in presence of SAM followed by substrate addition by fluorescence assay	ki	0.1210	uM
(2S)-N-[(2S)-6-amino-1-(3-carbamoylanilino)-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.1300	uM
(2S)-2-amino-4-[3-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660875: Inhibition of NTMT1 (unknown origin) pre-incubated for 10 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay	ic50	0.2000	uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-1-[2-(4-hydroxyphenyl)acetyl]pyrrolidine-2-carbonyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]pentanediamide	1721195: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells assessed as Me3RCC1 level at 50 uM pre-incubated for 10 mins before RCC1 substrate addition and measured after 15 mins by Western blot analysis relative to control	ic50	0.2000	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-fluoro-2-hydroxyphenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1966359: Inhibition of N-terminal 6-his tagged TEV fused full length human NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-Codonplus(DE3)-RIL cells using GPKRIA peptide as substrate preincubated with compound for 10 mins followed by substrate addition and measured immediately by SAHH-coupled fluorescence analysis	ic50	0.3000	uM
(2S)-2-amino-4-[2-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]ethyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660875: Inhibition of NTMT1 (unknown origin) pre-incubated for 10 mins before GPKRIA peptide substrate addition by SAHH coupled fluorescence assay	ic50	0.3200	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.3400	uM
(2S)-N-[(2S)-6-amino-1-(2-carbamoylanilino)-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.3400	uM
N-methyl-2,3-diphenyl-1,2,4-thiadiazol-5-imine	1864737: Inhibition of full length His-NTMT1 (1 to 222 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as SAH production by Mtase-glo luminescence assay	ic50	0.4600	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]-methylamino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.4700	uM
(2S)-2-amino-4-[5-[[2-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]pentyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1660884: Binding affinity to NTMT1 (unknown origin) assessed as binding constant Kd2 by ITC assay	kd	0.4800	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.4900	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(3-hydroxyphenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1966359: Inhibition of N-terminal 6-his tagged TEV fused full length human NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-Codonplus(DE3)-RIL cells using GPKRIA peptide as substrate preincubated with compound for 10 mins followed by substrate addition and measured immediately by SAHH-coupled fluorescence analysis	ic50	0.5600	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-1-oxopropan-2-yl]-methylamino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.5800	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]-methylamino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.6000	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-bromonaphthalen-1-yl)acetyl]pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.6800	uM
(2S)-N-[(2S)-6-amino-1-(1H-benzimidazol-2-ylmethylamino)-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.7400	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.7800	uM
(2S)-2-amino-4-[[1-[(2S)-1-[(2S)-2-[[(2S)-6-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]triazol-4-yl]methyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1593532: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using SPKRIAKRRS as substrate in presence of SAM by fluorescence assay	ic50	0.8100	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.8400	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-fluoronaphthalen-1-yl)acetyl]pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.8800	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-quinolin-8-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.8900	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1864747: Inhibition of full length NTMT1 (1 to 222 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using GPKRIA as substrate preincubated for 10 mins followed by substrate addition measured after 15 mins by microplate reader method	ic50	0.9100	uM
(2S)-N-[(2S)-6-amino-1-oxo-1-(2-phenylethylamino)hexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1966357: Inhibition of NTMT1 (unknown origin) by SAHH-coupled fluorescence assay	ic50	0.9300	uM
(2S)-2-amino-4-[3-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]propyl-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl]amino]butanoic acid	1593531: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells using peptide substrate in presence of SAM by fluorescence assay	ic50	0.9400	uM
(2S)-N-[(2S)-6-amino-1-(naphthalen-1-ylamino)-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	0.9700	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-(4-hydroxyphenyl)acetyl]pyrrolidine-2-carboxamide	1721183: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells pre-incubated for 10 mins in presence of SAM and SAHH before RCC1-6 addition and measured after 15 mins by fluorescence based SAHH-coupled assay	ic50	1.0000	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	1.1000	uM
(2S)-N-[(2S)-6-amino-1-anilino-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	1.1000	uM
(2S)-N-[(2S)-6-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	1.2000	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carboxamide	1694800: Inhibition of recombinant human N-terminal His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL using GPKRIA peptide and SAM as substrate pre-incubated for 10 mins in presence of SAM followed by substrate addition by SAHH coupled fluorescence assay	ic50	1.3000	uM
(2S)-N-[(2S)-6-amino-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]-1-[2-[4-(hydroxymethyl)phenyl]acetyl]pyrrolidine-2-carboxamide	1721183: Inhibition of recombinant human full-length His6-tagged NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-CodonPlus(DE3)-RIL competent cells pre-incubated for 10 mins in presence of SAM and SAHH before RCC1-6 addition and measured after 15 mins by fluorescence based SAHH-coupled assay	ic50	1.5000	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-bromophenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1864747: Inhibition of full length NTMT1 (1 to 222 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using GPKRIA as substrate preincubated for 10 mins followed by substrate addition measured after 15 mins by microplate reader method	ic50	1.5000	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(6-fluoro-3-pyridinyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1966359: Inhibition of N-terminal 6-his tagged TEV fused full length human NTMT1 (1 to 222 residues) expressed in Escherichia coli BL21-Codonplus(DE3)-RIL cells using GPKRIA peptide as substrate preincubated with compound for 10 mins followed by substrate addition and measured immediately by SAHH-coupled fluorescence analysis	ic50	1.5000	uM
[(3S)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-methylphenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1864747: Inhibition of full length NTMT1 (1 to 222 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using GPKRIA as substrate preincubated for 10 mins followed by substrate addition measured after 15 mins by microplate reader method	ic50	1.7000	uM
[(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-[2-[2-(4-fluorophenyl)-1,3-thiazol-4-yl]propan-2-yl]carbamate	1864747: Inhibition of full length NTMT1 (1 to 222 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using GPKRIA as substrate preincubated for 10 mins followed by substrate addition measured after 15 mins by microplate reader method	ic50	1.7000	uM
(2S,4R)-N-[[2-[2-[[2-[[(2S)-6-amino-2-[[(2S)-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carbonyl]amino]hexanoyl]amino]benzoyl]amino]ethoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-4-hydroxy-1-[(2S)-3-methyl-2-(3-oxo-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide	1945225: Inhibition of NTMT1 (unknown origin) using SPKRIAKRRS(CONH2) peptide as substrate assessed as SAH production incubated for 10 mins in the presence of SAM by HPLC analysis	ic50	1.7700	uM
(2S,4R)-N-[[2-[2-[2-[[2-[[(2S)-6-amino-2-[[(2S)-1-(2-naphthalen-1-ylacetyl)pyrrolidine-2-carbonyl]amino]hexanoyl]amino]benzoyl]amino]ethoxy]ethoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-4-hydroxy-1-[(2S)-3-methyl-2-(3-oxo-1H-isoindol-2-yl)butanoyl]pyrrolidine-2-carboxamide	1945225: Inhibition of NTMT1 (unknown origin) using SPKRIAKRRS(CONH2) peptide as substrate assessed as SAH production incubated for 10 mins in the presence of SAM by HPLC analysis	ic50	2.0000	uM

CTD chemical–gene interactions

25 total (human), top 25 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	decreases expression, increases expression	3
Cadmium Chloride	decreases expression, increases expression	2
GSK-J4	increases expression	1
bisphenol A	decreases expression	1
sodium arsenate	decreases expression	1
beta-lapachone	increases expression	1
mono-(2-ethylhexyl)phthalate	decreases expression	1
manganese chloride	increases abundance, increases expression	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
abrine	increases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	decreases expression, increases response to substance	1
LDN 193189	affects cotreatment, decreases expression	1
Air Pollutants	affects expression, increases abundance	1
Arsenic	affects expression	1
Dichlorodiphenyl Dichloroethylene	increases expression	1
Doxorubicin	decreases expression	1
Ivermectin	decreases expression	1
Manganese	increases expression, increases abundance	1
Nickel	increases expression	1
Ozone	increases abundance, affects expression	1
Smoke	decreases expression	1
Tobacco Smoke Pollution	increases expression	1
Tretinoin	decreases expression	1
Copper Sulfate	increases expression	1

ChEMBL screening assays

119 unique, capped per target: 119 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4324380	Binding	Inhibition of NTMT1 (unknown origin) assessed as enzyme activity at 3.7 uM using GPKRIA peptide as substrate preincubated for 10 mins in presence of AdoMet followed by susbtrate addition by fluorescence based SAHH enzyme coupled assay relat	Novel Propargyl-Linked Bisubstrate Analogues as Tight-Binding Inhibitors for Nicotinamide N-Methyltransferase. — J Med Chem

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00142259	PHASE4	UNKNOWN	Efficacy and Safety of DBS of the GPi in Patients With Primary Generalized and Segmental Dystonia
NCT00950196	PHASE4	COMPLETED	Amantadine for Improving Neurologic Symptoms in Ataxia-Telangiectasia
NCT00998660	PHASE4	COMPLETED	RECHARGE Sub-Study to the Implantable Systems Performance Registry (ISPR)
NCT02263417	PHASE4	COMPLETED	A Randomized Controlled Trail Comparing Subthalamic and Pallidal Deep Brain Stimulation for Dystonia
NCT00169403	PHASE3	UNKNOWN	Pallidal Stimulation in Patients With Idiopathic Generalised Dystonia
NCT03232320	PHASE3	COMPLETED	Meditoxin® Treatment in Patients With Cervical Dystonia
NCT00001784	PHASE2	COMPLETED	Mexiletine for the Treatment of Focal Dystonia
NCT00105430	PHASE2	COMPLETED	Deep Brain Stimulation for Cervical Dystonia
NCT00106782	PHASE2	COMPLETED	Transcranial Electrical Polarization to Treat Focal Hand Dystonia
NCT00122044	PHASE2	COMPLETED	Childhood Hypertonia of Central Origin: A Trial of Anticholinergic Treatment Effects
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NCT02470325	PHASE2	UNKNOWN	The Effects of Cannabis on Dystonia and Spasticity on Pediatric Patients
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NCT07304089	PHASE2	RECRUITING	A Study to Evaluate the Efficacy, Safety, and Tolerability of VIM0423 in Individuals With Isolated Dystonia
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NCT02982304	PHASE1	UNKNOWN	Multi-Target Pallidal and Thalamic Deep Brain Stimulation for Hemi-Dystonia
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NCT02911103	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Deep Brain Stimulation Surgery for Focal Hand Dystonia
NCT04727177	EARLY_PHASE1	UNKNOWN	Precision-targeted Transcranial Magnetic Stimulation in the Treatment of Primary Dystonia
NCT00006336	Not specified	COMPLETED	Sensory Training to Treat Focal Dystonia
NCT00017875	Not specified	COMPLETED	Transcranial Magnetic Stimulation (TMS) Studies of Dystonia
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NCT00031369	Not specified	TERMINATED	Brain Anatomy in Dystonia
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NCT00355927	Not specified	UNKNOWN	Sedation During Microelectrode Recordings Before Deep Brain Stimulation for Movement Disorders.