NMT1

gene
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Also known as NMT

Summary

NMT1 (N-myristoyltransferase 1, HGNC:7857) is a protein-coding gene on chromosome 17q21.31, encoding Glycylpeptide N-tetradecanoyltransferase 1 (P30419). Adds a myristoyl group to the N-terminal glycine residue of certain cellular and viral proteins. It is a selective cancer dependency (DepMap: 67.6% of cell lines).

Myristate, a rare 14-carbon saturated fatty acid, is cotranslationally attached by an amide linkage to the N-terminal glycine residue of cellular and viral proteins with diverse functions. N-myristoyltransferase (NMT; EC 2.3.1.97) catalyzes the transfer of myristate from CoA to proteins. N-myristoylation appears to be irreversible and is required for full expression of the biologic activities of several N-myristoylated proteins, including the alpha subunit of the signal-transducing guanine nucleotide-binding protein (G protein) GO (GNAO1; MIM 139311) (Duronio et al., 1992 [PubMed 1570339]).

Source: NCBI Gene 4836 — RefSeq curated summary.

At a glance

  • GWAS associations: 18
  • Clinical variants (ClinVar): 43 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • Cancer dependency (DepMap): dependent in 67.6% of screened cell lines
  • MANE Select transcript: NM_021079

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:7857
Approved symbolNMT1
NameN-myristoyltransferase 1
Location17q21.31
Locus typegene with protein product
StatusApproved
AliasesNMT
Ensembl geneENSG00000136448
Ensembl biotypeprotein_coding
OMIM160993
Entrez4836

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 8 protein_coding, 8 nonsense_mediated_decay, 4 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000258960, ENST00000543908, ENST00000585561, ENST00000587014, ENST00000587120, ENST00000587670, ENST00000588455, ENST00000590114, ENST00000590310, ENST00000591931, ENST00000592654, ENST00000592782, ENST00000676753, ENST00000676828, ENST00000677949, ENST00000678332, ENST00000678576, ENST00000678606, ENST00000678938, ENST00000902321, ENST00000927701

RefSeq mRNA: 1 — MANE Select: NM_021079 NM_021079

CCDS: CCDS11494

Canonical transcript exons

ENST00000258960 — 12 exons

ExonStartEnd
ENSE000013243124506131745061460
ENSE000034829034509619445096285
ENSE000035028314508164445081752
ENSE000035081554509368545093803
ENSE000035304694509838245098552
ENSE000036579194509712845097244
ENSE000037573064508650845086652
ENSE000038890064510561945109016
ENSE000038891704510295145103121
ENSE000038921024510485945104996
ENSE000038943954510370945103876
ENSE000038954014509940545099513

Expression profiles

Bgee: expression breadth ubiquitous, 296 present calls, max score 94.42.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 128.3673 / max 1259.8621, expressed in 1827 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
161230128.22811827
1612310.080761
1612250.040631
1612290.01794

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
monocyteCL:000057694.42gold quality
right adrenal glandUBERON:000123394.34gold quality
islet of LangerhansUBERON:000000694.30gold quality
mononuclear cellCL:000084294.28gold quality
sural nerveUBERON:001548894.27gold quality
leukocyteCL:000073894.21gold quality
gastrocnemiusUBERON:000138894.09gold quality
left adrenal glandUBERON:000123493.95gold quality
right adrenal gland cortexUBERON:003582793.93gold quality
muscle of legUBERON:000138393.89gold quality
calcaneal tendonUBERON:000370193.87gold quality
left adrenal gland cortexUBERON:003582593.76gold quality
granulocyteCL:000009493.74gold quality
adrenal glandUBERON:000236993.50gold quality
adrenal cortexUBERON:000123593.46gold quality
right frontal lobeUBERON:000281093.38gold quality
adrenal tissueUBERON:001830393.31gold quality
smooth muscle tissueUBERON:000113593.16gold quality
prefrontal cortexUBERON:000045193.08gold quality
stromal cell of endometriumCL:000225592.93gold quality
lower esophagus muscularis layerUBERON:003583392.83gold quality
lower esophagusUBERON:001347392.82gold quality
lymph nodeUBERON:000002992.72gold quality
right lobe of liverUBERON:000111492.70gold quality
hindlimb stylopod muscleUBERON:000425292.70gold quality
thoracic aortaUBERON:000151592.67gold quality
right coronary arteryUBERON:000162592.67gold quality
descending thoracic aortaUBERON:000234592.67gold quality
esophagogastric junction muscularis propriaUBERON:003584192.66gold quality
ascending aortaUBERON:000149692.59gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes11.95

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

113 targeting NMT1, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-190A-3P100.0080.355520
HSA-MIR-5011-5P100.0083.465820
HSA-MIR-1277-5P100.0073.955056
HSA-MIR-5692B100.0071.322622
HSA-MIR-5692C100.0071.322622
HSA-MIR-9-5P100.0072.282361
HSA-MIR-4668-3P100.0068.742635
HSA-MIR-4262100.0073.263931
HSA-MIR-10401-5P99.9965.79948
HSA-MIR-3667-3P99.9967.171636
HSA-MIR-23B-5P99.9866.07587
HSA-MIR-211099.9666.681930
HSA-MIR-3605-5P99.9667.12932
HSA-MIR-493-5P99.9672.472382
HSA-MIR-4725-3P99.9669.532520
HSA-MIR-6780B-5P99.9669.602562
HSA-MIR-589-3P99.9169.622088
HSA-MIR-449399.9066.48977
HSA-MIR-367199.9073.043897
HSA-MIR-374A-5P99.9071.342923
HSA-MIR-374B-5P99.9069.982734
HSA-MIR-990299.8969.152250
HSA-MIR-427199.8868.322244
HSA-MIR-1211999.8768.351653
HSA-MIR-30D-3P99.8769.922917
HSA-MIR-30A-3P99.8769.742928
HSA-MIR-30E-3P99.8769.682942
HSA-MIR-369-3P99.8570.522264
HSA-MIR-5003-3P99.8569.292517
HSA-MIR-444799.8567.812900

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 67.6% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 17)

  • In this study, we found decreases in the mRNA levels of human NMT isoforms and the NMT activities in the course of HIV-1 infection in the human T-cell line (PMID:12220649)
  • role of HSC70 in the regulation of NMT (PMID:15156568)
  • NMT1 and NMT2 have only partially overlapping functions; NMT1 is critical for tumor cell proliferation (PMID:16123142)
  • Elevated N-myristoyltransferase activity is associated with oral squamous cell carcinoma (PMID:17549352)
  • N-myristoyltransferase may have a role in progression of colonic neoplasms (PMID:18021392)
  • Nef is preferentially myristoylated by NMT2, suggesting that selective inhibition of NMT2 may provide a novel means of blocking HIV virulence. (PMID:18089753)
  • These results strongly suggest that HIV-1 production is specifically associated with hNMT1, particularly hNMT1(L), but not with hNMT2 in vivo, contributing to the understanding of a step in HIV-1 replication. (PMID:18248763)
  • we propose a model of the Nef:NMT complex in which only the myristoyl moiety holds the two proteins together in complex and speculate that perhaps NMT chaperones Nef to the membrane and thereby protects the myristic acid group from the cytosol (PMID:21449607)
  • findings suggest that both NMT1 and hnRNP A2/B1 take part in the regulation of HIV-1 RNA expression through their mutual opposite effects on the viral RNA expression in HIV-1-producing cells (PMID:26074144)
  • These observations point at a previously unrecognized contribution of calnexin to the retention of NMT1 at the ER membrane. (PMID:26603938)
  • Genetic and pharmacologic evidence that inhibiting the N-myristoyltransferase NMT1 suppresses cell-cycle progression, proliferation, and malignant growth of prostate cancer cells. (PMID:29038344)
  • mTOR, a downstream target of PKB/Akt, regulates NMT1 in ER positive breast cancer cells (MCF7 cells). NMT1 increased with rapamycin treatment over the period of time with a concomitant decrease in mTOR phosphorylation. (PMID:30154572)
  • inhibition of NMT1 caused degraded proteins increase and ER stress, which cross-talked with mitochondria to produce more ROS. And both of oxidative stress and ER stress could activate JNK pathway, leading to autophagy which abrogated breast cancer progression especially triple-negative breast cancer (TNBC). (PMID:30446635)
  • Data showed that rheumatoid arthritis (RA) T cells had a defect in type I N-myristoyltransferase (NMT1) function, which prevented AMP-activated protein kinase (AMPK) activation. (PMID:30718913)
  • N-myristoyltransferase-1 deficiency blocks myristoylation of LAMTOR1 and inhibits bladder cancer progression. (PMID:34999170)
  • N-mytistoyltransferase 1 and 2 are potential tumor suppressors and novel targets of miR-182 in human non-small cell lung carcinomas. (PMID:35930829)
  • SPI1 Mediates N-Myristoyltransferase 1 to Advance Gastric Cancer Progression via PI3K/AKT/mTOR Pathway. (PMID:36967718)

Cross-species orthologs

6 orthologs

OrganismSymbolGene ID
danio_rerionmt1aENSDARG00000052966
danio_rerionmt1bENSDARG00000057206
mus_musculusNmt1ENSMUSG00000020936
rattus_norvegicusNmt1ENSRNOG00000002989
drosophila_melanogasterNmtFBGN0020392
caenorhabditis_elegansWBGENE00020549

Paralogs (1): NMT2 (ENSG00000152465)

Protein

Protein identifiers

Glycylpeptide N-tetradecanoyltransferase 1P30419 (reviewed: P30419)

Alternative names: Myristoyl-CoA:protein N-myristoyltransferase 1, Peptide N-myristoyltransferase 1, Protein-lysine myristoyltransferase NMT1

All UniProt accessions (11): A0A7I2V3M5, A0A7I2V3U5, A0A7I2V3X4, A0A7I2V4Y5, A0A7I2V539, A0A7I2V5J6, A0A7I2V5M6, B7Z8J4, P30419, K7EN42, K7EN82

UniProt curated annotations — full annotation on UniProt →

Function. Adds a myristoyl group to the N-terminal glycine residue of certain cellular and viral proteins. Also able to mediate N-terminal lysine myristoylation of proteins: catalyzes myristoylation of ARF6 on both ‘Gly-2’ and ‘Lys-3’. Lysine myristoylation is required to maintain ARF6 on membranes during the GTPase cycle.

Subcellular location. Cytoplasm. Cytosol. Membrane.

Tissue specificity. Heart, gut, kidney, liver and placenta.

Similarity. Belongs to the NMT family.

Isoforms (2)

UniProt IDNamesCanonical?
P30419-1Longyes
P30419-2Short

RefSeq proteins (1): NP_066565* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000903NMTFamily
IPR016181Acyl_CoA_acyltransferaseHomologous_superfamily
IPR022676NMT_NDomain
IPR022677NMT_CDomain
IPR022678NMT_CSConserved_site

Pfam: PF01233, PF02799

Enzyme classification (BRENDA):

  • EC 2.3.1.97 — glycylpeptide N-tetradecanoyltransferase (BRENDA: 25 organisms, 184 substrates, 380 inhibitors, 83 Km, 22 kcat entries)

Substrate kinetics (BRENDA)

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

SubstrateKm (mM)Measurements
MYRISTOYL-COA23
CAMP-DEPENDENT PROTEIN KINASE-DERIVED PEPTIDE0.1–0.25
GLY-ASN-ALA-ALA-SER-ALA-ARG-ARG0.0001–0.0065
GLY-ASN-ALA-ALA-ALA-ALA-ARG-ARG0.016–0.64
P60SRC-DERIVED PEPTIDE0.016–0.064
CAP5.5 PEPTIDE0.012–0.252
HIV-1 NEGATIVE REGULATORY FACTOR0.0144–0.02572
HIV1 GAG PROTEIN N-TERMINAL PEPTIDE0.196–0.332
HIV1 NEF PROTEIN N-TERMINAL PEPTIDE0.0015–0.0112
PEPTIDE HS PP60SRC(2-9)0.00282
11-(ETHYLTHIO)-UNDECANOYL-COA0.00071
ARABIDOPSIS THALIANA PROTEIN CDPK6-DERIVED PEPTI0.02051
ARF PEPTIDE0.01751
CAP5.50.0221
GCGGSKVK0.01131

Catalyzed reactions (Rhea), 2 shown:

  • N-terminal glycyl-[protein] + tetradecanoyl-CoA = N-tetradecanoylglycyl-[protein] + CoA + H(+) (RHEA:15521)
  • N-terminal glycyl-L-lysyl-[protein] + tetradecanoyl-CoA = N-terminal glycyl-(N(6)-tetradecanoyl)-L-lysyl-[protein] + CoA + H(+) (RHEA:70671)

UniProt features (65 total): strand 23, helix 15, binding site 11, mutagenesis site 4, turn 4, modified residue 3, chain 1, region of interest 1, splice variant 1, sequence variant 1, compositionally biased region 1

Structure

Experimental structures (PDB)

52 structures, top 30 by resolution.

PDBMethodResolution (Å)
5O6HX-RAY DIFFRACTION1.29
3IU1X-RAY DIFFRACTION1.42
5O6JX-RAY DIFFRACTION1.45
7OWMX-RAY DIFFRACTION1.5
3JTKX-RAY DIFFRACTION1.61
4C2YX-RAY DIFFRACTION1.64
7OWOX-RAY DIFFRACTION1.7
3IU2X-RAY DIFFRACTION1.73
8Q3SX-RAY DIFFRACTION1.78
3IWEX-RAY DIFFRACTION1.79
7OWPX-RAY DIFFRACTION1.81
5O9UX-RAY DIFFRACTION1.85
6SK8X-RAY DIFFRACTION1.87
5MU6X-RAY DIFFRACTION1.88
8Q2ZX-RAY DIFFRACTION1.88
6FZ5X-RAY DIFFRACTION1.89
8Q23X-RAY DIFFRACTION1.9
8Q24X-RAY DIFFRACTION1.9
8Q26X-RAY DIFFRACTION1.9
6SK2X-RAY DIFFRACTION1.9
6F56X-RAY DIFFRACTION1.94
8Q3TX-RAY DIFFRACTION1.96
6SJZX-RAY DIFFRACTION2
6FZ3X-RAY DIFFRACTION2
6FZ2X-RAY DIFFRACTION2.05
7RK3X-RAY DIFFRACTION2.05
4C2ZX-RAY DIFFRACTION2.08
7OWUX-RAY DIFFRACTION2.08
6EHJX-RAY DIFFRACTION2.1
7OWNX-RAY DIFFRACTION2.1

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P30419-F184.050.71

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 (11): 256; 258; 259; 260; 118; 119; 120; 247; 248; 249; 250

Post-translational modifications (3): 31, 47, 83

Mutagenesis-validated functional residues (4):

PositionPhenotype
180abolished glycine- and lysine-myristoyltransferase activities.
181reduced glycine n-myristoyltransferase activity.
192reduced glycine n-myristoyltransferase activity.
492reduced activity.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

IDPathway
R-HSA-162599Late Phase of HIV Life Cycle
R-HSA-203615eNOS activation
R-HSA-2514859Inactivation, recovery and regulation of the phototransduction cascade
R-HSA-75108Activation, myristolyation of BID and translocation to mitochondria
R-HSA-9918432Maturation of DENV proteins

MSigDB gene sets: 266 (showing top): GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, CHIARADONNA_NEOPLASTIC_TRANSFORMATION_KRAS_DN, TSENG_IRS1_TARGETS_UP, MORF_MSH3, SWEET_KRAS_ONCOGENIC_SIGNATURE, GOBP_LIPOPROTEIN_METABOLIC_PROCESS, BECKER_TAMOXIFEN_RESISTANCE_UP, GOBP_CELLULAR_RESPONSE_TO_LIGHT_STIMULUS, MORF_BRCA1, MORF_ATRX, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, TATTATA_MIR374, GOBP_PHOTOTRANSDUCTION, KYNG_DNA_DAMAGE_DN

GO Biological Process (10): in utero embryonic development (GO:0001701), N-terminal peptidyl-glycine N-myristoylation (GO:0018008), regulation of opsin-mediated signaling pathway (GO:0022400), ketone metabolic process (GO:0042180), protein localization to membrane (GO:0072657), positive regulation of protein localization to mitochondrion (GO:1903749), N-terminal protein myristoylation (GO:0006499), cellular response to nutrient levels (GO:0031669), positive regulation of protein localization to lysosome (GO:0150032), positive regulation of TORC1 signaling (GO:1904263)

GO Molecular Function (6): glycylpeptide N-tetradecanoyltransferase activity (GO:0004379), peptidyl-lysine N6-myristoyltransferase activity (GO:0018030), myristoyltransferase activity (GO:0019107), protein binding (GO:0005515), transferase activity (GO:0016740), acyltransferase activity (GO:0016746)

GO Cellular Component (4): cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

CategoryPathways
HIV Life Cycle1
Metabolism of nitric oxide: NOS3 activation and regulation1
The phototransduction cascade1
Intrinsic Pathway for Apoptosis1
Dengue Virus Genome Translation and Replication1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
positive regulation of protein localization2
myristoyltransferase activity2
chordate embryonic development1
N-terminal protein myristoylation1
peptidyl-glycine modification1
regulation of G protein-coupled receptor signaling pathway1
G protein-coupled opsin signaling pathway1
regulation of response to external stimulus1
metabolic process1
intracellular protein localization1
localization within membrane1
protein localization to mitochondrion1
regulation of protein localization to mitochondrion1
N-terminal protein lipidation1
protein myristoylation1
response to nutrient levels1
cellular response to stimulus1
protein localization to lysosome1
regulation of protein localization to lysosome1
positive regulation of TOR signaling1
TORC1 signaling1
regulation of TORC1 signaling1
catalytic activity, acting on a protein1
acyltransferase activity, transferring groups other than amino-acyl groups1
binding1
catalytic activity1
transferase activity1
intracellular anatomical structure1
cytoplasm1
membrane1
cell periphery1

Protein interactions and networks

STRING

1588 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
NMT1SRCP12931619
NMT1GNAO1P09471601
NMT1DBIP07108554
NMT1UGP2Q16851545
NMT1DCAKDQ8WVC6533
NMT1ACBD6Q9BR61502
NMT1ARF1P10947500
NMT1POTEIP0CG38490
NMT1PKNOX1P55347464
NMT1POTEJP0CG39456
NMT1LGI1O95970446
NMT1METAP2P50579435
NMT1GPR132Q9UNW8434
NMT1UNC119Q13432410
NMT1XPO7Q9UIA9406

IntAct

98 interactions, top by confidence:

ABTypeScore
ACBD6NMT2psi-mi:“MI:0914”(association)0.870
NMT1ACBD6psi-mi:“MI:0915”(physical association)0.820
nefACOT8psi-mi:“MI:0914”(association)0.710
LRATD2NMT2psi-mi:“MI:0914”(association)0.640
MGST3GAPDHSpsi-mi:“MI:0914”(association)0.530
NCS1NMT2psi-mi:“MI:0914”(association)0.530
MARCKSL1NMT2psi-mi:“MI:0914”(association)0.530
CIMAP1DNMT2psi-mi:“MI:0914”(association)0.530
TGFB1NMT2psi-mi:“MI:0914”(association)0.530
ANGPTL4NMT2psi-mi:“MI:0914”(association)0.530
MEAK7NMT2psi-mi:“MI:0914”(association)0.530
ANGPTL7TCP1psi-mi:“MI:0914”(association)0.530
FBXO17NMT2psi-mi:“MI:0914”(association)0.530
CASP3NMT1psi-mi:“MI:0570”(protein cleavage)0.440
CASP8NMT1psi-mi:“MI:0570”(protein cleavage)0.440
CAPN2NMT1psi-mi:“MI:0915”(physical association)0.400
TP53NMT1psi-mi:“MI:0915”(physical association)0.400

BioGRID (207): NMT1 (Affinity Capture-RNA), CAPN1 (Affinity Capture-Western), TP53 (Affinity Capture-Western), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), NMT1 (Affinity Capture-MS), ACSL4 (Co-fractionation)

ESM2 similar proteins: A2VE39, A4IFJ5, A4IHT9, A8K855, B1WAZ6, D2HRF1, O00763, O02697, O60551, O70310, O77793, P19447, P30419, P31717, P35574, P47712, P47713, P48736, P49147, P50392, P50393, Q0E908, Q2PQH8, Q2TBU5, Q4R6Y8, Q5R8A5, Q5R981, Q5U2Z5, Q5ZJT0, Q641K1, Q66HX8, Q6DD21, Q7K556, Q7T0T9, Q7XQT2, Q80YD1, Q811C2, Q8C5P5, Q8IYB8, Q8K1Q0

Diamond homologs: A7YT82, O43010, O60551, O61613, O70310, O70311, O74234, P0CP20, P0CP21, P14743, P30418, P30419, P31717, P34763, P34809, P46548, Q4I061, Q4PB56, Q553B6, Q5RAF3, Q6BJF4, Q6C7G2, Q6CMK4, Q75EK2, Q7S3C8, Q8ILW6, Q8K1Q0, Q8TFN1, Q94L32, Q9LTR9, Q9N181, Q9U419, Q9UVX3, Q9EMI7

SIGNOR signaling

2 interactions.

AEffectBMechanism
FYNunknownNMT1phosphorylation
LYNunknownNMT1phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 112 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
SARS-CoV-2 modulates host translation machinery516.7×2e-03
Influenza Infection513.1×3e-03
Signaling by ALK fusions and activated point mutants511.2×3e-03
SARS-CoV-2-host interactions610.7×2e-03
Anchoring of the basal body to the plasma membrane58.4×7e-03
SARS-CoV-2 Infection67.2×5e-03
Signaling by Interleukins65.8×1e-02
Viral Infection Pathways94.1×7e-03

GO biological processes:

GO termPartnersFoldFDR
cytoplasmic translation611.9×6e-03
cilium assembly118.7×5e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance29
Likely benign1
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

4261 predictions. Top by Δscore:

VariantEffectΔscore
17:44960363:CGCAC:Cacceptor_gain1.0000
17:44960364:GCAC:Gacceptor_gain1.0000
17:44960365:CAC:Cacceptor_gain1.0000
17:44960365:CACC:Cacceptor_gain1.0000
17:44960366:AC:Aacceptor_gain1.0000
17:44960367:CC:Cacceptor_gain1.0000
17:44960367:CCTG:Cacceptor_loss1.0000
17:44960368:CTGCG:Cacceptor_loss1.0000
17:44960369:T:Cacceptor_loss1.0000
17:44960374:G:GCacceptor_gain1.0000
17:44960382:C:CTacceptor_gain1.0000
17:44960385:G:Tacceptor_gain1.0000
17:45024722:TCG:Tacceptor_gain1.0000
17:45024723:CG:Cacceptor_gain1.0000
17:45024723:CGC:Cacceptor_gain1.0000
17:45030444:T:Cacceptor_gain1.0000
17:45034185:A:ACdonor_gain1.0000
17:45034185:AC:Adonor_gain1.0000
17:45034185:ACC:Adonor_gain1.0000
17:45034185:ACCC:Adonor_gain1.0000
17:45034186:C:CCdonor_gain1.0000
17:45034186:CC:Cdonor_gain1.0000
17:45034186:CCC:Cdonor_gain1.0000
17:45034186:CCCC:Cdonor_gain1.0000
17:45034186:CCCCG:Cdonor_gain1.0000
17:45034386:CACGA:Cacceptor_gain1.0000
17:45034387:ACGA:Aacceptor_gain1.0000
17:45034388:CGA:Cacceptor_gain1.0000
17:45034388:CGAC:Cacceptor_gain1.0000
17:45034389:GA:Gacceptor_gain1.0000

AlphaMissense

3300 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
17:45086550:G:CA95P1.000
17:45086622:T:CF119L1.000
17:45086622:T:GF119V1.000
17:45086623:T:CF119S1.000
17:45086623:T:GF119C1.000
17:45086624:C:AF119L1.000
17:45086624:C:GF119L1.000
17:45086625:T:AW120R1.000
17:45086625:T:CW120R1.000
17:45086626:G:CW120S1.000
17:45086627:G:CW120C1.000
17:45086627:G:TW120C1.000
17:45086636:G:CQ123H1.000
17:45086636:G:TQ123H1.000
17:45086641:T:AV125D1.000
17:45093765:T:CF156L1.000
17:45093766:T:CF156S1.000
17:45093767:C:AF156L1.000
17:45093767:C:GF156L1.000
17:45093771:T:AW158R1.000
17:45093771:T:CW158R1.000
17:45093772:G:CW158S1.000
17:45093773:G:CW158C1.000
17:45093773:G:TW158C1.000
17:45096204:T:CL172P1.000
17:45096213:T:CL175P1.000
17:45096216:T:AL176Q1.000
17:45096216:T:CL176P1.000
17:45096226:C:AN179K1.000
17:45096226:C:GN179K1.000

dbSNP variants (sampled 300 via entrez): RS1000019596 (17:45083098 C>T), RS1000044869 (17:45090234 T>C), RS1000090905 (17:45085570 A>G), RS1000141883 (17:45066060 A>C,G), RS1000165309 (17:45100084 A>G), RS1000329032 (17:45106401 C>T), RS1000390616 (17:45083214 G>A), RS1000475446 (17:45099740 T>G), RS1000517927 (17:45067281 G>A,C), RS1000524224 (17:45069042 C>A), RS1000544875 (17:45109476 T>C), RS1000722861 (17:45072875 A>T), RS1000823635 (17:45079040 G>T), RS1001017632 (17:45094269 C>T), RS1001044217 (17:45091487 T>C)

Disease associations

OMIM: gene MIM:160993 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

18 associations (top):

StudyTraitp-value
GCST004412_12Craniofacial microsomia9.000000e-06
GCST007267_237Systolic blood pressure1.000000e-14
GCST007269_305Pulse pressure1.000000e-13
GCST008512_36Multisite chronic pain2.000000e-09
GCST008916_39Asthma8.000000e-12
GCST010101_17White matter hyperintensities3.000000e-16
GCST010396_198Gut microbiota (bacterial taxa, hurdle binary method)3.000000e-06
GCST010661_9Blood glucose levels3.000000e-06
GCST010662_15Systolic blood pressure2.000000e-21
GCST010703_91Brain morphology (MOSTest)2.000000e-65
GCST010726_66Periventricular white matter hyperintensities9.000000e-09
GCST011122_24Walking pace3.000000e-09
GCST011947_2White matter hyperintensity volume3.000000e-19
GCST012332_3Multisite chronic pain1.000000e-09
GCST90002400_216Plateletcrit3.000000e-10
GCST90020026_436Hip index1.000000e-11
GCST90020026_437Hip index3.000000e-18
GCST90020028_1372Hip circumference adjusted for BMI3.000000e-11

EFO canonical traits (9, from GWAS)

EFO IDTrait name
EFO:0006335systolic blood pressure
EFO:0005763pulse pressure measurement
EFO:0010100multisite chronic pain
EFO:0005665white matter hyperintensity measurement
EFO:0007874gut microbiome measurement
EFO:0004468glucose measurement
EFO:0004346neuroimaging measurement
EFO:0007985platelet crit
EFO:0008039BMI-adjusted hip circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2096973 (PROTEIN FAMILY), CHEMBL2593 (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: 21 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL3357685ZELENIRSTAT221

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — N-myristoyltransferases

Most potent curated ligand interactions (3 total), top 3:

LigandActionAffinityParameter
zelenirstatInhibition9.0pIC50
MYX1715Inhibition8.82pIC50
NMT inhibitor 1 [WO2024052685A1]Inhibition8.66pIC50

Binding affinities (BindingDB)

207 measured of 233 human assays (233 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2-methyl-1,3,4,5-tetrahydro-2-benzazepin-8-yl)benzenesulfonamideIC502 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC503 nMUS-9156811: N-myristoyl transferase inhibitors
2-chloro-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC503 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamideIC503 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-ethyl-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC503 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-methyl-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC504 nMUS-9156811: N-myristoyl transferase inhibitors
N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2,3,4,5-tetrahydro-1H-2-benzazepin-8-yl)benzenesulfonamideIC504 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-(4-piperidin-4-ylbutyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC504 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-methyl-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC505 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(1-methylpiperidin-4-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC505 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-methyl-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC505 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-[3-(1-methylpiperidin-4-yl)oxypropyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC505 nMUS-9156811: N-myristoyl transferase inhibitors
2-methyl-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC506 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-[4-(1-methylpiperidin-4-yl)butyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC506 nMUS-9156811: N-myristoyl transferase inhibitors
N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-[3-[(2-pyridin-3-ylethylamino)methyl]phenyl]benzenesulfonamideIC506 nMUS-9156811: N-myristoyl transferase inhibitors
4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC507 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC507 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-[3-(4-methyl-1,4-diazepan-1-yl)propyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC507 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC508 nMUS-9156811: N-myristoyl transferase inhibitors
4-[2-(3-methylpiperazin-1-yl)-4-pyridinyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC508 nMUS-9156811: N-myristoyl transferase inhibitors
4-[2-(1,4-diazepan-1-yl)-4-pyridinyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC508 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC508 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-[3-(1,4-diazepan-1-yl)propyl]-N-(difluoromethyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC508 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(1,5-dimethylpyrazol-4-yl)-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamideIC509 nMUS-9156811: N-myristoyl transferase inhibitors
2-fluoro-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC509 nMUS-9156811: N-myristoyl transferase inhibitors
N-methyl-4-[3-[(1-methylpiperidin-4-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC509 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-ethyl-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC509 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC509 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(1,3-dimethylpyrazol-4-yl)-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamideIC5010 nMUS-9156811: N-myristoyl transferase inhibitors
6-(3-piperazin-1-ylpiperidin-1-yl)-N-(1,3,5-trimethylpyrazol-4-yl)pyridine-3-sulfonamideIC5010 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(3-piperidin-4-ylpropyl)benzenesulfonamideIC5010 nMUS-9156811: N-myristoyl transferase inhibitors
4-[4-chloro-3-[(dimethylamino)methyl]phenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5010 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-[3-(1,4-diazepan-1-yl)propyl]-N-methyl-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5011 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(dimethylamino)methyl]-4-fluorophenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5011 nMUS-9156811: N-myristoyl transferase inhibitors
N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(1,2,3,4-tetrahydroisoquinolin-7-yl)benzenesulfonamideIC5011 nMUS-9156811: N-myristoyl transferase inhibitors
N-(difluoromethyl)-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5012 nMUS-9156811: N-myristoyl transferase inhibitors
2,5-difluoro-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5013 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(dimethylamino)methyl]-4-methylphenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5013 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(dimethylamino)methyl]phenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5014 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(dimethylamino)methyl]phenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5015 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-4-(3-piperazin-1-ylphenyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5016 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-[3-(1-methylpiperidin-4-yl)propyl]benzenesulfonamideIC5016 nMUS-9156811: N-myristoyl transferase inhibitors
N-methyl-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5017 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-[(dimethylamino)methyl]phenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-3-(trifluoromethyl)benzenesulfonamideIC5017 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-(1-azabicyclo[2.2.2]octan-3-yloxy)propyl]-2,6-dichloro-N-(difluoromethyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5017 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-methyl-4-[3-(1-methylpiperidin-4-yl)propyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5018 nMUS-9156811: N-myristoyl transferase inhibitors
4-[3-(2-aminopropan-2-yl)phenyl]-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]benzenesulfonamideIC5018 nMUS-9156811: N-myristoyl transferase inhibitors
2,6-dichloro-N-(difluoromethyl)-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5018 nMUS-9156811: N-myristoyl transferase inhibitors
N-(2,2-difluoroethyl)-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamideIC5019 nMUS-9156811: N-myristoyl transferase inhibitors
N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-[3-(methylaminomethyl)phenyl]benzenesulfonamideIC5019 nMUS-9156811: N-myristoyl transferase inhibitors

ChEMBL bioactivities

521 potent at pChembl≥5 of 627 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
9.41IC500.39nMCHEMBL170807
9.40IC500.4nMCHEMBL173370
9.24IC500.58nMCHEMBL171506
9.15IC500.71nMCHEMBL170524
9.05Ki0.9nMCHEMBL3357688
8.89IC501.3nMCHEMBL422896
8.89IC501.3nMCHEMBL355497
8.70IC502nMCHEMBL422746
8.70IC502nMCHEMBL4115136
8.52IC503nMCHEMBL1230468
8.52IC503nMCHEMBL4111551
8.52IC503nMZELENIRSTAT
8.52IC503nMCHEMBL3980411
8.46IC503.5nMCHEMBL355250
8.43IC503.7nMCHEMBL158172
8.43IC503.7nMCHEMBL155301
8.43IC503.7nMCHEMBL347895
8.43IC503.7nMCHEMBL155469
8.43IC503.7nMCHEMBL345893
8.43IC503.7nMCHEMBL347048
8.40IC504nMZELENIRSTAT
8.40IC504nMCHEMBL3357697
8.40IC504nMCHEMBL3357702
8.40IC504nMCHEMBL3358119
8.40IC504nMCHEMBL3920615
8.40IC504nMCHEMBL4110040
8.40IC504nMCHEMBL1230468
8.40Ki4nMCHEMBL1230468
8.32Ki4.8nMCHEMBL3770219
8.30IC505nMCHEMBL3357699
8.30IC505nMCHEMBL3358120
8.30IC505nMCHEMBL3358121
8.30IC505nMCHEMBL3357702
8.30IC505nMCHEMBL4106967
8.30IC505nMCHEMBL3911634
8.28IC505.2nMCHEMBL158172
8.25IC505.6nMCHEMBL347048
8.24IC505.7nMCHEMBL347048
8.22IC506nMCHEMBL4109103
8.22IC506nMCHEMBL3358120
8.22IC506nMCHEMBL4113504
8.21Ki6.2nMCHEMBL3357688
8.15IC507nMCHEMBL4112331
8.15IC507nMCHEMBL1951295
8.15IC507nMCHEMBL3894086
8.12IC507.5nMCHEMBL345893
8.10IC508nMCHEMBL3357695
8.10IC508nMCHEMBL3358122
8.10IC508nMCHEMBL3357704
8.10IC508nMCHEMBL4107350

PubChem BioAssay actives

310 with measured affinity, of 619 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.

CompoundAssayTypeValueUnit
(5-methyl-2-pyridinyl)-[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methanone143932: In vitro inhibitory activity against candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0004uM
(1-methylbenzimidazol-2-yl)-[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0004uM
[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]-(1-prop-2-enylbenzimidazol-2-yl)methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0006uM
(4,5-dimethyl-1,3-thiazol-2-yl)-[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0007uM
2,6-dichloro-4-[2-(4-methylpiperazin-1-yl)-4-pyridinyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1545668: Inhibition of human NMT1 L495M mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0009uM
1-[5-[3,4-difluoro-2-[2-(1,3,5-trimethylpyrazol-4-yl)ethoxy]phenyl]-1-methylindazol-3-yl]-N,N-dimethylmethanamine1582663: Inhibition of human N-myristoyltransferase assessed as reduction in CoASH production by fluorogenic detection based assayic500.0010uM
(1-methylimidazol-2-yl)-[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0013uM
[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]-(1-propan-2-ylbenzimidazol-2-yl)methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0013uM
[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]-(4-methyl-1,3-thiazol-2-yl)methanone143930: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0020uM
2,6-dichloro-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0030uM
[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]-pyridin-2-ylmethanone143923: In vitro inhibitory activity against Candida albicans Nmt (CaNmt) using substrate peptide GLTISKLFR-R-NH2 (0.5 uM) and myristoyl-CoA (0.5 uM)ic500.0035uM
3-[[2-[(2-fluorophenoxy)methyl]-3-methyl-1-benzofuran-4-yl]oxy]-N-(pyridin-3-ylmethyl)propan-1-amine143884: Inhibitory activity against Candida albicans (Nmt) assessed as inhibitory concentrationic500.0037uM
3-[[2-[(4-fluorophenoxy)methyl]-3-methyl-1-benzofuran-4-yl]oxy]-N-(pyridin-3-ylmethyl)propan-1-amine143885: Inhibitory activity against Candida albicans (Nmt) assessed as inhibitory concentration (nM)ic500.0037uM
3-[[2-[(2,3-difluorophenoxy)methyl]-3-methyl-1-benzofuran-4-yl]oxy]-N-(pyridin-3-ylmethyl)propan-1-amine143885: Inhibitory activity against Candida albicans (Nmt) assessed as inhibitory concentration (nM)ic500.0037uM
3-[[2-[(2,4-difluorophenoxy)methyl]-3-methyl-1-benzofuran-4-yl]oxy]-N-(pyridin-3-ylmethyl)propan-1-amine143885: Inhibitory activity against Candida albicans (Nmt) assessed as inhibitory concentration (nM)ic500.0037uM
3-[[3-methyl-2-[(2,3,4-trifluorophenoxy)methyl]-1-benzofuran-4-yl]oxy]-N-(pyridin-3-ylmethyl)propan-1-amine143886: Inhibitory activity against Candida albicans (Nmt) assessed as inhibitory concentration (nM); 3.7-9.4 nMic500.0037uM
4-[[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methoxy]benzonitrile143889: Inhibitory activity against Candida albicans N-Myristoyltransferase (Nmt)ic500.0037uM
2,6-dichloro-4-[4-(1-methylpiperidin-4-yl)butyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0040uM
2,6-dichloro-N-(difluoromethyl)-4-(4-piperidin-4-ylbutyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0040uM
2,6-dichloro-N-methyl-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0040uM
2,6-dichloro-N-[1,5-dimethyl-3-(2-methylpropyl)pyrazol-4-yl]-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0040uM
2-(5-chloro-2-piperidin-4-yloxyphenyl)-5-[(1,3,5-trimethylpyrazol-4-yl)methyl]-1,3,4-oxadiazole1545670: Inhibition of human NMT1 R295Q/W297F/A452M/L453V/L462V/N473H/L495M/Q496L mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0048uM
2,6-dichloro-4-(4-piperidin-4-ylbutyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0050uM
2,6-dichloro-N-(difluoromethyl)-4-[3-(1-methylpiperidin-4-yl)oxypropyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0050uM
2,6-dichloro-N-(difluoromethyl)-4-[4-(1-methylpiperidin-4-yl)butyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0050uM
2,6-dichloro-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide646358: Inhibition of human N-myristoyltransferase 1 using [3H]myristoyl-CoA and GCGGSKVKPQPPQAK(biotin)-amide as substrate preincubated for 5 mins prior substrate addition measured after 50 mins by streptavidin-coated scintillation proximity assayic500.0070uM
2,6-dichloro-N-(difluoromethyl)-4-[6-(dimethylamino)hexyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0080uM
ethyl 6-[[6-(3-aminopropylamino)-3-pyridinyl]methoxy]-4-ethylsulfanylquinoline-3-carboxylate1506565: Inhibition of N-terminal deletion human NMT1 expressed in Escherichia coli BL21 (DE3) using Hs pp60src (2 to 9 residues) as substrate measured every min for 30 mins by CPM-based fluorescence assayki0.0080uM
2,6-dichloro-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0080uM
4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0090uM
2,6-dichloro-N-(difluoromethyl)-4-(3-piperidin-4-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0090uM
2,6-dichloro-N-(1,5-dimethylpyrazol-4-yl)-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0090uM
1-[4-[2,5-difluoro-4-[(2-methyl-3-pyridinyl)methoxy]phenyl]-2-pyridinyl]piperazine1477251: Inhibition of human NMT1 using [3H]-myristoyl-coA/biotinylated CAP5.5 as substrate after 15 mins by scintillation/luminescence counting methodic500.0100uM
2,6-dichloro-N-(difluoromethyl)-4-[3-(1-methylpiperidin-4-yl)propyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0120uM
2,6-dichloro-N-(1,3-dimethylpyrazol-4-yl)-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0120uM
N-[[2-(1-methylazepan-4-yl)-3-pyridinyl]methyl]-2-(5-methylimidazol-1-yl)propanamide1545670: Inhibition of human NMT1 R295Q/W297F/A452M/L453V/L462V/N473H/L495M/Q496L mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0145uM
4-[1-(2-methoxyphenyl)pyrazol-4-yl]-N-[2-(1-methylpyrrolidin-2-yl)ethyl]pyrimidin-2-amine1545670: Inhibition of human NMT1 R295Q/W297F/A452M/L453V/L462V/N473H/L495M/Q496L mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0167uM
2-[[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methoxy]benzonitrile143887: Inhibitory activity against Candida albicans N-Myristoyltransferase (CaNmt) assessed as inhibitory concentration using substrate peptide and myristotyl-CoA at 0.5 uMic500.0170uM
N-methyl-4-[3-[(4-methylpiperazin-1-yl)methyl]phenyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0170uM
2,6-dichloro-4-(3-piperazin-1-ylphenyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0170uM
4-[3-[(8aR)-3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazin-2-yl]propyl]-2,6-dichloro-N-methyl-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1545668: Inhibition of human NMT1 L495M mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0180uM
2,6-dichloro-N-methyl-4-[3-(1-methylpiperidin-4-yl)propyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0180uM
2,6-dichloro-N-methyl-4-(3-piperazin-1-ylpropyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1545668: Inhibition of human NMT1 L495M mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0191uM
(2S)-6-amino-N-(2-cyclohexylethyl)-2-[[(2S)-3-hydroxy-2-[[(2R)-2-[4-[4-(2-methylimidazol-1-yl)butyl]phenyl]propanoyl]amino]propanoyl]amino]hexanamide143938: Inhibition activity against N-myristoyltransferase (NMT) of candida albicans.ic500.0200uM
N-methyl-4-(2-piperazin-1-yl-4-pyridinyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0220uM
2,6-dichloro-4-(3-piperidin-4-ylphenyl)-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0230uM
4-[1-(3-methoxyphenyl)pyrazol-4-yl]-N-[2-(1-methylpyrrolidin-2-yl)ethyl]pyrimidin-2-amine1545670: Inhibition of human NMT1 R295Q/W297F/A452M/L453V/L462V/N473H/L495M/Q496L mutant expressed in Escherichia coli Rosetta-2 cells using GSNKSKPK as substrate in presence of MyrCoA after 30 mins by CPM dye based fluorescence assayki0.0238uM
5-(2-piperidin-4-yloxy-3-pyridinyl)-3-(quinolin-5-ylmethyl)-1,2,4-oxadiazole1270572: Inhibition of human NMT1 by 7-diethylamine-3-(4’maleimidylphenyl)-4-methylcoumarin based fluorescence assayki0.0240uM
2,6-dichloro-N-ethyl-4-[3-(1-methylpiperidin-4-yl)propyl]-N-(1,3,5-trimethylpyrazol-4-yl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0240uM
2,6-dichloro-N-[1,3-dimethyl-5-(2-methylpropyl)pyrazol-4-yl]-4-(2-piperazin-1-yl-4-pyridinyl)benzenesulfonamide1171505: Inhibition of human N-myristoyltransferase 1 assessed as transfer of [3H]-myristic acid to a biotinylated substrate peptide (GCGGSKVKPQPPQAK(biotin)-amide by scintillation proximity assayic500.0250uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Estradioldecreases expression, affects cotreatment3
sodium arseniteaffects binding, decreases reaction, decreases expression, increases activity, increases expression2
aristolochic acid Iincreases expression1
FR900359affects phosphorylation1
bisphenol Fincreases expression1
bufotalinincreases expression1
triphenyl phosphateaffects expression1
bisphenol Aaffects cotreatment, increases expression1
beta-lapachoneincreases expression1
tris(1,3-dichloro-2-propyl)phosphatedecreases expression1
benzo(e)pyrenedecreases methylation, increases methylation1
cadmium acetatedecreases expression1
aflatoxin B2decreases methylation1
di-n-butylphosphoric acidaffects expression1
2,3,5-(triglutathion-S-yl)hydroquinonedecreases ADP-ribosylation1
cylindrospermopsinincreases expression1
CGP 52608affects binding, increases reaction1
desloratadineaffects binding, decreases activity, affects response to substance1
monomethylarsonous acidincreases expression1
K 7174decreases expression1
bisphenol Bincreases expression1
N’-((2-hydroxyphenyl)carbonothioyl)pyridine-2-carbohydrazideaffects binding, decreases activity1
bisphenol Sdecreases methylation1
bisphenol AFincreases expression1
Arsenic Trioxideincreases expression1
Acetaminophendecreases expression1
Benzo(a)pyreneaffects methylation1
Caffeineincreases phosphorylation1
Copperaffects binding, decreases activity1
Coumestrolincreases expression1

ChEMBL screening assays

93 unique, capped per target: 75 binding, 18 admet

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL744115BindingTested for Inhibitory concentration against human N-myristoyltransferase (NMT) in radiochemical HPLC end point assay with peptide GNAASARR-NH2 and [3H]myristoyl-CoA radioligand at 1 uMReplacements for lysine in l-seryl-l-lysyl dipeptide amide inhibitors of candida albicans myristoyl-CoA:protein N-myristoyltransferase — Bioorg Med Chem Lett
CHEMBL4236878ADMETInhibition of human NMT1 using [3H]-myristoyl-coA/biotinylated CAP5.5 as substrate after 15 mins by scintillation proximity assayA Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors. — J Med Chem

Cellosaurus cell lines

8 cell lines: 7 cancer cell line, 1 transformed cell line

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

CellosaurusNameCategorySex
CVCL_D1P8Abcam K-562 NMT1 KOCancer cell lineFemale
CVCL_D2KUAbcam Raji NMT1 KOCancer cell lineMale
CVCL_D9LDUbigene HEK293 NMT1 KOTransformed cell lineFemale
CVCL_TA80HAP1 NMT1 (-) 1Cancer cell lineMale
CVCL_TA81HAP1 NMT1 (-) 2Cancer cell lineMale
CVCL_TA82HAP1 NMT1 (-) 3Cancer cell lineMale
CVCL_TA83HAP1 NMT1 (-) 4Cancer cell lineMale
CVCL_WQ11Abcam Jurkat NMT1 KOCancer cell lineMale

Clinical trials (associated diseases)

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

  • Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): craniofacial microsomia