METTL14
gene geneOn this page
Also known as KIAA1627
Summary
METTL14 (methyltransferase 14, N6-adenosine-methyltransferase non-catalytic subunit, HGNC:29330) is a protein-coding gene on chromosome 4q26, encoding N(6)-adenosine-methyltransferase non-catalytic subunit METTL14 (Q9HCE5). The METTL3-METTL14 heterodimer forms a N6-methyltransferase complex that methylates adenosine residues at the N(6) position of some mRNAs and regulates the circadian clock, differentiation of embryonic stem cells and cortical neurogenesis. It is a selective cancer dependency (DepMap: 78.8% of cell lines).
Enables mRNA binding activity and mRNA m(6)A methyltransferase activity. Involved in mRNA modification; mRNA splicing, via spliceosome; and mRNA stabilization. Located in nucleoplasm. Is active in RNA N6-methyladenosine methyltransferase complex.
Source: NCBI Gene 57721 — RefSeq curated summary.
At a glance
- Clinical variants (ClinVar): 37 total
- Druggable target: yes — 4 molecules with ChEMBL bioactivity
- Cancer dependency (DepMap): dependent in 78.8% of screened cell lines
- MANE Select transcript:
NM_020961
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:29330 |
| Approved symbol | METTL14 |
| Name | methyltransferase 14, N6-adenosine-methyltransferase non-catalytic subunit |
| Location | 4q26 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | KIAA1627 |
| Ensembl gene | ENSG00000145388 |
| Ensembl biotype | protein_coding |
| OMIM | 616504 |
| Entrez | 57721 |
Gene structure
Transcript identifiers
Ensembl transcripts: 11 — 8 protein_coding, 2 nonsense_mediated_decay, 1 retained_intron
ENST00000388822, ENST00000502564, ENST00000506780, ENST00000508801, ENST00000626212, ENST00000628452, ENST00000900246, ENST00000900247, ENST00000900248, ENST00000900250, ENST00000949682
RefSeq mRNA: 1 — MANE Select: NM_020961
NM_020961
CCDS: CCDS34053
Canonical transcript exons
ENST00000388822 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00000935079 | 118691981 | 118692068 |
| ENSE00001016825 | 118705611 | 118705821 |
| ENSE00001016833 | 118703935 | 118704051 |
| ENSE00001161537 | 118691532 | 118691612 |
| ENSE00001226176 | 118709998 | 118715430 |
| ENSE00001504043 | 118689370 | 118689457 |
| ENSE00002045472 | 118685392 | 118685600 |
| ENSE00003579246 | 118687923 | 118688011 |
| ENSE00003637889 | 118694436 | 118694526 |
| ENSE00003658931 | 118700550 | 118700642 |
| ENSE00003659042 | 118697182 | 118697323 |
Expression profiles
Bgee: expression breadth ubiquitous, 253 present calls, max score 95.46.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 23.1406 / max 617.2054, expressed in 1788 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 49425 | 22.7997 | 1788 |
| 49426 | 0.3409 | 126 |
Top tissues by expression
255 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| calcaneal tendon | UBERON:0003701 | 95.46 | gold quality |
| secondary oocyte | CL:0000655 | 93.03 | gold quality |
| cauda epididymis | UBERON:0004360 | 91.23 | gold quality |
| islet of Langerhans | UBERON:0000006 | 91.10 | gold quality |
| caput epididymis | UBERON:0004358 | 90.50 | gold quality |
| corpus epididymis | UBERON:0004359 | 90.42 | gold quality |
| ventricular zone | UBERON:0003053 | 89.54 | gold quality |
| colonic epithelium | UBERON:0000397 | 89.41 | gold quality |
| tendon | UBERON:0000043 | 89.27 | gold quality |
| thymus | UBERON:0002370 | 89.14 | gold quality |
| epithelial cell of pancreas | CL:0000083 | 89.07 | silver quality |
| right testis | UBERON:0004534 | 88.82 | gold quality |
| adrenal tissue | UBERON:0018303 | 88.78 | gold quality |
| left testis | UBERON:0004533 | 88.66 | gold quality |
| smooth muscle tissue | UBERON:0001135 | 88.36 | gold quality |
| bone marrow | UBERON:0002371 | 88.32 | gold quality |
| ganglionic eminence | UBERON:0004023 | 88.24 | gold quality |
| amniotic fluid | UBERON:0000173 | 88.00 | gold quality |
| testis | UBERON:0000473 | 88.00 | gold quality |
| sperm | CL:0000019 | 87.99 | gold quality |
| trabecular bone tissue | UBERON:0002483 | 87.86 | gold quality |
| sural nerve | UBERON:0015488 | 87.73 | gold quality |
| kidney epithelium | UBERON:0004819 | 87.63 | silver quality |
| cortical plate | UBERON:0005343 | 87.26 | gold quality |
| nipple | UBERON:0002030 | 87.15 | gold quality |
| corpus callosum | UBERON:0002336 | 87.00 | gold quality |
| endothelial cell | CL:0000115 | 86.93 | gold quality |
| upper arm skin | UBERON:0004263 | 86.86 | silver quality |
| skeletal muscle tissue of biceps brachii | UBERON:0004502 | 86.86 | gold quality |
| endometrium | UBERON:0001295 | 86.69 | gold quality |
Single-cell (SCXA)
Detected in 1 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 6.70 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): SPI1
miRNA regulators (miRDB)
94 targeting METTL14, 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-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-4682 | 100.00 | 68.89 | 1258 |
| HSA-MIR-4668-3P | 100.00 | 68.74 | 2635 |
| HSA-MIR-450A-1-3P | 100.00 | 69.33 | 1837 |
| HSA-MIR-6867-5P | 100.00 | 82.21 | 3464 |
| HSA-MIR-9-5P | 100.00 | 72.28 | 2361 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-371B-5P | 99.99 | 75.34 | 4759 |
| HSA-MIR-196A-1-3P | 99.99 | 72.15 | 2772 |
| HSA-MIR-548P | 99.98 | 72.25 | 3784 |
| HSA-MIR-5696 | 99.98 | 72.36 | 4487 |
| HSA-MIR-373-5P | 99.98 | 75.36 | 4753 |
| HSA-MIR-616-5P | 99.98 | 75.58 | 4775 |
| HSA-MIR-548AN | 99.97 | 70.91 | 2817 |
| HSA-MIR-1468-3P | 99.96 | 72.74 | 3797 |
| HSA-MIR-3605-5P | 99.96 | 67.12 | 932 |
| HSA-MIR-548AT-5P | 99.96 | 70.83 | 2666 |
| HSA-MIR-545-3P | 99.95 | 70.74 | 2783 |
| HSA-MIR-9718 | 99.94 | 68.91 | 918 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-6835-3P | 99.93 | 70.49 | 2904 |
| HSA-MIR-3919 | 99.87 | 69.45 | 2489 |
| HSA-MIR-548D-3P | 99.87 | 70.67 | 4362 |
| HSA-MIR-5582-3P | 99.86 | 72.48 | 4221 |
| HSA-MIR-579-3P | 99.86 | 71.66 | 3628 |
| HSA-MIR-548BB-3P | 99.86 | 70.58 | 4354 |
| HSA-MIR-664B-3P | 99.84 | 71.65 | 3590 |
| HSA-MIR-548AC | 99.84 | 70.77 | 4351 |
| HSA-MIR-548H-3P | 99.84 | 70.80 | 4349 |
| HSA-MIR-548Z | 99.84 | 70.80 | 4349 |
Functional genomics
DepMap (CRISPR cell-line fitness): dependent in 78.8% of screened cell lines.
Literature-anchored findings (GeneRIF, showing 40)
- methyltransferase-like protein 14 in a complex with METTL3 mediates nuclear RNA methylation (PMID:24316715)
- Structure of the METTL3-METTL14 complex (PMID:27281194)
- The structure reveals the heterodimeric architecture of the complex and donor substrate binding by METTL3. Structure-guided mutagenesis indicates that METTL3 is the catalytic subunit of the complex, whereas METTL14 has a degenerate active site and plays non-catalytic roles in maintaining complex integrity and substrate RNA binding. (PMID:27627798)
- methylation at m6A by METTL3/METTL14 facilitates the methylation of m5C by NSUN2, and vice versa. NSUN2-mediated m5C and METTL3/METTL14-mediated m6A methylation synergistically enhance p21 expression at the translational level (PMID:28247949)
- The critical roles of METTL14 and N(6)-methyladenosine modification in normal and malignant hematopoiesis, are reported. (PMID:29290617)
- METTL3 is soluble and inactive while the catalytic center of METTL14 is degenerated and thus also inactive. In addition, the C-terminal RGG repeats of METTL14 are required for METTL3/14 activity by contributing to RNA substrate binding. (PMID:29348140)
- The Mettl3-Mettl14-mediated m6A was found to promote the development of acute myeloid leukemia and maintain leukemia-initiating cells. (PMID:30006613)
- METTL14 and ALKBH5 determine the N6-methyladenosine of target genes by controlling each other’s expression and by inhibiting YTHDF3.METTL14 role in the cancer growth and progression. (PMID:30306128)
- This demonstrated that EBV hijacks METTL14 to drive EBV-mediated tumorigenesis. METTL14 is now a new target for development of therapeutics for treatment of EBV-associated cancers. (PMID:31226160)
- The N6-methyladenosine mRNA methylase METTL14 promotes renal ischemic reperfusion injury via suppressing YAP1. (PMID:31318098)
- A Mass Spectrometric Assay of METTL3/METTL14 Methyltransferase Activity. (PMID:31585521)
- our results demonstrated the functional importance of METTL14-dependent vascular m6A methylome in vascular functions during calcification and provided a novel mechanistic insight to the therapeutic mechanisms of METTL14 (PMID:31697949)
- This work reveals a novel role of Mettl14 and N(6)-methyladenosine in bladder tumorigenesis and bladder TICs, adding new layers for bladder TIC regulation and N(6)-methyladenosine function. (PMID:31760940)
- Bioinformatics analysis demonstrated that downregulated METTL14 mRNA expression has a significantly negative correlation with the kidney renal clear cell carcinoma (KIRC) stages and a positive correlation with overall survival of KIRC patients. Furthermore, circRNAs may regulate METTL14 mRNA as miRNAs sponge to affect the progression of KIRC. (PMID:31976022)
- Downregulation of METTL14 increases apoptosis and autophagy induced by cisplatin in pancreatic cancer cells. (PMID:32097728)
- METTL14 suppresses proliferation and metastasis of colorectal cancer by down-regulating oncogenic long non-coding RNA XIST. (PMID:32111213)
- METTL14 promotes the migration and invasion of breast cancer cells by modulating N6methyladenosine and hsamiR146a5p expression. (PMID:32323801)
- m6A RNA methylation regulators correlate with malignant progression and have potential predictive values in clear cell renal cell carcinoma. (PMID:32333907)
- METTL14-mediated N6-methyladenosine modification of SOX4 mRNA inhibits tumor metastasis in colorectal cancer. (PMID:32552762)
- LNC942 promoting METTL14-mediated m(6)A methylation in breast cancer cell proliferation and progression. (PMID:32576970)
- The study of METTL14, ALKBH5, and YTHDF2 in peripheral blood mononuclear cells from systemic lupus erythematosus. (PMID:32583611)
- METTL14 regulates M6A methylation-modified primary miR-19a to promote cardiovascular endothelial cell proliferation and invasion. (PMID:32633395)
- Lamin A safeguards the m(6) A methylase METTL14 nuclear speckle reservoir to prevent cellular senescence. (PMID:32813328)
- Upregulation of METTL14 mediates the elevation of PERP mRNA N(6) adenosine methylation promoting the growth and metastasis of pancreatic cancer. (PMID:32843065)
- m(6) A RNA methyltransferases METTL3/14 regulate immune responses to anti-PD-1 therapy. (PMID:32964498)
- Downregulated METTL14 Expression Correlates with Breast Cancer Tumor Grade and Molecular Classification. (PMID:33134390)
- Analysis of METTL3 and METTL14 in hepatocellular carcinoma. (PMID:33159022)
- The m6A methyltransferase METTL14 inhibits the proliferation, migration, and invasion of gastric cancer by regulating the PI3K/AKT/mTOR signaling pathway. (PMID:33314339)
- METTL14-regulated PI3K/Akt signaling pathway via PTEN affects HDAC5-mediated epithelial-mesenchymal transition of renal tubular cells in diabetic kidney disease. (PMID:33414476)
- RNA secondary structure dependence in METTL3-METTL14 mRNA methylation is modulated by the N-terminal domain of METTL3. (PMID:33544495)
- Downregulated METTL14 accumulates BPTF that reinforces super-enhancers and distal lung metastasis via glycolytic reprogramming in renal cell carcinoma. (PMID:33664855)
- CLK1/SRSF5 pathway induces aberrant exon skipping of METTL14 and Cyclin L2 and promotes growth and metastasis of pancreatic cancer. (PMID:33849617)
- USP48 Is Upregulated by Mettl14 to Attenuate Hepatocellular Carcinoma via Regulating SIRT6 Stabilization. (PMID:33903120)
- Methyl CpG binding protein 2 promotes colorectal cancer metastasis by regulating N(6) -methyladenosine methylation through methyltransferase-like 14. (PMID:34097350)
- METTL14 promotes tumorigenesis by regulating lncRNA OIP5-AS1/miR-98/ADAMTS8 signaling in papillary thyroid cancer. (PMID:34131102)
- Isorhapontigenin (ISO) inhibits EMT through FOXO3A/METTL14/VIMENTIN pathway in bladder cancer cells. (PMID:34332039)
- Human umbilical cord mesenchymal stem cells deliver exogenous miR-26a-5p via exosomes to inhibit nucleus pulposus cell pyroptosis through METTL14/NLRP3. (PMID:34412584)
- METTL14 promotes glomerular endothelial cell injury and diabetic nephropathy via m6A modification of alpha-klotho. (PMID:34503454)
- METTL14-Mediated miR-30c-1-3p Maturation Represses the Progression of Lung Cancer via Regulation of MARCKSL1 Expression. (PMID:34586620)
- A methyltransferase-like 14/miR-99a-5p/tribble 2 positive feedback circuit promotes cancer stem cell persistence and radioresistance via histone deacetylase 2-mediated epigenetic modulation in esophageal squamous cell carcinoma. (PMID:34586732)
Cross-species orthologs
4 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | mettl14 | ENSDARG00000070278 |
| mus_musculus | Mettl14 | ENSMUSG00000028114 |
| rattus_norvegicus | Mettl14 | ENSRNOG00000015250 |
| drosophila_melanogaster | Mettl14 | FBGN0032016 |
Protein
Protein identifiers
N(6)-adenosine-methyltransferase non-catalytic subunit METTL14 — Q9HCE5 (reviewed: Q9HCE5)
Alternative names: Methyltransferase-like protein 14
All UniProt accessions (5): A0A0D9SF88, A0A0D9SFW0, D6RBL4, D6RD73, Q9HCE5
UniProt curated annotations — full annotation on UniProt →
Function. The METTL3-METTL14 heterodimer forms a N6-methyltransferase complex that methylates adenosine residues at the N(6) position of some mRNAs and regulates the circadian clock, differentiation of embryonic stem cells and cortical neurogenesis. In the heterodimer formed with METTL3, METTL14 constitutes the RNA-binding scaffold that recognizes the substrate rather than the catalytic core. N6-methyladenosine (m6A), which takes place at the 5’-[AG]GAC-3’ consensus sites of some mRNAs, plays a role in mRNA stability and processing. M6A acts as a key regulator of mRNA stability by promoting mRNA destabilization and degradation. In embryonic stem cells (ESCs), m6A methylation of mRNAs encoding key naive pluripotency-promoting transcripts results in transcript destabilization. M6A regulates spermatogonial differentiation and meiosis and is essential for male fertility and spermatogenesis. M6A also regulates cortical neurogenesis: m6A methylation of transcripts related to transcription factors, neural stem cells, the cell cycle and neuronal differentiation during brain development promotes their destabilization and decay, promoting differentiation of radial glial cells.
Subunit / interactions. Heterodimer; heterodimerizes with METTL3 to form an antiparallel heterodimer that constitutes an active methyltransferase. Component of the WMM complex, a N6-methyltransferase complex composed of a catalytic subcomplex, named MAC, and of an associated subcomplex, named MACOM. The MAC subcomplex is composed of METTL3 and METTL14. The MACOM subcomplex is composed of WTAP, ZC3H13, CBLL1/HAKAI, VIRMA, and, in some cases of RBM15 (RBM15 or RBM15B).
Subcellular location. Nucleus.
Similarity. Belongs to the MT-A70-like family.
RefSeq proteins (1): NP_066012* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR007757 | MT-A70-like | Family |
| IPR029063 | SAM-dependent_MTases_sf | Homologous_superfamily |
| IPR045123 | METTL14-like | Family |
Pfam: PF05063
Enzyme classification (BRENDA):
- EC 2.1.1.348 — mRNA m6A methyltransferase (BRENDA: 11 organisms, 24 substrates, 64 inhibitors, 6 Km, 5 kcat entries)
Substrate kinetics (BRENDA)
3 substrates with measured Km, best-characterized 3. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| ADENINE IN DOUBLE-STRANDED DNA CONTAINING A CYCL | 0.0006–0.0007 | 2 |
| ADENINE IN MRNA | 0.0002–0.023 | 2 |
| ADENINE IN SINGLE-STRANDED DNA | 0.0032–0.0077 | 2 |
UniProt features (60 total): mutagenesis site 13, helix 12, strand 12, region of interest 9, site 5, turn 4, compositionally biased region 3, chain 1, modified residue 1
Structure
Experimental structures (PDB)
76 structures, top 30 by resolution.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5IL2 | X-RAY DIFFRACTION | 1.61 |
| 7RX7 | X-RAY DIFFRACTION | 1.65 |
| 5K7M | X-RAY DIFFRACTION | 1.65 |
| 5K7W | X-RAY DIFFRACTION | 1.65 |
| 5K7U | X-RAY DIFFRACTION | 1.7 |
| 5IL1 | X-RAY DIFFRACTION | 1.71 |
| 9RS1 | X-RAY DIFFRACTION | 1.73 |
| 9Q8G | X-RAY DIFFRACTION | 1.75 |
| 5TEY | X-RAY DIFFRACTION | 1.8 |
| 7O09 | X-RAY DIFFRACTION | 1.8 |
| 7RX6 | X-RAY DIFFRACTION | 1.8 |
| 7NHI | X-RAY DIFFRACTION | 1.85 |
| 7RX8 | X-RAY DIFFRACTION | 1.85 |
| 9G4W | X-RAY DIFFRACTION | 1.85 |
| 9IH5 | X-RAY DIFFRACTION | 1.85 |
| 5L6D | X-RAY DIFFRACTION | 1.85 |
| 7OEL | X-RAY DIFFRACTION | 1.86 |
| 5IL0 | X-RAY DIFFRACTION | 1.88 |
| 6Y4G | X-RAY DIFFRACTION | 1.9 |
| 7O0L | X-RAY DIFFRACTION | 1.9 |
| 7OEK | X-RAY DIFFRACTION | 1.9 |
| 5L6E | X-RAY DIFFRACTION | 1.9 |
| 7NHV | X-RAY DIFFRACTION | 1.91 |
| 9RRY | X-RAY DIFFRACTION | 1.91 |
| 9G4S | X-RAY DIFFRACTION | 1.95 |
| 9Q89 | X-RAY DIFFRACTION | 1.95 |
| 9Q8A | X-RAY DIFFRACTION | 1.95 |
| 6TTP | X-RAY DIFFRACTION | 2 |
| 6TTX | X-RAY DIFFRACTION | 2 |
| 7O08 | X-RAY DIFFRACTION | 2 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q9HCE5-F1 | 79.88 | 0.58 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (5): 146 (interaction with mettl3); 242 (interaction with mettl3); 245 (interaction with mettl3); 298 (interaction with mettl3); 399 (interaction with mettl3)
Post-translational modifications (1): 399
Mutagenesis-validated functional residues (13):
| Position | Phenotype |
|---|---|
| 63–65 | does not affect nuclear localization. |
| 173 | little or no effect on s-adenosyl-l-methionine-binding or methyltransferase activity; when associated with a-192. |
| 192 | little or no effect on methyltransferase activity. little or no effect on s-adenosyl-l-methionine-binding or methyltrans |
| 198 | does not affect methyltransferase activity of the heterodimer complex formed with mettl3. |
| 245 | reduced rna-binding. reduced rna-binding; when associated with e-255. |
| 254–255 | strongly reduced methyltransferase activity of the heterodimer complex formed with mettl3. |
| 255 | reduced rna-binding; when associated with e-245. |
| 297–298 | reduced rna-binding. |
| 298 | strongly decreased methyltransferase activity of the heterodimer complex formed with mettl3, probably due to reduced rna |
| 312 | decreased methyltransferase activity of the heterodimer complex formed with mettl3. |
| 338 | does not affect methyltransferase activity of the heterodimer complex formed with mettl3. |
| 362–363 | little or no effect on methyltransferase activity of the heterodimer complex formed with mettl3. |
| 399 | does not affect interaction with mettl3. |
Function
Pathways and Gene Ontology
Reactome pathways
2 pathways
| ID | Pathway |
|---|---|
| R-HSA-72203 | Processing of Capped Intron-Containing Pre-mRNA |
| R-HSA-8953854 | Metabolism of RNA |
MSigDB gene sets: 154 (showing top):
GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_HEMATOPOIETIC_PROGENITOR_CELL_DIFFERENTIATION, LU_IL4_SIGNALING, GOBP_REGULATION_OF_MRNA_CATABOLIC_PROCESS, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_NEUROGENESIS, GOBP_MALE_GAMETE_GENERATION, GOBP_RNA_METHYLATION, GOBP_FOREBRAIN_DEVELOPMENT, GOBP_MRNA_MODIFICATION, GOBP_FOREBRAIN_GENERATION_OF_NEURONS, GOBP_TRANSLATION, GOBP_POST_TRANSCRIPTIONAL_REGULATION_OF_GENE_EXPRESSION, GOBP_REGULATION_OF_LEUKOCYTE_DIFFERENTIATION, GOBP_REGULATION_OF_HEMOPOIESIS
GO Biological Process (16): mRNA splicing, via spliceosome (GO:0000398), RNA methylation (GO:0001510), mRNA processing (GO:0006397), spermatogenesis (GO:0007283), mRNA modification (GO:0016556), stem cell population maintenance (GO:0019827), forebrain radial glial cell differentiation (GO:0021861), response to nutrient levels (GO:0031667), gliogenesis (GO:0042063), regulation of neuron differentiation (GO:0045664), positive regulation of translation (GO:0045727), mRNA stabilization (GO:0048255), mRNA destabilization (GO:0061157), negative regulation of hematopoietic progenitor cell differentiation (GO:1901533), mRNA export from nucleus (GO:0006406), cell differentiation (GO:0030154)
GO Molecular Function (6): mRNA m(6)A methyltransferase activity (GO:0001734), mRNA binding (GO:0003729), RNA binding (GO:0003723), protein binding (GO:0005515), S-adenosylmethionine-dependent methyltransferase activity (GO:0008757), catalytic activity, acting on a nucleic acid (GO:0140640)
GO Cellular Component (3): nucleus (GO:0005634), nucleoplasm (GO:0005654), RNA N6-methyladenosine methyltransferase complex (GO:0036396)
Reactome top-level categories
Rollup of top-1 pathways:
| Category | Pathways |
|---|---|
| Metabolism of RNA | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| RNA modification | 2 |
| mRNA metabolic process | 2 |
| regulation of mRNA stability | 2 |
| RNA splicing, via transesterification reactions with bulged adenosine as nucleophile | 1 |
| mRNA processing | 1 |
| macromolecule methylation | 1 |
| RNA processing | 1 |
| developmental process involved in reproduction | 1 |
| male gamete generation | 1 |
| multicellular organismal process | 1 |
| maintenance of cell number | 1 |
| forebrain generation of neurons | 1 |
| radial glial cell differentiation | 1 |
| response to stimulus | 1 |
| neurogenesis | 1 |
| neuron differentiation | 1 |
| regulation of cell differentiation | 1 |
| translation | 1 |
| regulation of translation | 1 |
| positive regulation of gene expression | 1 |
| positive regulation of protein metabolic process | 1 |
| RNA stabilization | 1 |
| negative regulation of mRNA catabolic process | 1 |
| negative regulation of gene expression | 1 |
| RNA destabilization | 1 |
| positive regulation of mRNA catabolic process | 1 |
| hematopoietic progenitor cell differentiation | 1 |
| negative regulation of cell differentiation | 1 |
| regulation of hematopoietic progenitor cell differentiation | 1 |
| RNA export from nucleus | 1 |
| gene expression | 1 |
| mRNA transport | 1 |
| cellular developmental process | 1 |
| mRNA methyltransferase activity | 1 |
| RNA binding | 1 |
| nucleic acid binding | 1 |
| binding | 1 |
| methyltransferase activity | 1 |
| catalytic activity | 1 |
| intracellular membrane-bounded organelle | 1 |
Protein interactions and networks
STRING
3086 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| METTL14 | VIRMA | Q69YN4 | 999 |
| METTL14 | WTAP | Q15007 | 999 |
| METTL14 | ZC3H13 | Q5T200 | 998 |
| METTL14 | RBM15 | Q96T37 | 998 |
| METTL14 | RBM15B | Q8NDT2 | 998 |
| METTL14 | CBLL1 | Q75N03 | 997 |
| METTL14 | METTL16 | Q86W50 | 995 |
| METTL14 | METTL3 | Q86U44 | 993 |
| METTL14 | METTL4 | Q8N3J2 | 992 |
| METTL14 | DGCR8 | Q8WYQ5 | 989 |
| METTL14 | SMAD2 | Q15796 | 975 |
| METTL14 | ALKBH5 | Q6P6C2 | 952 |
| METTL14 | YTHDF1 | Q9BYJ9 | 950 |
| METTL14 | YTHDC1 | Q96MU7 | 949 |
| METTL14 | YTHDF2 | Q9Y5A9 | 945 |
IntAct
47 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| METTL14 | METTL3 | psi-mi:“MI:0915”(physical association) | 0.940 |
| METTL14 | METTL3 | psi-mi:“MI:0407”(direct interaction) | 0.940 |
| METTL3 | METTL14 | psi-mi:“MI:0407”(direct interaction) | 0.940 |
| METTL3 | METTL14 | psi-mi:“MI:0914”(association) | 0.940 |
| METTL3 | METTL14 | psi-mi:“MI:0407”(direct interaction) | 0.780 |
| METTL14 | METTL3 | psi-mi:“MI:0915”(physical association) | 0.780 |
| METTL14 | WTAP | psi-mi:“MI:0915”(physical association) | 0.580 |
| METTL14 | WTAP | psi-mi:“MI:0914”(association) | 0.580 |
| WTAP | METTL14 | psi-mi:“MI:0915”(physical association) | 0.580 |
| METTL3 | EIF3H | psi-mi:“MI:0914”(association) | 0.560 |
| METTL3 | WTAP | psi-mi:“MI:0914”(association) | 0.530 |
| METTL14 | WTAP | psi-mi:“MI:0914”(association) | 0.530 |
| METTL14 | psi-mi:“MI:0213”(methylation reaction) | 0.440 |
BioGRID (618): DDI2 (Co-fractionation), METTL3 (Co-fractionation), METTL14 (Affinity Capture-MS), METTL14 (Affinity Capture-MS), METTL14 (Affinity Capture-MS), SMAD2 (Affinity Capture-Western), SMAD3 (Affinity Capture-Western), METTL3 (Affinity Capture-Western), METTL14 (Affinity Capture-Western), METTL14 (Affinity Capture-MS), HSPA8 (Affinity Capture-MS), KRT1 (Affinity Capture-MS), KRT2 (Affinity Capture-MS), HSPA1A (Affinity Capture-MS), KRT10 (Affinity Capture-MS)
ESM2 similar proteins: A2QVS9, A3LS77, A4IFD8, A5E7T4, A8WRG3, A8XYX2, C8V3W5, F4JRS4, F4KAF2, J9VI03, O45380, O60306, O82486, O89042, O94268, P0CO28, P0CO29, P13382, P25583, P32335, P33294, P97496, Q04089, Q2HVD6, Q3UIK4, Q5ADX5, Q5K2C1, Q5K2C4, Q5R5N4, Q5ZK35, Q62847, Q66KJ9, Q6FKD6, Q6FPQ3, Q6FWI7, Q6NU56, Q6NZ22, Q756E1, Q7SB74, Q7YZT6
Diamond homologs: A4IFD8, F1R777, O82486, Q3UIK4, Q5R5N4, Q5ZK35, Q66KJ9, Q6EU10, Q6NU56, Q6NZ22, Q86U44, Q8C3P7, Q94AI4, Q9HCE5, Q9VCE6, Q9VLP7, P41833, Q2HVD6
SIGNOR signaling
0 interactions.
Disease & clinical
Clinical variants and AI predictions
ClinVar
37 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 27 |
| Likely benign | 1 |
| Benign | 0 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
2009 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 4:118685597:GCAG:G | donor_gain | 1.0000 |
| 4:118685600:GGT:G | donor_loss | 1.0000 |
| 4:118685601:G:C | donor_loss | 1.0000 |
| 4:118687921:A:AG | acceptor_gain | 1.0000 |
| 4:118687921:AGTT:A | acceptor_gain | 1.0000 |
| 4:118687921:AGTTG:A | acceptor_gain | 1.0000 |
| 4:118687922:G:GG | acceptor_gain | 1.0000 |
| 4:118687922:GT:G | acceptor_gain | 1.0000 |
| 4:118687922:GTT:G | acceptor_gain | 1.0000 |
| 4:118687922:GTTG:G | acceptor_gain | 1.0000 |
| 4:118687922:GTTGG:G | acceptor_gain | 1.0000 |
| 4:118688009:CAGGT:C | donor_loss | 1.0000 |
| 4:118688010:AGG:A | donor_loss | 1.0000 |
| 4:118688012:G:GC | donor_loss | 1.0000 |
| 4:118688013:T:A | donor_loss | 1.0000 |
| 4:118689361:A:AG | acceptor_gain | 1.0000 |
| 4:118689362:T:G | acceptor_gain | 1.0000 |
| 4:118689364:TTTCA:T | acceptor_loss | 1.0000 |
| 4:118689367:CAG:C | acceptor_loss | 1.0000 |
| 4:118689368:A:AG | acceptor_gain | 1.0000 |
| 4:118689368:AG:A | acceptor_gain | 1.0000 |
| 4:118689368:AGG:A | acceptor_gain | 1.0000 |
| 4:118689369:G:A | acceptor_gain | 1.0000 |
| 4:118689369:G:GT | acceptor_gain | 1.0000 |
| 4:118689369:GGG:G | acceptor_gain | 1.0000 |
| 4:118689369:GGGC:G | acceptor_gain | 1.0000 |
| 4:118689369:GGGCT:G | acceptor_gain | 1.0000 |
| 4:118691520:AT:A | acceptor_gain | 1.0000 |
| 4:118691521:T:G | acceptor_gain | 1.0000 |
| 4:118691521:T:TA | acceptor_gain | 1.0000 |
AlphaMissense
2992 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 4:118691604:T:C | F106L | 1.000 |
| 4:118691605:T:G | F106C | 1.000 |
| 4:118691606:T:A | F106L | 1.000 |
| 4:118691606:T:G | F106L | 1.000 |
| 4:118691608:T:C | L107P | 1.000 |
| 4:118691981:G:A | G109R | 1.000 |
| 4:118691981:G:C | G109R | 1.000 |
| 4:118691982:G:A | G109E | 1.000 |
| 4:118691990:A:C | S112R | 1.000 |
| 4:118691992:C:A | S112R | 1.000 |
| 4:118691992:C:G | S112R | 1.000 |
| 4:118692002:C:G | H116D | 1.000 |
| 4:118692005:A:G | N117D | 1.000 |
| 4:118692007:T:A | N117K | 1.000 |
| 4:118692007:T:G | N117K | 1.000 |
| 4:118692008:G:C | D118H | 1.000 |
| 4:118692008:G:T | D118Y | 1.000 |
| 4:118692009:A:C | D118A | 1.000 |
| 4:118692009:A:G | D118G | 1.000 |
| 4:118692009:A:T | D118V | 1.000 |
| 4:118692010:T:A | D118E | 1.000 |
| 4:118692010:T:G | D118E | 1.000 |
| 4:118692011:T:C | Y119H | 1.000 |
| 4:118692011:T:G | Y119D | 1.000 |
| 4:118692014:T:C | C120R | 1.000 |
| 4:118692015:G:A | C120Y | 1.000 |
| 4:118692016:C:G | C120W | 1.000 |
| 4:118692018:A:C | Q121P | 1.000 |
| 4:118692019:A:C | Q121H | 1.000 |
| 4:118692019:A:T | Q121H | 1.000 |
dbSNP variants (sampled 300 via entrez): RS1000171053 (4:118686395 G>A), RS10002843 (4:118687821 G>A), RS1000351122 (4:118684947 C>T), RS1000354689 (4:118709549 A>G), RS1000385956 (4:118698908 C>G,T), RS1000535510 (4:118691146 G>A), RS1000559837 (4:118687734 C>T), RS1000726918 (4:118704551 T>G), RS1000779691 (4:118704764 A>C), RS1000909806 (4:118687999 G>A), RS1000959954 (4:118711555 C>T), RS10011169 (4:118702971 A>C,G), RS1001255771 (4:118713844 C>G), RS1001480097 (4:118706756 C>T), RS1001529565 (4:118684493 G>A,T)
Disease associations
OMIM: gene MIM:616504 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
0 associations (top):
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL4106140 (PROTEIN COMPLEX)
Molecules with ChEMBL bioactivity
4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 100,849 (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 |
|---|---|---|---|
| CHEMBL461101 | ELTROMBOPAG | 4 | 602 |
| CHEMBL50 | QUERCETIN | 3 | 74,559 |
| CHEMBL1214186 | SINEFUNGIN | 2 | 2,165 |
| CHEMBL151 | LUTEOLIN | 2 | 23,523 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
PharmGKB variants
1 variants.
| Variant | Genes | Level | Score | #Clin annots | Drugs |
|---|---|---|---|---|---|
| rs62328061 | METTL14 | 0.00 | 0 |
Binding affinities (BindingDB)
135 measured of 135 human assays (135 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value | Patent |
|---|---|---|---|
| US20250214997, Compound E-57 | IC50 | 0.1 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 5-[1-[[2-[(4,4-dimethylpiperidin-1-yl)methyl]-1H-indol-6-yl]methyl]triazol-4-yl]-N,N-dimethylpyridin-3-amine | IC50 | 0.12 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| N-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methyl]-1-[2-[[4-[5-(3-fluoropyrrolidin-1-yl)-3-pyridinyl]triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | IC50 | 0.16 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| N-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methyl]-1-[2-[[4-(5-pyrrolidin-1-yl-3-pyridinyl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | IC50 | 0.16 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-140 | IC50 | 0.17 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-87 | IC50 | 0.19 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-121 | IC50 | 0.2 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-84 | IC50 | 0.24 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-111 | IC50 | 0.24 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-51 | IC50 | 0.25 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-101 | IC50 | 0.25 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-50 | IC50 | 0.29 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-105 | IC50 | 0.29 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-119 | IC50 | 0.29 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-2-[(1-methylpiperidin-4-yl)amino]-4-(4-phenylmethoxyanilino)-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 0.3 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| N-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methyl]-1-[2-[[4-(5-pyrrol-1-yl-3-pyridinyl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | IC50 | 0.31 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-56 | IC50 | 0.32 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| N-[[6-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-5-pyrrolidin-1-ylpyridine-3-carboxamide | IC50 | 0.33 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 2-[[4-[5-(2,5-dihydropyrrol-1-yl)-3-pyridinyl]triazol-1-yl]methyl]-6-[(4,4-dimethylpiperidin-1-yl)methyl]imidazo[1,2-a]pyridine | IC50 | 0.36 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-49 | IC50 | 0.37 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 6-(aziridin-1-yl)-4-[1-[[2-[(4,4-dimethylpiperidin-1-yl)methyl]-1H-indol-6-yl]methyl]triazol-4-yl]-1H-indazole | IC50 | 0.4 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 6-[(4,4-dimethylpiperidin-1-yl)methyl]-2-[[4-(5-pyrrolidin-1-yl-3-pyridinyl)triazol-1-yl]methyl]imidazo[1,2-a]pyridine | IC50 | 0.4 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 1-[2-[[4-[5-(3,3-difluoropyrrolidin-1-yl)-3-pyridinyl]triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]-N-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methyl]methanamine | IC50 | 0.41 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-106 | IC50 | 0.48 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 6-[[4-[5-(azetidin-1-yl)-3-pyridinyl]triazol-1-yl]methyl]-2-[(4,4-dimethylpiperidin-1-yl)methyl]-1H-indole | IC50 | 0.5 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-79 | IC50 | 0.54 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-(4-phenoxyanilino)-2-[[1-(2,2,2-trifluoroethyl)piperidin-4-yl]amino]-6H-pyrido[4,3-d]pyrimidin-5-one | IC50 | 0.56 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-59 | IC50 | 0.59 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-(3-methyl-4-phenoxyanilino)-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 0.61 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-[4-(3,5-difluorophenoxy)anilino]-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 0.69 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 1-cyclobutyl-N-[[2-[[4-[5-(2,5-dihydropyrrol-1-yl)-3-pyridinyl]triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | IC50 | 0.74 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-2-[(1-methylpiperidin-4-yl)amino]-4-(4-phenylmethoxyanilino)-6H-pyrido[4,3-d]pyrimidin-5-one | IC50 | 0.75 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-39 | IC50 | 0.75 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-143 | IC50 | 0.77 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-[3-fluoro-4-(3-fluorophenoxy)anilino]-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 0.8 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-chloro-4-(4-cyclohexyloxyanilino)-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one | IC50 | 0.9 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 1-cyclobutyl-N-[[2-[[4-(5-pyrrolidin-1-yl-3-pyridinyl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | IC50 | 1.02 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 5-[1-[[6-[(4,4-dimethylpiperidin-1-yl)methyl]imidazo[1,2-a]pyridin-2-yl]methyl]triazol-4-yl]-N,N-dimethylpyridin-3-amine | IC50 | 1.06 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 5-(dimethylamino)-N-[[2-[(4,4-dimethylpiperidin-1-yl)methyl]-1H-indol-6-yl]methyl]pyridine-3-carboxamide | IC50 | 1.09 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 2-[[(3S)-pyrrolidin-3-yl]amino]-4-[4-(trifluoromethyl)anilino]-6H-pyrido[4,3-d]pyrimidin-5-one | IC50 | 1.17 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-58 | IC50 | 1.18 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-[4-(4-chlorophenoxy)anilino]-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 1.21 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 4-[1-[[2-(6-azaspiro[3.4]octan-6-ylmethyl)-1H-indol-6-yl]methyl]triazol-4-yl]-6-methylsulfanyl-1H-indazole | IC50 | 1.23 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 1-cyclobutyl-N-[[2-[[4-(6-iodo-1H-indazol-4-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | IC50 | 1.24 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-112 | IC50 | 1.25 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 4-[1-[[2-(6-azaspiro[3.4]octan-6-ylmethyl)-1H-indol-6-yl]methyl]triazol-4-yl]-6-bromo-1H-indazole | IC50 | 1.37 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-[4-(4-methylphenoxy)anilino]-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one | IC50 | 1.38 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-60 | IC50 | 1.39 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 8-bromo-4-[4-(3-fluorophenoxy)-3-methylanilino]-2-[(1-methylpiperidin-4-yl)amino]-6H-pyrido[4,3-d]pyrimidin-5-one;hydrochloride | IC50 | 1.4 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| US20250214997, Compound E-43 | IC50 | 1.4 nM | US-20250214997: METTL3 INHIBITOR COMPOUND, AND PHARMACEUTICAL COMPOSITION AND USE THEREOF |
ChEMBL bioactivities
271 potent at pChembl≥5 of 282 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
67 with measured affinity, of 128 total; 46 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 |
|---|---|---|---|---|
| N-[[6-[(cyclohexylmethylamino)methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986901: Binding affinity to full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system assessed as dissociation constant using SAM as substrate by SPR assay | kd | 0.0014 | uM |
| 1-cyclobutyl-N-[[2-[[4-(6-methoxy-1H-indazol-4-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0036 | uM |
| N-[[2-[[4-(6-chloro-1H-indazol-4-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]-1-cyclobutylmethanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0043 | uM |
| (1R,2S,3R,5R)-3-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-5-[2-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]-1H-indol-6-yl]cyclopentane-1,2-diol | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0060 | uM |
| N-[(1-methoxycyclobutyl)methyl]-1-[2-[[4-(6-methoxy-1H-indazol-4-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[6-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| 1-cyclobutyl-N-[[2-[[4-(5-methoxy-1H-indazol-4-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]-1H-indol-6-yl]methyl]-5-oxo-[1,3]thiazolo[3,2-a]pyrimidine-7-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[(cyclobutylmethylamino)methyl]-1H-indol-6-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[(cyclobutylmethylamino)methyl]-5-fluoro-1H-indol-6-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]-1H-indol-6-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[(3,3-diethylazetidin-1-yl)methyl]-1H-indol-6-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[[2-[[1-(3-fluoro-1-bicyclo[1.1.1]pentanyl)ethylamino]methyl]-1H-indol-6-yl]methyl]-4-oxopyrido[1,2-a]pyrimidine-2-carboxamide | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-(1-bicyclo[1.1.1]pentanylmethyl)-1-[2-[[4-(6-methoxyimidazo[1,5-a]pyridin-8-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| 1-cyclobutyl-N-[[2-[[4-(6-methoxyimidazo[1,5-a]pyridin-8-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methyl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| N-[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methyl]-1-[2-[[4-(6-methoxyimidazo[1,5-a]pyridin-8-yl)triazol-1-yl]methyl]imidazo[1,2-a]pyridin-6-yl]methanamine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| (1R,2S,3R,5R)-3-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-5-[2-(6-azaspiro[3.4]octan-6-ylmethyl)-1H-indol-6-yl]cyclopentane-1,2-diol | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| (1R,2S,3R,5R)-3-(4-amino-5-chloropyrrolo[2,3-d]pyrimidin-7-yl)-5-[2-[[(3-fluoro-1-bicyclo[1.1.1]pentanyl)methylamino]methyl]-1H-indol-6-yl]cyclopentane-1,2-diol | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0061 | uM |
| (1R,2S,3R,5R)-3-(4-aminopyrrolo[2,3-d]pyrimidin-7-yl)-5-[2-(6-azaspiro[3.4]octan-6-ylmethyl)-1H-indol-6-yl]cyclopentane-1,2-diol | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0062 | uM |
| 2-[[4-(6-bromo-1H-indazol-4-yl)triazol-1-yl]methyl]-6-[(4,4-dimethylpiperidin-1-yl)methyl]imidazo[1,2-a]pyridine | 1986899: Inhibition of full-length His-tagged METTL3/full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using synthetic RNA 5’P-uacacucgaucuggacuaaagcugcuc-3’ and SAM as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by RF/MS analysis | ic50 | 0.0079 | uM |
| 7-[2-[5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-3-pyridinyl]ethyl]-N-methylquinolin-2-amine | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| 7-[2-[5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-3-pyridinyl]ethyl]-2-ethyl-N-(2-methoxyethyl)-N-methylquinolin-4-amine | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| 7-[2-[5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-3-pyridinyl]ethyl]-2-ethyl-N-(2-methoxyethyl)quinolin-4-amine | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| 7-[[5-[4-amino-5-[(2S)-oxolan-2-yl]pyrrolo[2,3-d]pyrimidin-7-yl]-3-pyridinyl]methoxy]-N-methylquinolin-2-amine | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3R,4S,5R)-5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-2-[[2-(azetidin-1-yl)quinolin-7-yl]oxymethyl]-4-fluorooxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3S,5R)-5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-2-[[2-(azetidin-1-yl)quinolin-7-yl]oxymethyl]oxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3R,4S,5R)-5-(4-amino-5-pyrazol-1-ylpyrrolo[2,3-d]pyrimidin-7-yl)-2-[[2-(azetidin-1-yl)quinolin-7-yl]oxymethyl]-4-fluorooxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3R,4S,5R)-5-[4-amino-5-(4-methyl-1,3-oxazol-2-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-2-[[2-(azetidin-1-yl)quinolin-7-yl]oxymethyl]-4-fluorooxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3R,4S,5R)-5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-2-[[2-(cyclobutylamino)quinolin-7-yl]oxymethyl]-4-fluorooxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3S,5R)-5-(4-amino-5-pyrazol-1-ylpyrrolo[2,3-d]pyrimidin-7-yl)-2-[[2-(azetidin-1-yl)quinolin-7-yl]oxymethyl]oxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2R,3R,4S,5R)-5-[4-amino-5-[(2S)-oxolan-2-yl]pyrrolo[2,3-d]pyrimidin-7-yl]-4-fluoro-2-[[2-(methylamino)quinolin-7-yl]oxymethyl]oxolan-3-ol | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| (2S,3R,4S,5R)-5-[4-amino-5-(1-methylpyrazol-3-yl)pyrrolo[2,3-d]pyrimidin-7-yl]-N-[2-(azetidin-1-yl)quinolin-7-yl]-4-fluoro-3-hydroxyoxolane-2-carboxamide | 1986933: Inhibition of METTL3/METTL14 (unknown origin) using biotinylated RNA (UCUGGACUAAA-biotin) and 3H-SAM as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by scintillation counter analysis | ic50 | 0.0100 | uM |
| N-[[(3R)-1-[6-(benzylamino)pyrimidin-4-yl]-3-hydroxypiperidin-3-yl]methyl]-4-[(4,4-dimethylpiperidin-1-yl)methyl]-2-hydroxybenzamide | 1986898: Inhibition of recombinant METTL3 (354 to 580 residues)/METTL14 (106 to 396 residues) (unknown origin) using m6A oligonucleotide as substrate by HTRF assay | ic50 | 0.2800 | uM |
| (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid | 2119490: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 0.5200 | uM |
| (2S,5S)-2,5-diamino-6-[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]hexanoic acid | 2119490: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 1.3000 | uM |
| Quercetin | 2119492: Inhibition of full length His-tagged METTL3 co-expressed with full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using (5’P-UACACUCGAUCUGGACUAAAGCUGCUC-3’) as substrate pre-treated for 60 mins followed by substrate addition and measured for 1 hr by RapidFire mass spectrometry analysis | ic50 | 2.7000 | uM |
| 2-[2-[5-(4-fluorophenyl)-1-(3-phenylphenyl)indol-3-yl]ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 2.7400 | uM |
| 2-[2-[1-[4-(2,6-dichlorophenyl)phenyl]-5-(4-fluorophenyl)indol-3-yl]ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 2.8100 | uM |
| 2-[2-[5-(4-fluorophenyl)-1-(4-phenylphenyl)indol-3-yl]ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 2.9500 | uM |
| 2-[2-[1-[4-(4-chlorophenyl)phenyl]-5-(4-fluorophenyl)indol-3-yl]ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 3.1300 | uM |
| 3-[3-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]diazenyl]-2-hydroxyphenyl]benzoic acid | 1986923: Inhibition of METTL3/METTL14 (unknown origin) by bioluminescence assay | ic50 | 3.6500 | uM |
| 5,7,17,19-tetraoxa-13-azoniahexacyclo[11.11.0.02,10.04,8.015,23.016,20]tetracosa-1(13),2,4(8),9,14,16(20),21,23-octaene chloride | 2127402: Inhibition of METTL3/METTL14 (unknown origin) by FRET assay | ic50 | 5.4900 | uM |
| 2-[2-[1-benzhydryl-5-(4-fluorophenyl)indol-3-yl]ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 6.0000 | uM |
| 2-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-4-one | 2119492: Inhibition of full length His-tagged METTL3 co-expressed with full length FLAG-tagged METTL14 (unknown origin) expressed in baculovirus expression system using (5’P-UACACUCGAUCUGGACUAAAGCUGCUC-3’) as substrate pre-treated for 60 mins followed by substrate addition and measured for 1 hr by RapidFire mass spectrometry analysis | ic50 | 6.2000 | uM |
| 2-[2-(1-benzhydryl-5-phenylindol-3-yl)ethoxy]benzoic acid | 1986910: Inhibition of METTL3/METTL14 (unknown origin) | ic50 | 8.6300 | uM |
| (2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxy-N-(4-pyrrolidin-1-ylbutyl)oxolane-2-carboxamide | 1986897: Competive inhibition of full length human METTL3/METTL14 expressed in Sf9 cells using single strand RNA 5’-AAGAACCGGACUAAGCU-3’ and SAM as substrate incubated for 40 mins by HTRF assay | ic50 | 8.7000 | uM |
CTD chemical–gene interactions
34 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | affects expression, decreases expression, decreases reaction, increases expression | 5 |
| Valproic Acid | decreases methylation, decreases expression | 2 |
| aristolochic acid I | decreases expression, increases expression | 1 |
| TAK-243 | increases sumoylation | 1 |
| dicrotophos | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| bisphenol A | decreases expression | 1 |
| deoxynivalenol | increases expression | 1 |
| beta-lapachone | decreases expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| 3-deazaadenosine | decreases reaction, increases expression | 1 |
| thallium acetate | decreases reaction, increases expression, affects reaction | 1 |
| cupric oxide | increases expression | 1 |
| cadmium sulfate | increases expression | 1 |
| fumonisin B1 | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| Docetaxel | increases expression, affects binding, increases reaction, increases methylation, increases response to substance (+2 more) | 1 |
| Resveratrol | affects cotreatment, increases expression | 1 |
| Decitabine | decreases reaction, decreases response to substance, increases expression, affects binding, increases reaction | 1 |
| Arsenic Trioxide | affects binding, increases reaction, decreases reaction, increases phosphorylation, increases expression (+2 more) | 1 |
| Acetylcysteine | decreases reaction, increases expression | 1 |
| Arsenic | increases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Doxorubicin | increases expression, increases abundance, increases reaction, increases methylation, increases stability (+1 more) | 1 |
| Ethyl Methanesulfonate | increases expression | 1 |
| Ivermectin | decreases expression | 1 |
| Lipid Peroxides | increases abundance, increases reaction | 1 |
| Lipopolysaccharides | affects reaction, increases expression | 1 |
| Methyl Methanesulfonate | increases expression | 1 |
| Plant Extracts | affects cotreatment, increases expression | 1 |
ChEMBL screening assays
45 unique, capped per target: 45 binding
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL4005637 | Binding | Inhibition of METTL3-14 (unknown origin) at 10 uM using biotin-labeled peptide as substrate and [3H]-SAM measured after 1 hr by scintillation proximity assay | Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase. — J Med Chem |
Cellosaurus cell lines
1 cell lines: 1 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_SX93 | HAP1 METTL14 (-) | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.