PRMT3
gene geneOn this page
Summary
PRMT3 (protein arginine methyltransferase 3, HGNC:30163) is a protein-coding gene on chromosome 11p15.1, encoding Protein arginine N-methyltransferase 3 (O60678). Protein-arginine N-methyltransferase that catalyzes both the monomethylation and asymmetric dimethylation of the guanidino nitrogens of arginine residues in target proteins, and therefore falls into the group of type I methyltransferases.
This gene belongs to the protein arginine methyltransferase (PRMT) family. The encoded enzyme catalyzes the methylation of guanidino nitrogens of arginyl residues of proteins. The enzyme acts on 40S ribosomal protein S2 (rpS2), which is its major in-vivo substrate, and is involved in the proper maturation of the 80S ribosome. Alternative splicing results in multiple transcript variants.
Source: NCBI Gene 10196 — RefSeq curated summary.
At a glance
- GWAS associations: 4
- Clinical variants (ClinVar): 85 total
- Druggable target: yes — 1 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_005788
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:30163 |
| Approved symbol | PRMT3 |
| Name | protein arginine methyltransferase 3 |
| Location | 11p15.1 |
| Locus type | gene with protein product |
| Status | Approved |
| Ensembl gene | ENSG00000185238 |
| Ensembl biotype | protein_coding |
| OMIM | 603190 |
| Entrez | 10196 |
Gene structure
Transcript identifiers
Ensembl transcripts: 13 — 9 protein_coding, 3 nonsense_mediated_decay, 1 retained_intron
ENST00000330796, ENST00000331079, ENST00000437750, ENST00000525188, ENST00000526583, ENST00000529592, ENST00000862431, ENST00000862432, ENST00000862433, ENST00000862434, ENST00000962519, ENST00000962520, ENST00000962521
RefSeq mRNA: 3 — MANE Select: NM_005788
NM_001145166, NM_001145167, NM_005788
CCDS: CCDS44554, CCDS7853
Canonical transcript exons
ENST00000331079 — 16 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001293242 | 20388019 | 20388154 |
| ENSE00002154431 | 20387716 | 20387774 |
| ENSE00002195347 | 20508304 | 20509338 |
| ENSE00003469168 | 20493919 | 20493969 |
| ENSE00003507093 | 20397577 | 20397721 |
| ENSE00003515447 | 20407911 | 20408032 |
| ENSE00003531785 | 20389744 | 20389826 |
| ENSE00003534033 | 20395803 | 20395962 |
| ENSE00003550456 | 20402919 | 20402984 |
| ENSE00003553403 | 20494167 | 20494254 |
| ENSE00003592179 | 20464460 | 20464546 |
| ENSE00003592826 | 20392897 | 20392999 |
| ENSE00003630415 | 20426766 | 20426865 |
| ENSE00003639695 | 20392211 | 20392260 |
| ENSE00003644096 | 20461980 | 20462167 |
| ENSE00003673129 | 20452130 | 20452208 |
Expression profiles
Bgee: expression breadth ubiquitous, 269 present calls, max score 84.63.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 19.2870 / max 238.3430, expressed in 1808 samples.
FANTOM5 promoters (5 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 113426 | 8.3473 | 1633 |
| 113424 | 8.0203 | 1735 |
| 113425 | 2.6012 | 1337 |
| 113427 | 0.2408 | 105 |
| 206225 | 0.0775 | 25 |
Top tissues by expression
291 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| ventricular zone | UBERON:0003053 | 84.63 | gold quality |
| calcaneal tendon | UBERON:0003701 | 84.55 | gold quality |
| primordial germ cell in gonad | CL:0000670 ∩ UBERON:0000991 | 84.39 | gold quality |
| gingival epithelium | UBERON:0001949 | 84.29 | gold quality |
| gastrocnemius | UBERON:0001388 | 83.86 | gold quality |
| left lobe of thyroid gland | UBERON:0001120 | 83.37 | gold quality |
| muscle of leg | UBERON:0001383 | 83.17 | gold quality |
| thyroid gland | UBERON:0002046 | 82.96 | gold quality |
| germinal epithelium of ovary | UBERON:0001304 | 82.91 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 82.76 | gold quality |
| adrenal tissue | UBERON:0018303 | 82.74 | gold quality |
| islet of Langerhans | UBERON:0000006 | 82.16 | gold quality |
| C1 segment of cervical spinal cord | UBERON:0006469 | 81.69 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 81.21 | gold quality |
| left adrenal gland | UBERON:0001234 | 81.19 | gold quality |
| right adrenal gland | UBERON:0001233 | 81.13 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 81.08 | gold quality |
| gingiva | UBERON:0001828 | 81.01 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 80.91 | gold quality |
| hindlimb stylopod muscle | UBERON:0004252 | 80.79 | gold quality |
| stromal cell of endometrium | CL:0002255 | 80.53 | gold quality |
| ganglionic eminence | UBERON:0004023 | 80.50 | gold quality |
| rectum | UBERON:0001052 | 80.21 | gold quality |
| male germ line stem cell (sensu Vertebrata) in testis | CL:0000089 ∩ UBERON:0000473 | 80.19 | gold quality |
| heart left ventricle | UBERON:0002084 | 80.19 | gold quality |
| adrenal gland | UBERON:0002369 | 80.17 | gold quality |
| esophagus mucosa | UBERON:0002469 | 80.14 | gold quality |
| monocyte | CL:0000576 | 80.08 | gold quality |
| right atrium auricular region | UBERON:0006631 | 80.05 | gold quality |
| mononuclear cell | CL:0000842 | 79.96 | gold quality |
Single-cell (SCXA)
Detected in 2 experiment(s), a significant marker in 1.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-ANND-3 | yes | 5.06 |
| E-MTAB-6058 | no | 165.44 |
Regulation
Is transcription factor: no
miRNA regulators (miRDB)
70 targeting PRMT3, 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-5193 | 100.00 | 67.26 | 1744 |
| HSA-MIR-188-3P | 100.00 | 68.76 | 1240 |
| HSA-MIR-6873-3P | 100.00 | 71.42 | 2626 |
| HSA-MIR-5692B | 100.00 | 71.32 | 2622 |
| HSA-MIR-5692C | 100.00 | 71.32 | 2622 |
| HSA-LET-7A-3P | 100.00 | 74.03 | 3932 |
| HSA-LET-7B-3P | 100.00 | 74.08 | 3913 |
| HSA-LET-7F-1-3P | 100.00 | 74.02 | 3928 |
| HSA-MIR-98-3P | 100.00 | 74.08 | 3907 |
| HSA-MIR-7110-3P | 100.00 | 73.18 | 2486 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-3662 | 99.99 | 73.82 | 5684 |
| HSA-MIR-607 | 99.97 | 73.62 | 5593 |
| HSA-MIR-548AJ-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-548X-3P | 99.96 | 73.38 | 5345 |
| HSA-MIR-146A-5P | 99.96 | 68.93 | 988 |
| HSA-MIR-146B-5P | 99.96 | 69.13 | 977 |
| HSA-MIR-4666A-3P | 99.96 | 71.71 | 3434 |
| HSA-MIR-548J-3P | 99.94 | 72.61 | 4881 |
| HSA-MIR-1236-3P | 99.94 | 68.04 | 1695 |
| HSA-MIR-7153-5P | 99.94 | 68.89 | 1006 |
| HSA-MIR-548AE-3P | 99.93 | 72.66 | 4867 |
| HSA-MIR-548AH-3P | 99.93 | 72.54 | 4872 |
| HSA-MIR-548AM-3P | 99.93 | 72.54 | 4872 |
| HSA-MIR-548AQ-3P | 99.93 | 72.66 | 4867 |
| HSA-MIR-218-5P | 99.93 | 72.22 | 2103 |
| HSA-MIR-6508-5P | 99.92 | 70.67 | 2465 |
| HSA-MIR-374A-5P | 99.90 | 71.34 | 2923 |
| HSA-MIR-374B-5P | 99.90 | 69.98 | 2734 |
| HSA-MIR-548D-3P | 99.87 | 70.67 | 4362 |
Literature-anchored findings (GeneRIF, showing 21)
- PRMT3 is a ribosomal protein methyltransferase that affects the cellular level of ribosomal subunits. (PMID:15175657)
- DAL-1/4.1B protein significantly inhibits PRMT3 methylation of cellular substrates, which may affect mechanism through which DAL-1/4.1B affects tumor cell growth. (PMID:15334060)
- Type I Arginine Methyltransferases PRMT1 and PRMT-3 Act Distributively (PMID:19158082)
- results suggest that the pathological mutation in the PABPN1 gene alters the protein conformation and induces a preferential interaction with type I PRMTs and Hsp70 chaperones (PMID:19641605)
- The Tyr87Cys and Tyr87Glu-PRMT3 variants had markedly decreased affinity to ribosomal protein S2 and, consequently, reduced enzymatic activity compared to the wild-type enzyme. (PMID:21059412)
- release of VHL30 from the E3 ligase complex, promotes the binding of VHL30 to a protein arginine methyltransferase, PRMT3 (PMID:21942715)
- The crystal structure of PRMT3 in complex with an inhibitor as well as kinetic analysis reveals an allosteric site of inhibition. (PMID:22795084)
- Mutational defects in PRMT3 is not the cause of frontotemporal lobar degeneration. (PMID:23635657)
- results show that protein arginine methyl transferase (PRMT)-3 and -5 methylate NaV1.5 in vitro, interact with NaV1.5 in human embryonic kidney (HEK) cells, and increase NaV1.5 current density (PMID:23912080)
- This work profilies substrates of protein arginine N-methyltransferase 3 with S-adenosyl-L-methionine analogues. (PMID:24320160)
- PRMT3 translocation by palmitic acid is coupled to the binding of LXRalpha, which is responsible for the onset of fatty liver. (PMID:25187371)
- Findings uncover the existence of an extra-ribosomal complex consisting of PDCD2L, RPS2, and PRMT3 and support a role for PDCD2L in the late maturation of 40S ribosomal subunits. (PMID:27697862)
- ZNF277 and PRMT3 compete for uS5 binding, because overexpression of PRMT3 inhibited the formation of the ZNF277-uS5 complex, whereas depletion of cellular ZNF277 resulted in increased levels of uS5-PRMT3. (PMID:30530495)
- PRMT3 is an essential regulator of mesenchymal stem cell-mediated osteogenesis and bone homeostasis. (PMID:31378783)
- PRMT3 interacts with ALDH1A1 and regulates gene-expression by inhibiting retinoic acid signaling. (PMID:33495566)
- Arginine methyltransferase PRMT3 promote tumorigenesis through regulating c-MYC stabilization in colorectal cancer. (PMID:33991650)
- Decreased nitric oxide content mediated by asymmetrical dimethylarginine and protein l-arginine methyltransferase 3 in macrophages induces trophoblast apoptosis: a potential cause of recurrent miscarriage. (PMID:34647126)
- Protein arginine methyltransferase 3: A crucial regulator in metabolic reprogramming and gene expression in cancers. (PMID:36400311)
- PRMT3 regulates the progression of invasive micropapillary carcinoma of the breast. (PMID:36637351)
- PRMT3-mediated arginine methylation of IGF2BP1 promotes oxaliplatin resistance in liver cancer. (PMID:37024475)
- PRMT3-Mediated Arginine Methylation of METTL14 Promotes Malignant Progression and Treatment Resistance in Endometrial Carcinoma. (PMID:37973560)
Cross-species orthologs
7 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | prmt3 | ENSDARG00000019791 |
| mus_musculus | Prmt3 | ENSMUSG00000030505 |
| rattus_norvegicus | Prmt3 | ENSRNOG00000014829 |
| drosophila_melanogaster | Art9 | FBGN0038188 |
| drosophila_melanogaster | Art6 | FBGN0038189 |
| drosophila_melanogaster | Art3 | FBGN0038306 |
| drosophila_melanogaster | CG32152 | FBGN0052152 |
Paralogs (7): PRMT8 (ENSG00000111218), PRMT1 (ENSG00000126457), PRMT7 (ENSG00000132600), CARM1 (ENSG00000142453), PRMT2 (ENSG00000160310), PRMT9 (ENSG00000164169), PRMT6 (ENSG00000198890)
Protein
Protein identifiers
Protein arginine N-methyltransferase 3 — O60678 (reviewed: O60678)
Alternative names: Heterogeneous nuclear ribonucleoprotein methyltransferase-like protein 3
All UniProt accessions (3): E9PLF6, E9PRB4, O60678
UniProt curated annotations — full annotation on UniProt →
Function. Protein-arginine N-methyltransferase that catalyzes both the monomethylation and asymmetric dimethylation of the guanidino nitrogens of arginine residues in target proteins, and therefore falls into the group of type I methyltransferases. Catalyzes the asymmetric arginine dimethylation at multiple sites in the Arg/Gly-rich region of small ribosomal subunit protein uS5/RPS2. Also appears to methylate other ribosomal proteins. May regulate retinoic acid synthesis and signaling by inhibiting ALDH1A1 retinal dehydrogenase activity. Contributes to methylation of histone H4 ‘Arg-3’, a specific tag for epigenetic transcriptional activation. Mediates asymmetric arginine dimethylation of histone H4 ‘Arg-3’ (H4R3me2a) in the promoter region of miRNA miR-3648, to promote its transcription and osteogenesis.
Subunit / interactions. Monomer and homodimer. Interacts with EPB41L3 (via FERM domain); the interaction is direct and inhibits the protein-arginine N-methyltransferase activity of PRMT3. Interacts with the 40S ribosomal protein RPS2/uS5. Interacts with ALDH1A1; the interaction is direct, inhibits ALDH1A1 aldehyde dehydrogenase activity and is independent of the methyltransferase activity of PRMT3. Interacts (via zinc-finger) with ZNF200 (via C-terminus); the interaction is direct and required to localize PRMT3 to the nucleus and inhibit its proteasomal degradation.
Subcellular location. Cytoplasm. Cytosol. Nucleus.
Activity regulation. Inhibited by N-ethylmaleimide and high concentrations of zinc chloride. Allosterically inhibited by SGC707. Allosterically inhibited by (1-(benzo[d][1,2,3]thiadiazol- 6-yl)-3-(2-cyclohexenylethyl)urea) and derivatives thereof.
Domain organisation. The C2H2-type zinc-finger is responsible for substrate specificity.
Similarity. Belongs to the class I-like SAM-binding methyltransferase superfamily. Protein arginine N-methyltransferase family.
Isoforms (2)
| UniProt ID | Names | Canonical? |
|---|---|---|
| O60678-1 | 1 | yes |
| O60678-2 | 2 |
RefSeq proteins (3): NP_001138638, NP_001138639, NP_005779* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR013087 | Znf_C2H2_type | Domain |
| IPR025799 | Arg_MeTrfase | Family |
| IPR029063 | SAM-dependent_MTases_sf | Homologous_superfamily |
| IPR036236 | Znf_C2H2_sf | Homologous_superfamily |
| IPR049009 | ANM3_Znf-C2H2 | Domain |
| IPR049482 | ANM3-like_C2H2_Zf | Domain |
| IPR055135 | PRMT_dom | Domain |
Pfam: PF06325, PF21137, PF21336, PF22528
Enzyme classification (BRENDA):
- EC 2.1.1.319 — type I protein arginine methyltransferase (BRENDA: 13 organisms, 109 substrates, 121 inhibitors, 26 Km, 24 kcat entries)
Substrate kinetics (BRENDA)
16 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| [HISTONE H2A]-L-ARGININE | 0.0005–0.128 | 3 |
| [HISTONE H3]-L-ARGININE | 0.001–0.0282 | 3 |
| [HISTONE H4]-L-ARGININE | 0.0017–0.0388 | 3 |
| [GRGGFGGRGGFRGGRGG]-L-ARGININE | 0.0003–0.0008 | 2 |
| [HISTONE H4(1-22) PEPTIDE]-L-ARGININE3 | 0.0002–0.0008 | 2 |
| FYSGFNS-DIMETHYL-R8-P-DIMETHYL-R10-GRVYATSWY | 0.0222 | 1 |
| FYSGFNS-DIMETHYL-R8-PRG-DIMETHYL-R12-VYATSWY | 0.0007 | 1 |
| FYSGFNS-DIMETHYL-R8-PRGRVYATSWY | 0.0006 | 1 |
| FYSGFNSRP-DIMETHYL-R10-G-DIMETHYL-R12-VYATSWY | 0.008 | 1 |
| FYSGFNSRP-METHYL-R10-GRVYATSWY | 0.0007 | 1 |
| [HISTONE H4(1-16) PEPTIDE]-L-ARGININE3 | 0.0003 | 1 |
| [PABPN1 MUTANT DELTAC20]-L-ARGININE | 0.0004 | 1 |
| [PABPN1 MUTANT DELTAC27]-L-ARGININE | 0.0001 | 1 |
| [PABPN1 MUTANT DELTAC33]-L-ARGININE | — | 1 |
| [PABPN1 MUTANT DELTAC40]-L-ARGININE | 0.0032 | 1 |
Catalyzed reactions (Rhea), 2 shown:
- L-arginyl-[protein] + 2 S-adenosyl-L-methionine = N(omega),N(omega)-dimethyl-L-arginyl-[protein] + 2 S-adenosyl-L-homocysteine + 2 H(+) (RHEA:48096)
- L-arginyl-[protein] + S-adenosyl-L-methionine = N(omega)-methyl-L-arginyl-[protein] + S-adenosyl-L-homocysteine + H(+) (RHEA:48100)
UniProt features (71 total): strand 16, helix 13, mutagenesis site 9, binding site 6, turn 5, modified residue 4, sequence variant 3, sequence conflict 3, region of interest 3, active site 2, initiator methionine 1, chain 1, site 1, domain 1, splice variant 1, zinc finger region 1, compositionally biased region 1
Structure
Experimental structures (PDB)
10 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 8SHR | X-RAY DIFFRACTION | 1.92 |
| 2FYT | X-RAY DIFFRACTION | 2 |
| 3SMQ | X-RAY DIFFRACTION | 2 |
| 8G2G | X-RAY DIFFRACTION | 2.02 |
| 8G2F | X-RAY DIFFRACTION | 2.06 |
| 4QQN | X-RAY DIFFRACTION | 2.08 |
| 8SHB | X-RAY DIFFRACTION | 2.09 |
| 4RYL | X-RAY DIFFRACTION | 2.1 |
| 8SIO | X-RAY DIFFRACTION | 2.2 |
| 4HSG | X-RAY DIFFRACTION | 2.3 |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-O60678-F1 | 85.63 | 0.69 |
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 (3): 87 (not phosphorylated); 329; 338
Ligand- & substrate-binding residues (6): 239; 263; 285; 313; 314; 343
Post-translational modifications (4): 2, 25, 27, 171
Mutagenesis-validated functional residues (9):
| Position | Phenotype |
|---|---|
| 87 | markedly reduced affinity for rps2. |
| 87 | no effect on interaction with rps2. |
| 338 | loss of catalytic activity. no effect on aldh1a1 activity regulation. |
| 403 | reduces catalytic activity. |
| 464 | loss of interaction with aldh1a1. |
| 465 | loss of interaction with aldh1a1. |
| 466 | loss of interaction with aldh1a1. |
| 468 | loss of interaction with aldh1a1. |
Function
Pathways and Gene Ontology
Reactome pathways
6 pathways
| ID | Pathway |
|---|---|
| R-HSA-3214858 | RMTs methylate histone arginines |
| R-HSA-8876725 | Protein methylation |
| R-HSA-3247509 | Chromatin modifying enzymes |
| R-HSA-392499 | Metabolism of proteins |
| R-HSA-4839726 | Chromatin organization |
| R-HSA-597592 | Post-translational protein modification |
MSigDB gene sets: 317 (showing top):
RNGTGGGC_UNKNOWN, E2F_Q4_01, GOBP_NEGATIVE_REGULATION_OF_LIPID_METABOLIC_PROCESS, GCANCTGNY_MYOD_Q6, AREB6_03, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_NEGATIVE_REGULATION_OF_LIPID_BIOSYNTHETIC_PROCESS, GOBP_OSTEOBLAST_DIFFERENTIATION, MEF2_02, TAL1ALPHAE47_01, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_KETONE_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_BIOSYNTHETIC_PROCESS, GOBP_REGULATION_OF_VITAMIN_METABOLIC_PROCESS, SRF_Q5_01
GO Biological Process (8): chromatin remodeling (GO:0006338), regulation of DNA-templated transcription (GO:0006355), negative regulation of protein ubiquitination (GO:0031397), methylation (GO:0032259), positive regulation of osteoblast differentiation (GO:0045669), transcription initiation-coupled chromatin remodeling (GO:0045815), negative regulation of retinoic acid biosynthetic process (GO:1900053), peptidyl-arginine methylation (GO:0018216)
GO Molecular Function (10): methyltransferase activity (GO:0008168), zinc ion binding (GO:0008270), protein-arginine N-methyltransferase activity (GO:0016274), protein-arginine omega-N monomethyltransferase activity (GO:0035241), protein-arginine omega-N asymmetric methyltransferase activity (GO:0035242), histone methyltransferase activity (GO:0042054), histone H4R3 methyltransferase activity (GO:0044020), protein binding (GO:0005515), transferase activity (GO:0016740), metal ion binding (GO:0046872)
GO Cellular Component (4): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), membrane (GO:0016020)
Reactome top-level categories
Rollup of top-4 pathways:
| Category | Pathways |
|---|---|
| Chromatin modifying enzymes | 1 |
| Post-translational protein modification | 1 |
| Chromatin organization | 1 |
| Metabolism of proteins | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| protein-arginine N-methyltransferase activity | 3 |
| cellular anatomical structure | 3 |
| protein methyltransferase activity | 2 |
| chromatin organization | 1 |
| DNA-templated transcription | 1 |
| regulation of gene expression | 1 |
| regulation of RNA biosynthetic process | 1 |
| protein ubiquitination | 1 |
| regulation of protein ubiquitination | 1 |
| negative regulation of protein modification by small protein conjugation or removal | 1 |
| metabolic process | 1 |
| osteoblast differentiation | 1 |
| positive regulation of cell differentiation | 1 |
| regulation of osteoblast differentiation | 1 |
| transcription initiation at RNA polymerase II promoter | 1 |
| positive regulation of gene expression, epigenetic | 1 |
| retinoic acid biosynthetic process | 1 |
| negative regulation of hormone metabolic process | 1 |
| negative regulation of isoprenoid metabolic process | 1 |
| negative regulation of vitamin metabolic process | 1 |
| negative regulation of lipid biosynthetic process | 1 |
| regulation of retinoic acid biosynthetic process | 1 |
| protein methylation | 1 |
| peptidyl-arginine modification | 1 |
| transferase activity, transferring one-carbon groups | 1 |
| transition metal ion binding | 1 |
| arginine N-methyltransferase activity | 1 |
| histone modifying activity | 1 |
| histone H4 methyltransferase activity | 1 |
| binding | 1 |
| catalytic activity | 1 |
| cation binding | 1 |
| intracellular membrane-bounded organelle | 1 |
| intracellular anatomical structure | 1 |
| cytoplasm | 1 |
Protein interactions and networks
STRING
2474 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PRMT3 | EPB41L3 | Q9Y2J2 | 914 |
| PRMT3 | PRMT5 | O14744 | 892 |
| PRMT3 | RPS2 | P15880 | 843 |
| PRMT3 | PRMT1 | Q99873 | 838 |
| PRMT3 | CARM1 | Q86X55 | 790 |
| PRMT3 | SETD7 | Q8WTS6 | 708 |
| PRMT3 | SUV39H2 | Q9H5I1 | 637 |
| PRMT3 | HNRNPA1 | P09651 | 624 |
| PRMT3 | EZH2 | Q15910 | 615 |
| PRMT3 | HNRNPDL | O14979 | 608 |
| PRMT3 | PDCD2L | Q9BRP1 | 591 |
| PRMT3 | KMT5A | Q9NQR1 | 585 |
| PRMT3 | SMYD3 | Q9H7B4 | 581 |
| PRMT3 | WDR77 | Q9BQA1 | 576 |
| PRMT3 | KDM1A | O60341 | 562 |
IntAct
75 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| PRMT3 | RPS2 | psi-mi:“MI:0915”(physical association) | 0.810 |
| RPS2 | PRMT3 | psi-mi:“MI:0915”(physical association) | 0.810 |
| PRMT3 | RPS2 | psi-mi:“MI:0914”(association) | 0.810 |
| DYNLL2 | BLTP3B | psi-mi:“MI:0914”(association) | 0.640 |
| PRMT3 | PIH1D2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PRMT3 | BEND7 | psi-mi:“MI:0915”(physical association) | 0.560 |
| PRMT3 | MEOX2 | psi-mi:“MI:0915”(physical association) | 0.560 |
| FKBP6 | EEF2K | psi-mi:“MI:0914”(association) | 0.530 |
| RPS2 | MPHOSPH10 | psi-mi:“MI:0914”(association) | 0.530 |
| TSKS | RGPD8 | psi-mi:“MI:0914”(association) | 0.530 |
| PDCD2L | PRMT3 | psi-mi:“MI:0914”(association) | 0.530 |
| DDX21 | MED19 | psi-mi:“MI:2364”(proximity) | 0.480 |
| SCN5A | PRMT3 | psi-mi:“MI:2364”(proximity) | 0.470 |
| SCN5A | PRMT3 | psi-mi:“MI:0915”(physical association) | 0.470 |
| SH2D1B | PRMT3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| HNRNPK | PRMT3 | psi-mi:“MI:0915”(physical association) | 0.400 |
| PPARD | PRMT3 | psi-mi:“MI:0915”(physical association) | 0.370 |
| PRMT3 | RASSF2 | psi-mi:“MI:0915”(physical association) | 0.370 |
| Ranbp2 | POM121C | psi-mi:“MI:0914”(association) | 0.350 |
| HNRNPD | ARHGAP32 | psi-mi:“MI:0914”(association) | 0.350 |
| JUN | TPM3 | psi-mi:“MI:0914”(association) | 0.350 |
| Xpo1 | IFT56 | psi-mi:“MI:0914”(association) | 0.350 |
| HSCB | RBP5 | psi-mi:“MI:0914”(association) | 0.350 |
| ORF2 | PRMT3 | psi-mi:“MI:0914”(association) | 0.350 |
| PARP8 | PRMT3 | psi-mi:“MI:0914”(association) | 0.350 |
| PRMT3 | CSTA | psi-mi:“MI:0914”(association) | 0.350 |
| M | psi-mi:“MI:0914”(association) | 0.350 |
BioGRID (248): RPS2 (Biochemical Activity), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Proximity Label-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS), PRMT3 (Two-hybrid), PRMT3 (Affinity Capture-MS), PRMT3 (Affinity Capture-MS)
ESM2 similar proteins: A0JMU5, A1A4L5, A2AV36, A2Y8B9, B0X4N1, B3DLB3, B3M1E1, B3MF31, B3P4N5, B4GZ20, B4HJC0, B4I8G2, B4JXV2, B4KA23, B4LVS8, B4NKI9, B4P925, B4PVH6, B4QI55, B4QVW6, B6DMK2, D9IVE5, O14727, O60678, O70467, O88879, Q0V9P1, Q16NS8, Q29B63, Q3EBC8, Q3U213, Q3U3W5, Q4SBY6, Q5RAY7, Q5ZIB9, Q6P2P2, Q6P5U7, Q6PCI6, Q7QIL2, Q80VJ4
Diamond homologs: A0A3Q0KHE7, A0A411EW25, A0JMU5, A2AV36, A2Y953, A2YPT7, A2Z0C0, A3KPF2, A6QQV6, A8IEF3, B0JYW5, B0W3L6, B3DLB3, B3M1E1, B3P4N5, B4GZ20, B4HJC0, B4JXV2, B4KA23, B4LVS8, B4MNL1, B4NKI9, B4PVH6, B4QVW6, D9IVE5, O13648, O60678, O70467, O82210, P38074, P55345, Q08A71, Q0J2C6, Q174R2, Q28F07, Q29B63, Q3U3W5, Q4AE70, Q54EF2, Q54HI0
SIGNOR signaling
1 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PRMT3 | “down-regulates activity” | ALDH1A1 | binding |
Disease & clinical
Clinical variants and AI predictions
ClinVar
85 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 63 |
| Likely benign | 1 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
3604 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 11:20388153:AG:A | donor_loss | 1.0000 |
| 11:20388154:GG:G | donor_loss | 1.0000 |
| 11:20388156:T:A | donor_loss | 1.0000 |
| 11:20395798:TTTA:T | acceptor_loss | 1.0000 |
| 11:20395799:TTA:T | acceptor_loss | 1.0000 |
| 11:20395800:TA:T | acceptor_loss | 1.0000 |
| 11:20395801:A:AG | acceptor_gain | 1.0000 |
| 11:20395802:G:A | acceptor_loss | 1.0000 |
| 11:20395802:G:GA | acceptor_gain | 1.0000 |
| 11:20395802:GAT:G | acceptor_gain | 1.0000 |
| 11:20395937:GCAC:G | donor_gain | 1.0000 |
| 11:20395960:G:GT | donor_gain | 1.0000 |
| 11:20395960:GAA:G | donor_gain | 1.0000 |
| 11:20395963:G:GG | donor_gain | 1.0000 |
| 11:20402914:CCTAG:C | acceptor_loss | 1.0000 |
| 11:20402915:CTAGG:C | acceptor_loss | 1.0000 |
| 11:20402916:TAG:T | acceptor_loss | 1.0000 |
| 11:20402918:G:A | acceptor_loss | 1.0000 |
| 11:20402982:AAGG:A | donor_loss | 1.0000 |
| 11:20402984:GGT:G | donor_loss | 1.0000 |
| 11:20402985:G:GC | donor_loss | 1.0000 |
| 11:20402986:T:A | donor_loss | 1.0000 |
| 11:20407900:A:AG | acceptor_gain | 1.0000 |
| 11:20407901:A:G | acceptor_gain | 1.0000 |
| 11:20407904:A:AG | acceptor_gain | 1.0000 |
| 11:20407910:GGTA:G | acceptor_gain | 1.0000 |
| 11:20408028:ATAAG:A | donor_loss | 1.0000 |
| 11:20408029:TAAG:T | donor_loss | 1.0000 |
| 11:20408030:AAG:A | donor_loss | 1.0000 |
| 11:20408033:GT:G | donor_loss | 1.0000 |
AlphaMissense
3522 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 11:20402944:G:C | R244P | 1.000 |
| 11:20397714:T:C | M233T | 0.999 |
| 11:20402919:G:C | D236H | 0.999 |
| 11:20407915:T:A | V259D | 0.999 |
| 11:20426858:A:T | E329V | 0.999 |
| 11:20426860:T:A | W330R | 0.999 |
| 11:20426860:T:C | W330R | 0.999 |
| 11:20452130:G:C | G332R | 0.999 |
| 11:20452145:T:C | F337L | 0.999 |
| 11:20452147:T:A | F337L | 0.999 |
| 11:20452147:T:G | F337L | 0.999 |
| 11:20452149:A:T | E338V | 0.999 |
| 11:20493934:T:C | F455L | 0.999 |
| 11:20493936:T:A | F455L | 0.999 |
| 11:20493936:T:G | F455L | 0.999 |
| 11:20494206:T:A | W480R | 0.999 |
| 11:20494206:T:C | W480R | 0.999 |
| 11:20494208:G:C | W480C | 0.999 |
| 11:20494208:G:T | W480C | 0.999 |
| 11:20392942:T:A | W115R | 0.998 |
| 11:20392942:T:C | W115R | 0.998 |
| 11:20397714:T:G | M233R | 0.998 |
| 11:20397715:G:A | M233I | 0.998 |
| 11:20397715:G:C | M233I | 0.998 |
| 11:20397715:G:T | M233I | 0.998 |
| 11:20402920:A:C | D236A | 0.998 |
| 11:20402920:A:T | D236V | 0.998 |
| 11:20407939:G:A | G267E | 0.998 |
| 11:20407957:C:A | A273D | 0.998 |
| 11:20407990:T:A | V284D | 0.998 |
dbSNP variants (sampled 300 via entrez): RS1000120912 (11:20440533 T>G), RS1000124689 (11:20456608 T>C), RS1000200330 (11:20397043 C>G), RS1000230690 (11:20493896 A>C,G), RS1000232884 (11:20407489 T>G), RS1000265163 (11:20479328 T>A), RS1000283276 (11:20493583 A>G,T), RS1000283931 (11:20450279 T>G), RS1000347358 (11:20395443 A>C), RS1000378301 (11:20480876 G>C), RS1000413527 (11:20414018 A>G), RS1000426964 (11:20443761 G>A), RS1000430153 (11:20499827 C>T), RS1000435857 (11:20443467 C>A,G), RS1000463858 (11:20487392 C>T)
Disease associations
OMIM: gene MIM:603190 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
4 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002754_2 | Response to inhaled glucocorticoid treatment in asthma (change in FEV1) | 6.000000e-11 |
| GCST005024_106 | Pursuit maintenance gain | 8.000000e-06 |
| GCST008447_2 | Number of alcoholic drinks required to feel an effect (long-term average) | 6.000000e-10 |
| GCST009738_2 | Carotid intima media thickness (maximum) | 3.000000e-08 |
EFO canonical traits (2, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0005921 | FEV change measurement |
| EFO:0008433 | pursuit maintenance gain measurement |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL5891 (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: 1,522 (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 |
|---|---|---|---|
| CHEMBL1088977 | ADEMETIONINE | 3 | 1,522 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — 2.1.1.- Protein arginine N-methyltransferases
Most potent curated ligand interactions (3 total), top 3:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| SGC707 | Negative | 7.28 | pKd |
| MS023 | Inhibition | 7.26 | pKi |
| compound 1 [PMID: 22795084] | Inhibition | 5.6 | pIC50 |
Binding affinities (BindingDB)
2 measured of 5 human assays (5 total across all organisms); most potent 2 below. Values come from heterogeneous assays and are not directly comparable.
| Ligand | Measure | Value |
|---|---|---|
| MS023 (Compound 3) | KI | 23 nM |
| N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-pyrrol-3-yl)methyl)ethane-1,2-diamine (Compound 2) | KI | 120 nM |
ChEMBL bioactivities
125 potent at pChembl≥5 of 146 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
PubChem BioAssay actives
121 with measured affinity, of 370 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| N’-[[5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine | 2069866: Inhibition of N-terminal GST-tagged human PRMT3 (2 to end residues) expressed in Escherichia coli using SAM and Histone (1 to 21 residues) as substrate preincubated for 60 mins followed by substrate addition and measured after 40 mins by Topcount reader based analysis | ic50 | 0.0017 | uM |
| N’-methyl-N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine | 1319863: Inhibition of human PRMT3 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation proximity assay | ic50 | 0.0040 | uM |
| 1-(3-fluoroisoquinolin-6-yl)-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0100 | uM |
| 1-[2-(azepan-1-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0170 | uM |
| 1-(8-chloroisoquinolin-6-yl)-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0190 | uM |
| 1-(7-fluoroisoquinolin-6-yl)-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0190 | uM |
| 1-isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0190 | uM |
| 1-[2-(8-azabicyclo[3.2.1]octan-8-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0220 | uM |
| 1-[2-(2,5-dimethylpyrrolidin-1-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0220 | uM |
| N’-[[2-(2-chlorophenyl)sulfanylphenyl]methyl]-N’-methylethane-1,2-diamine | 1471457: Inhibition of PRMT3 (unknown origin) incubated for 15 mins followed by substrate addition measured after 60 mins by AlphaLisa method | ic50 | 0.0220 | uM |
| 1-isoquinolin-6-yl-3-[2-oxo-2-(3,3,4,4-tetrafluoropyrrolidin-1-yl)ethyl]urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0240 | uM |
| 1-[2-(4,4-difluoropiperidin-1-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0350 | uM |
| 1-(7-methylisoquinolin-6-yl)-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0360 | uM |
| 1-[2-(7-azabicyclo[2.2.1]heptan-7-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0460 | uM |
| 1-[2-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0550 | uM |
| 1-[2-(azetidin-1-yl)-2-oxoethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0610 | uM |
| 1-isoquinolin-6-yl-3-(2-oxo-2-piperidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0840 | uM |
| N-cyclopentyl-2-(isoquinolin-6-ylcarbamoylamino)-N-methylacetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.0870 | uM |
| (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid | 1689512: Inhibition of recombinant human PRMT8 using histone H4 as substrate by hotspot assay | ic50 | 0.1100 | uM |
| N,N-diethyl-2-(isoquinolin-6-ylcarbamoylamino)acetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1140 | uM |
| N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine | 2138374: Inhibition of PRMT3 (unknown origin) | ic50 | 0.1190 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-(2-oxo-2-piperidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1340 | uM |
| 2-(isoquinolin-6-ylcarbamoylamino)-N,N-dimethylacetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1500 | uM |
| N-cyclopropyl-2-(isoquinolin-6-ylcarbamoylamino)acetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1580 | uM |
| methyl (2S)-1-[2-(isoquinolin-6-ylcarbamoylamino)acetyl]pyrrolidine-2-carboxylate | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1660 | uM |
| 1-(1-methylisoquinolin-6-yl)-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.1940 | uM |
| 1-[2-[1-(aminomethyl)cyclohexyl]ethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.2910 | uM |
| N-cyclopentyl-2-(isoquinolin-6-ylcarbamoylamino)acetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.2920 | uM |
| 1-(2-cyclopentylethyl)-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.2950 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-[(4-nitrophenyl)methyl]urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.3000 | uM |
| 2-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-1-phenylguanidine | 2127550: Inhibition of human PRMT3 using Histone H3 as substrate and SAM as cofactor by radiometric HotSpot assay | ic50 | 0.3210 | uM |
| 2-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-1-(2-bromophenyl)guanidine | 2127582: Inhibition of PRMT3 (unknown origin) | ic50 | 0.3210 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-[2-(4-fluorophenyl)-2-oxoethyl]urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.3600 | uM |
| 1-[2-(cyclohexen-1-yl)ethyl]-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.4210 | uM |
| 2-(isoquinolin-6-ylcarbamoylamino)-N-methoxy-N-methylacetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.4760 | uM |
| N-cyclohexyl-2-(isoquinolin-6-ylcarbamoylamino)acetamide | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.4770 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-phenacylurea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.4800 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-(2-cyclohexyl-2-hydroxyethyl)urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.4900 | uM |
| N’-[[2-[4,4-bis(methoxymethyl)cyclohexyl]oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride | 2069842: Inhibition of PRMT3 (unknown origin) by AlphaLISA assay | ic50 | 0.4930 | uM |
| 1-(2-cyclohexylethyl)-3-isoquinolin-6-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.5400 | uM |
| N’-methyl-N’-[[4-[3-(trifluoromethyl)phenyl]-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine | 1801573: PRMT Biochemical Assays from Article 10.1021/acschembio.5b00839: “A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.” | ki | 0.5500 | uM |
| 1-(1-oxo-3H-2-benzofuran-5-yl)-3-(2-oxo-2-piperidin-1-ylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.7570 | uM |
| 1-isoquinolin-6-yl-3-(2-phenylethyl)urea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.8330 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-(2-cyclohexyl-2-oxoethyl)urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.8400 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-[(4-methylsulfonylphenyl)methyl]urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 0.8500 | uM |
| (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-amino-5-cyanopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid | 1636911: Inhibition of PRMT3 (unknown origin) | ic50 | 0.8700 | uM |
| (2S)-1-[[2-[[3-chloro-4-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl-methylamino]-3-(methylamino)propan-2-ol | 2104090: Inhibition of PRMT3 (unknown origin) | ic50 | 0.9420 | uM |
| 1-(2-oxo-2-piperidin-1-ylethyl)-3-quinazolin-7-ylurea | 1472768: Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | ic50 | 0.9670 | uM |
| 1-(1,2,3-benzothiadiazol-6-yl)-3-(2-cyclohexylethyl)urea | 729422: Inhibition of PRMT3 (unknown origin) using histone H4 (1 to 24) as substrate after 1 hr by scintillation proximity assay in presence of [3H]-S-adenosylmethionine | ic50 | 1.0000 | uM |
| (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid | 738921: Inhibition of PRMT3 (unknown origin) using [3H]SAM assessed as inhibition of biotinylated-H4 (1 to 24 amino acid residues) methylation after 1 hr by scintillation proximity assay | ki | 1.1500 | uM |
CTD chemical–gene interactions
47 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| sodium arsenite | decreases expression, affects cotreatment, increases abundance, increases expression | 3 |
| Air Pollutants | decreases expression, increases abundance, increases expression | 2 |
| Arsenic | increases abundance, increases expression, decreases expression, affects cotreatment | 2 |
| Dexamethasone | decreases expression, affects cotreatment | 2 |
| Particulate Matter | increases abundance, increases expression, decreases expression | 2 |
| aristolochic acid I | decreases expression | 1 |
| SGC707 | affects folding, affects binding, decreases activity | 1 |
| FR900359 | affects phosphorylation | 1 |
| bisphenol F | affects cotreatment, decreases expression | 1 |
| dicrotophos | decreases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| trichostatin A | affects expression | 1 |
| arsenite | affects binding, increases reaction | 1 |
| cobaltous chloride | decreases expression | 1 |
| manganese chloride | affects cotreatment, increases abundance, increases expression | 1 |
| potassium chromate(VI) | affects cotreatment, decreases expression | 1 |
| 1-nitropyrene | increases expression | 1 |
| epigallocatechin gallate | affects cotreatment, decreases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| Resveratrol | affects cotreatment, increases expression | 1 |
| Sunitinib | increases expression | 1 |
| Benzo(a)pyrene | increases methylation | 1 |
| Dichlorodiphenyl Dichloroethylene | increases expression | 1 |
| Doxorubicin | decreases expression | 1 |
| Enzyme Inhibitors | increases O-linked glycosylation, decreases activity | 1 |
| Estradiol | increases expression | 1 |
| Ethyl Methanesulfonate | decreases expression | 1 |
| Formaldehyde | decreases expression | 1 |
| Indomethacin | affects cotreatment, decreases expression | 1 |
| Ivermectin | decreases expression | 1 |
ChEMBL screening assays
148 unique, capped per target: 145 binding, 3 functional
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1037276 | Binding | Inhibition of PRMT3 | Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)–Hit to Lead studies. — Bioorg Med Chem Lett |
| CHEMBL5444955 | Functional | Affinity Phenotypic Cellular interaction: (Western Blot (inhibitor of H4R3 methylation in MCF-7 cells)) EUB0000261b PRMT3 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
Cellosaurus cell lines
3 cell lines: 3 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_KW00 | InCELL Hunter A549 PRMT3 Methyltransferase | Cancer cell line | Male |
| CVCL_TH12 | HAP1 PRMT3 (-) 1 | Cancer cell line | Male |
| CVCL_TH13 | HAP1 PRMT3 (-) 2 | 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.