PRMT1

Summary

PRMT1 (protein arginine methyltransferase 1, HGNC:5187) is a protein-coding gene on chromosome 19q13.33, encoding Protein arginine N-methyltransferase 1 (Q99873). Arginine methyltransferase that methylates (mono and asymmetric dimethylation) the guanidino nitrogens of arginyl residues present in proteins such as ESR1, histone H2, H3 and H4, FMR1, ILF3, HNRNPA1, HNRNPD, NFATC2IP, SUPT5H, TAF15, EWS, HABP4, SERBP1, RBM15, FOXO1, CHTOP, MAP3…. It is a common-essential gene (DepMap: required in 98.7% of cancer cell lines).

This gene encodes a member of the protein arginine N-methyltransferase (PRMT) family. Post-translational modification of target proteins by PRMTs plays an important regulatory role in many biological processes, whereby PRMTs methylate arginine residues by transferring methyl groups from S-adenosyl-L-methionine to terminal guanidino nitrogen atoms. The encoded protein is a type I PRMT and is responsible for the majority of cellular arginine methylation activity. Increased expression of this gene may play a role in many types of cancer. Alternatively spliced transcript variants encoding multiple isoforms have been observed for this gene, and a pseudogene of this gene is located on the long arm of chromosome 5.

Source: NCBI Gene 3276 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 38 total
• Druggable target: yes — 8 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 98.7% of screened cell lines (common-essential)
• MANE Select transcript: NM_001536

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:5187
Approved symbol	PRMT1
Name	protein arginine methyltransferase 1
Location	19q13.33
Locus type	gene with protein product
Status	Approved
Aliases	HCP1, ANM1
Ensembl gene	ENSG00000126457
Ensembl biotype	protein_coding
OMIM	602950
Entrez	3276

Gene structure

Transcript identifiers

Ensembl transcripts: 46 — 36 protein_coding, 6 retained_intron, 3 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000391851, ENST00000454376, ENST00000524771, ENST00000525616, ENST00000525915, ENST00000526224, ENST00000527382, ENST00000527412, ENST00000527866, ENST00000528126, ENST00000528623, ENST00000529284, ENST00000529650, ENST00000529836, ENST00000530070, ENST00000530361, ENST00000532489, ENST00000534280, ENST00000534465, ENST00000534676, ENST00000610806, ENST00000890738, ENST00000890739, ENST00000890740, ENST00000890741, ENST00000890742, ENST00000890743, ENST00000911931, ENST00000911932, ENST00000911933, ENST00000911934, ENST00000911935, ENST00000911936, ENST00000911937, ENST00000911938, ENST00000911939, ENST00000911940, ENST00000911941, ENST00000911942, ENST00000911943, ENST00000911944, ENST00000911945, ENST00000911946, ENST00000911947, ENST00000911948, ENST00000966375

RefSeq mRNA: 3 — MANE Select: NM_001536 NM_001207042, NM_001536, NM_198318

CCDS: CCDS42592, CCDS46145, CCDS74425

Canonical transcript exons

ENST00000454376 — 11 exons

Exon	Start	End
ENSE00000864518	49688162	49688447
ENSE00001372151	49679872	49679925
ENSE00002199981	49677271	49677316
ENSE00003462600	49683927	49684069
ENSE00003490501	49684754	49684841
ENSE00003496480	49681910	49682065
ENSE00003510606	49684922	49685037
ENSE00003576799	49682196	49682259
ENSE00003666279	49686605	49686726
ENSE00003674689	49686093	49686243
ENSE00003687086	49680487	49680588

Expression profiles

Bgee: expression breadth ubiquitous, 274 present calls, max score 98.81.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 38.3807 / max 183.4945, expressed in 1809 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
177047	29.2280	1803
177046	7.2535	1641
177050	0.8256	486
208899	0.5733	267
177045	0.3384	158
177048	0.1271	36
177049	0.0349	17

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
embryo	UBERON:0000922	98.81	gold quality
right uterine tube	UBERON:0001302	98.63	gold quality
ganglionic eminence	UBERON:0004023	98.63	gold quality
adenohypophysis	UBERON:0002196	98.50	gold quality
body of uterus	UBERON:0009853	98.49	gold quality
endocervix	UBERON:0000458	98.48	gold quality
hindlimb stylopod muscle	UBERON:0004252	98.46	gold quality
cortical plate	UBERON:0005343	98.46	gold quality
right hemisphere of cerebellum	UBERON:0014890	98.39	gold quality
pituitary gland	UBERON:0000007	98.37	gold quality
left uterine tube	UBERON:0001303	98.35	gold quality
right ovary	UBERON:0002118	98.31	gold quality
left ovary	UBERON:0002119	98.28	gold quality
gastrocnemius	UBERON:0001388	98.21	gold quality
cerebellar hemisphere	UBERON:0002245	98.20	gold quality
cerebellar cortex	UBERON:0002129	98.17	gold quality
stromal cell of endometrium	CL:0002255	98.14	gold quality
muscle of leg	UBERON:0001383	98.13	gold quality
ventricular zone	UBERON:0003053	98.11	gold quality
ectocervix	UBERON:0012249	98.09	gold quality
triceps brachii	UBERON:0001509	98.08	gold quality
apex of heart	UBERON:0002098	97.97	gold quality
right atrium auricular region	UBERON:0006631	97.96	gold quality
gluteal muscle	UBERON:0002000	97.95	gold quality
left adrenal gland cortex	UBERON:0035825	97.81	gold quality
right adrenal gland	UBERON:0001233	97.78	gold quality
left adrenal gland	UBERON:0001234	97.77	gold quality
muscle layer of sigmoid colon	UBERON:0035805	97.76	gold quality
right lobe of thyroid gland	UBERON:0001119	97.74	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	97.73	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-CURD-114	yes	59.21
E-HCAD-8	yes	47.10
E-HCAD-10	yes	34.57
E-CURD-112	yes	19.72
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
HSPA5

Upstream regulators (CollecTRI, top): ESR1, HIF1A, HNF4A, KLF1, MYC, NR1I2, NR5A2, PIAS1

miRNA regulators (miRDB)

25 targeting PRMT1, 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-4803	99.98	71.99	3117
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-3605-5P	99.96	67.12	932
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-548D-3P	99.87	70.67	4362
HSA-MIR-548BB-3P	99.86	70.58	4354
HSA-MIR-4728-5P	99.85	69.39	4718
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
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-1249-5P	99.61	66.55	2049
HSA-MIR-6797-5P	99.61	66.55	2084
HSA-MIR-7160-5P	99.11	67.17	2207
HSA-MIR-3679-5P	94.75	66.46	862
HSA-MIR-1185-5P	94.47	65.95	725
HSA-MIR-4734	88.28	63.44	87

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 98.7% of screened cell lines, common-essential.

Literature-anchored findings (GeneRIF, showing 40)

• several proteins extracted from HeLa cells were methylated by PRMT1 (PMID:12183049)
• SAF-A is arginine methylated by PRMT1 (PMID:15364944)
• These results suggest that PRMT1 plays a post-translationally important role in regulating the transcriptional activity. (PMID:15737635)
• PRMT1 arginine-methylates MRE11 and thus regulates the activity of MRE11-RAD50-NBS1 complex during the intra-S-phase DNA damage checkpoint response. (PMID:15741314)
• A fraction of PRMT1 is located in the nucleus, but the protein is predominantly cytoplasmic. (PMID:16159886)
• GAR (Glycine Arginine rich) motif is a region required for 53BP1 DNA binding activity and as the site of methylation by PRMT1. (PMID:16294045)
• a glycine-arginine rich (GAR) stretch of 53BP1 lying upstream of the Tudor motifs is methylated by PRMT1 (PMID:16294047)
• arginine dimethylation of heterogeneous nuclear ribonucleoprotein K by protein-arginine methyltransferase 1 inhibits its interaction with c-Src (PMID:16492668)
• SET-mediated promoter hypoacetylation is a prerequisite for coactivation of the estrogen-responsive pS2 gene by PRMT1 (PMID:16861234)
• Methylates Ki-1/57 and CGI-55 (PAI-1 mRNA-binding protein) at a conserved Gly/Arg-rich motif cluster. (PMID:16879614)
• PRMT1 is a coactivator for HNF4, an orphan nuclear receptor that regulates the expression of genes involved in diverse metabolic pathways (PMID:17052457)
• CAF1 is a new regulator of PRMT1-dependent arginine methylation. (PMID:17264152)
• Our results suggest that PRMT1 might be involved in the previously reported methylation of Arg25 in HMGA1a in vivo. (PMID:17550233)
• relative balance of PRMT1 isoforms is altered in breast cancer (PMID:17848568)
• Study uncovers an essential function of PRMTs in oncogenesis and reveals their potential as novel therapeutic targets in human cancer. (PMID:17891136)
• Our results suggest that PRMT1-mediated methylation serves as a positive modulator of IR/IRS-1/PI3-K pathway and subsequent glucose uptake in skeletal muscle cells. (PMID:17971302)
• PRMT1- dependent methylation of RUNX1 at arginine residues 206 and 210 abrogates its association with SIN3A. (PMID:18316480)
• C-terminal domain containing the methylated arginine residues is known to promote PAPBN1 self-association, and arginine methylation has been reported to inhibit self-association of an orthologous protein (PMID:18495660)
• These data indicate that the methylation of estrogen receptor alpha is a physiological process occurring in the cytoplasm of normal and malignant epithelial breast cells and that ERalpha is hypermethylated in a subset of breast cancers. (PMID:18657504)
• PRMT1 selectively recognizes a set of amino acid sequences in substrates that extend beyond the “RGG” paradigm. (PMID:18700728)
• examined the expression pattern of protein arginine methyltransferase 1 gene in colon cancer patients (PMID:19078953)
• Data demonstrate that arginine methylation of TAF15 by PRMT1 is a crucial event determining its proper localization and gene regulatory function. (PMID:19124016)
• demonstrated mutual interactions and functional interplays between PXR and PRMT1, and this interaction may be important for the epigenetics of PXR-regulated gene expression (PMID:19144646)
• Type I Arginine Methyltransferases PRMT1 and PRMT-3 Act Distributively (PMID:19158082)
• Study shows that enzymatic activity is required for nucleo-cytoplasmic shuttling of PRMT1v2, as a catalytically inactive mutant highly accumulates in the nucleus. (PMID:19170758)
• High PRMT1 variant v2 expression is associated with colon cancer. (PMID:19414388)
• 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)
• In this review, protein arginine methylation is a covalent modification that results in the addition of methyl groups to the nitrogen atoms of the arginine side chains and is catalyzed by a family of protein arginine methyltransferases (PRMTs). (PMID:19643181)
• In this review, the pathology previously attributed to elevated asymmetric dimethylarginine may be manifested, at least in part, through altered enzyme activity involved in ADMA regulation, specifically dimethylarginine dimethylaminohydrolase-1 and PRMT. (PMID:19682581)
• these data thus suggest that the PRMT1 plays a key role as a cellular regulator of HSV-1 replication through ICP27 RGG-box methylation. (PMID:19913501)
• we show that PRMT1 methylates FMRP in cells, suggesting a model where methylation of the RGG box modulates either the quantity or the identity of the RNAs bound by FMRP. (PMID:20064924)
• Modulation of the p38 MAPK pathway by PRMT1 is a novel mechanism regulating megakaryocytic differentiation. (PMID:20442406)
• PRMT1 may be involved in human carcinogenesis and may thus be a therapeutic target for various types of cancer. (PMID:20473859)
• PRMT1 was detected in colonic muscosa, enteric nervous system and endothelial cells of colon from patients with Hirschsprung disease. (PMID:20497508)
• In this study, we use Forster resonance energy transfer (FRET) to determine dissociation constant (K(D)) values for dimerization of PRMT1 and PRMT6. (PMID:20812326)
• The PRMT1 is transcriptional coactivators that deposit H3R17me2a and H4R3me2a marks, respectively. (PMID:21172665)
• these results identify preferred PRMT1 methylation sequences of hnRNP K by direct methylation assay and implicate a role of arginine methylation in regulating intracellular distribution of hnRNP K. (PMID:21184736)
• These results revealed a cooperative role of TLS and PRMT1 in transcriptional regulation of survivin. (PMID:21187067)
• Survival curves revealed that PRMT1-v1 status-low expression relates to longer disease-free survival (DFS; p = 0.036). (PMID:21229402)
• methylation of Axin by PRMT1 may serve as a finely tuned regulation mechanism for Wnt/beta-catenin signaling. (PMID:21242974)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	prmt1	ENSDARG00000010246
mus_musculus	Prmt1	ENSMUSG00000109324
rattus_norvegicus	Prmt1	ENSRNOG00000026109
drosophila_melanogaster	Art2	FBGN0031592

Paralogs (7): PRMT8 (ENSG00000111218), PRMT7 (ENSG00000132600), CARM1 (ENSG00000142453), PRMT2 (ENSG00000160310), PRMT9 (ENSG00000164169), PRMT3 (ENSG00000185238), PRMT6 (ENSG00000198890)

Protein

Protein identifiers

Protein arginine N-methyltransferase 1 — Q99873 (reviewed: Q99873)

Alternative names: Histone-arginine N-methyltransferase PRMT1, Interferon receptor 1-bound protein 4

All UniProt accessions (12): Q99873, A0A3Q8AM27, A0A3Q8ATF5, A0A3S6H812, E9PIE2, E9PIX6, E9PKG1, E9PMW9, E9PMZ2, E9PNR9, E9PQ98, H0YDE4

UniProt curated annotations — full annotation on UniProt →

Function. Arginine methyltransferase that methylates (mono and asymmetric dimethylation) the guanidino nitrogens of arginyl residues present in proteins such as ESR1, histone H2, H3 and H4, FMR1, ILF3, HNRNPA1, HNRNPD, NFATC2IP, SUPT5H, TAF15, EWS, HABP4, SERBP1, RBM15, FOXO1, CHTOP, MAP3K5/ASK1, MICU1 and NPRL2. Constitutes the main enzyme that mediates monomethylation and asymmetric dimethylation of histone H4 ‘Arg-3’ (H4R3me1 and H4R3me2a, respectively), a specific tag for epigenetic transcriptional activation. May be involved in the regulation of TAF15 transcriptional activity, act as an activator of estrogen receptor (ER)-mediated transactivation, play a key role in neurite outgrowth and act as a negative regulator of megakaryocytic differentiation, by modulating p38 MAPK pathway. Methylates RBM15, promoting ubiquitination and degradation of RBM15. Methylates MRE11 and TP53BP1, promoting the DNA damage response. Methylates FOXO1 and retains it in the nucleus increasing its transcriptional activity. Methylates CHTOP and this methylation is critical for its 5-hydroxymethylcytosine (5hmC)-binding activity. Methylates MAP3K5/ASK1 at ‘Arg-78’ and ‘Arg-80’ which promotes association of MAP3K5 with thioredoxin and negatively regulates MAP3K5 association with TRAF2, inhibiting MAP3K5 stimulation and MAP3K5-induced activation of JNK. Methylates H4R3 in genes involved in glioblastomagenesis in a CHTOP- and/or TET1-dependent manner. Plays a role in regulating alternative splicing in the heart. Methylates NPRL2 at ‘Arg-78’ leading to inhibition of its GTPase activator activity and then the GATOR1 complex and consequently inducing timely mTORC1 activation under methionine-sufficient conditions. Methylates the C-terminus of DSP, promoting its phosphorylation by GSK3B and subsequent recruitment to desmosome cell-cell junctions.

Subunit / interactions. Homodimer. Homooctamer; individual homodimers associates to form a homooctamer. Individual homodimers can associate to form a homohexamer. Heterodimer with PRMT8. Interacts with BTG1, BTG2, NFATC2IP and IFNAR1. Interacts with and methylates CHTOP, thereby enabling the interaction of CHTOP with the 5FMC complex. Interacts with ILF3 and SUPT5H. Interacts with and methylates FOXO1, leading to the nuclear retention of FOXO1 and the stimulation of FOXO1 transcriptional activity. Methylation of FOXO1 is increased upon oxidative stress. Interacts with and probably methylates ATXN2L. Component of the methylosome, a 20S complex containing at least CLNS1A/pICln, PRMT5/SKB1, WDR77/MEP50, PRMT1 and ERH. Interacts with DHX9 (via RGG region). Interacts (via N-terminus) with HABP4. Interacts with MAP3K5/ASK1; the interaction results in MAP3K5 methylation by PRMT1 which inhibits MAP3K5 activation. Interacts with TRIM48; the interaction results in ubiquitination of PRMT1 by TRIM48, leading to PRMT1 proteasomal degradation and activation of MAP3K5. Interacts with GATOR1 complex; this interaction is S-adenosyl-L-methionine (SAM) dependent and is perturbated by SAMTOR in a SAM-sensitive manner. Interacts with GFI1; promoting recognition and binding of MRE11 and TP53BP1 substrates by PRMT1.

Subcellular location. Nucleus. Nucleoplasm. Cytoplasm. Cytosol. Lysosome membrane.

Tissue specificity. Widely expressed. Expressed strongly in colorectal cancer cells (at protein level). Expressed strongly in colorectal cancer tissues compared to wild-type colon samples (at protein level). Expressed strongly in colorectal cancer tissues compared to wild-type colon samples.

Post-translational modifications. Polyubiquitinated at Lys-145 by the SCF(FBXL17) complex, leading to its subsequent degradation. Ubiquitination is regulated by acetylation at Lys-228 and Lys-233. Polyubiquitinated by E3 ubiquitin-protein ligase TRIM48, leading to suppression of MAP3K5/ASK1 methylation and subsequent MAP3K5 activation. Acetylation at Lys-228 and Lys-233 regulates ubiquitination by the SCF(FBXL17) complex. Acetylated at Lys-233 by p300/EP300. Deacetylated at Lys-228 and Lys-233 by SIRT1.

Similarity. Belongs to the class I-like SAM-binding methyltransferase superfamily. Protein arginine N-methyltransferase family.

Isoforms (4)

UniProt ID	Names	Canonical?
Q99873-1	1, V2	yes
Q99873-2	2, V3
Q99873-3	3, V1
Q99873-5	4

RefSeq proteins (3): NP_001193971, NP_001527, NP_938074 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR025799	Arg_MeTrfase	Family
IPR029063	SAM-dependent_MTases_sf	Homologous_superfamily
IPR041698	Methyltransf_25	Domain
IPR055135	PRMT_dom	Domain

Pfam: PF13649, 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), 3 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)
• N(omega)-methyl-L-arginyl-[protein] + S-adenosyl-L-methionine = N(omega),N(omega)-dimethyl-L-arginyl-[protein] + S-adenosyl-L-homocysteine + H(+) (RHEA:48104)

UniProt features (71 total): strand 17, helix 15, binding site 9, mutagenesis site 8, modified residue 5, splice variant 4, sequence conflict 3, turn 3, active site 2, sequence variant 2, chain 1, domain 1, cross-link 1

Structure

Experimental structures (PDB)

8 structures.

PDB	Method	Resolution (Å)
6NT2	X-RAY DIFFRACTION	2.48
9BH4	ELECTRON MICROSCOPY	2.55
8Z2Z	ELECTRON MICROSCOPY	3.25
9BHG	ELECTRON MICROSCOPY	3.25
8Z7O	ELECTRON MICROSCOPY	3.35
9BHD	ELECTRON MICROSCOPY	3.38
8Z7H	ELECTRON MICROSCOPY	3.56
9JP0	ELECTRON MICROSCOPY	3.68

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q99873-F1	89.14	0.83

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 (2): 162; 171

Ligand- & substrate-binding residues (9): 146; 147; 147; 63; 72; 72; 96; 118; 118

Post-translational modifications (6): 134, 228, 233, 304, 307, 145

Mutagenesis-validated functional residues (8):

Position	Phenotype
92	loss of foxo1 methylation, its nuclear retention, and transcriptional activity.
93	loss of foxo1 methylation, its nuclear retention, and transcriptional activity.
94	loss of foxo1 methylation, its nuclear retention, and transcriptional activity.
98	does not restore mtorc1 signaling pathway upon methionine or s-adenosyl-l-methionine (sam) stimulation in prmt1-depleted
162	does not restore mtorc1 signaling pathway upon methionine or sam stimulation in prmt1-depleted cells. does not affect in
280	no effect on s-adenosyl-l-methionine binding but reduced ews protein methylation; when associated with a-322 and a-359.
322	no effect on s-adenosyl-l-methionine binding but reduced ews protein methylation; when associated with a-280 and a-359.
359	no effect on s-adenosyl-l-methionine binding but reduced ews protein methylation; when associated with a-280 and a-322.

Function

Pathways and Gene Ontology

Reactome pathways

24 pathways

ID	Pathway
R-HSA-3214858	RMTs methylate histone arginines
R-HSA-6804114	TP53 Regulates Transcription of Genes Involved in G2 Cell Cycle Arrest
R-HSA-8936459	RUNX1 regulates genes involved in megakaryocyte differentiation and platelet function
R-HSA-9009391	Extra-nuclear estrogen signaling
R-HSA-9018519	Estrogen-dependent gene expression
R-HSA-9694631	Maturation of nucleoprotein
R-HSA-162582	Signal Transduction
R-HSA-1643685	Disease
R-HSA-212436	Generic Transcription Pathway
R-HSA-3247509	Chromatin modifying enzymes
R-HSA-3700989	Transcriptional Regulation by TP53
R-HSA-4839726	Chromatin organization
R-HSA-5663205	Infectious disease
R-HSA-6791312	TP53 Regulates Transcription of Cell Cycle Genes
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-8878171	Transcriptional regulation by RUNX1
R-HSA-8939211	ESR-mediated signaling
R-HSA-9006931	Signaling by Nuclear Receptors
R-HSA-9679506	SARS-CoV Infections
R-HSA-9694516	SARS-CoV-2 Infection
R-HSA-9694635	Translation of Structural Proteins
R-HSA-9772573	Late SARS-CoV-2 Infection Events
R-HSA-9824446	Viral Infection Pathways

MSigDB gene sets: 405 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_DOUBLE_STRAND_BREAK_REPAIR, GOBP_HEMOGLOBIN_METABOLIC_PROCESS, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_DNA_RECOMBINATION, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EMBRYO_DEVELOPMENT_ENDING_IN_BIRTH_OR_EGG_HATCHING, GOBP_MUSCLE_TISSUE_DEVELOPMENT, GOBP_POSITIVE_REGULATION_OF_ERYTHROCYTE_DIFFERENTIATION, GOBP_MYELOID_CELL_HOMEOSTASIS, GOBP_RESPONSE_TO_ACID_CHEMICAL, GOCC_VACUOLAR_MEMBRANE, MODULE_77, GCM_NPM1, GOBP_ERYTHROCYTE_HOMEOSTASIS

GO Biological Process (38): in utero embryonic development (GO:0001701), chromatin remodeling (GO:0006338), regulation of DNA-templated transcription (GO:0006355), protein methylation (GO:0006479), DNA damage response (GO:0006974), cell surface receptor signaling pathway (GO:0007166), positive regulation of cell population proliferation (GO:0008284), RNA splicing (GO:0008380), peptidyl-arginine methylation (GO:0018216), viral protein processing (GO:0019082), regulation of BMP signaling pathway (GO:0030510), neuron projection development (GO:0031175), negative regulation of apoptotic process (GO:0043066), positive regulation of erythrocyte differentiation (GO:0045648), regulation of megakaryocyte differentiation (GO:0045652), negative regulation of megakaryocyte differentiation (GO:0045653), positive regulation of translation (GO:0045727), negative regulation of JNK cascade (GO:0046329), positive regulation of hemoglobin biosynthetic process (GO:0046985), cardiac muscle tissue development (GO:0048738), protein homooligomerization (GO:0051260), cellular response to methionine (GO:0061431), positive regulation of p38MAPK cascade (GO:1900745), positive regulation of TORC1 signaling (GO:1904263), positive regulation of double-strand break repair via homologous recombination (GO:1905168), double-strand break repair via homologous recombination (GO:0000724), negative regulation of translation (GO:0017148), BMP signaling pathway (GO:0030509), negative regulation of BMP signaling pathway (GO:0030514), cellular response to nutrient levels (GO:0031669), methylation (GO:0032259), cellular response to amino acid starvation (GO:0034198), TORC1 signaling (GO:0038202), negative regulation of translational initiation (GO:0045947), protein localization to lysosome (GO:0061462), membraneless organelle assembly (GO:0140694), negative regulation of TORC1 signaling (GO:1904262), negative regulation of double-strand break repair via homologous recombination (GO:2000042)

GO Molecular Function (18): RNA binding (GO:0003723), methyltransferase activity (GO:0008168), N-methyltransferase activity (GO:0008170), protein methyltransferase activity (GO:0008276), methyl-CpG binding (GO:0008327), protein-arginine N-methyltransferase activity (GO:0016274), enzyme binding (GO:0019899), protein-arginine omega-N monomethyltransferase activity (GO:0035241), protein-arginine omega-N asymmetric methyltransferase activity (GO:0035242), histone methyltransferase activity (GO:0042054), identical protein binding (GO:0042802), histone H4R3 methyltransferase activity (GO:0044020), mitogen-activated protein kinase p38 binding (GO:0048273), GATOR1 complex binding (GO:0106080), S-adenosyl-L-methionine binding (GO:1904047), protein binding (GO:0005515), transferase activity (GO:0016740), histone H4 methyltransferase activity (GO:0140939)

GO Cellular Component (8): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), lysosomal membrane (GO:0005765), cytosol (GO:0005829), methylosome (GO:0034709), lysosome (GO:0005764), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-14 pathways:

Category	Pathways
ESR-mediated signaling	2
Generic Transcription Pathway	2
Chromatin modifying enzymes	1
TP53 Regulates Transcription of Cell Cycle Genes	1
Transcriptional regulation by RUNX1	1
Translation of Structural Proteins	1
RNA Polymerase II Transcription	1
Chromatin organization	1
Disease	1
Transcriptional Regulation by TP53	1
Gene expression (Transcription)	1
Signaling by Nuclear Receptors	1
Signal Transduction	1
Viral Infection Pathways	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
protein-arginine N-methyltransferase activity	3
megakaryocyte differentiation	2
positive regulation of protein metabolic process	2
methyltransferase activity	2
protein methyltransferase activity	2
protein binding	2
cytoplasm	2
chordate embryonic development	1
chromatin organization	1
DNA-templated transcription	1
regulation of gene expression	1
regulation of RNA biosynthetic process	1
protein alkylation	1
macromolecule methylation	1
cellular response to stress	1
signal transduction	1
cell population proliferation	1
regulation of cell population proliferation	1
positive regulation of cellular process	1
RNA processing	1
protein methylation	1
peptidyl-arginine modification	1
viral process	1
viral gene expression	1
BMP signaling pathway	1
regulation of transmembrane receptor protein serine/threonine kinase signaling pathway	1
regulation of cellular response to growth factor stimulus	1
neuron development	1
plasma membrane bounded cell projection organization	1
apoptotic process	1
regulation of apoptotic process	1
negative regulation of programmed cell death	1
erythrocyte differentiation	1
positive regulation of myeloid cell differentiation	1
regulation of erythrocyte differentiation	1
regulation of myeloid cell differentiation	1
negative regulation of myeloid cell differentiation	1
regulation of megakaryocyte differentiation	1
translation	1

Protein interactions and networks

STRING

3918 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PRMT1	BTG2	P78543	981
PRMT1	EP300	Q09472	934
PRMT1	PRMT5	O14744	927
PRMT1	CARM1	Q86X55	894
PRMT1	APOE	P02649	887
PRMT1	H4C16	P02304	859
PRMT1	PRMT3	O60678	838
PRMT1	TP53	P04637	835
PRMT1	NCOA2	Q15596	820
PRMT1	NCOA3	Q9Y6Q9	800
PRMT1	FUS	P35637	799
PRMT1	H4C7	Q99525	796
PRMT1	YY1	P25490	790
PRMT1	KHDRBS1	Q07666	775
PRMT1	CREBBP	Q92793	768

IntAct

293 interactions, top by confidence:

A	B	Type	Score
N	G3BP1	psi-mi:“MI:0914”(association)	0.980
AXIN1	CTNNB1	psi-mi:“MI:0914”(association)	0.940
EIF3D	EIF3A	psi-mi:“MI:0914”(association)	0.860
VIM	NEFL	psi-mi:“MI:0914”(association)	0.840
PRMT8	SYNCRIP	psi-mi:“MI:0914”(association)	0.830
FBL	NOP56	psi-mi:“MI:0914”(association)	0.800
HNRNPR	PRMT1	psi-mi:“MI:0915”(physical association)	0.740
PRMT1	HNRNPR	psi-mi:“MI:0915”(physical association)	0.740
PRMT1	PRMT1	psi-mi:“MI:0915”(physical association)	0.720
FUS	PRMT1	psi-mi:“MI:0915”(physical association)	0.660
FUS	PRMT1	psi-mi:“MI:0403”(colocalization)	0.660
	NR4A1	psi-mi:“MI:0915”(physical association)	0.650
USE1	NBAS	psi-mi:“MI:0914”(association)	0.640
DYNLT1	DYNC1LI2	psi-mi:“MI:0914”(association)	0.640
SLC17A5	LGALS8	psi-mi:“MI:0914”(association)	0.640
PRMT1	H4C16	psi-mi:“MI:0213”(methylation reaction)	0.620
NR4A1	PRMT1	psi-mi:“MI:0915”(physical association)	0.620
PRMT1	NR4A1	psi-mi:“MI:0915”(physical association)	0.620
SPEG	PRMT1	psi-mi:“MI:0915”(physical association)	0.560
NTAQ1	PRMT1	psi-mi:“MI:0915”(physical association)	0.560
PRMT8	PRMT1	psi-mi:“MI:0915”(physical association)	0.560
PRMT1	PRMT8	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (1252): PRMT1 (Affinity Capture-MS), PRMT1 (Affinity Capture-MS), PRMT1 (Two-hybrid), HNRNPR (Two-hybrid), SPEG (Two-hybrid), WDYHV1 (Two-hybrid), PRMT8 (Two-hybrid), PRMT1 (Affinity Capture-RNA), PRMT1 (Affinity Capture-RNA), PRMT1 (Affinity Capture-RNA), PRMT1 (Affinity Capture-MS), PRMT1 (Affinity Capture-MS), PRMT1 (Affinity Capture-MS), HIST1H4A (Biochemical Activity), PRMT1 (Affinity Capture-MS)

ESM2 similar proteins: A0JMU5, A2AV36, A2Y8B9, A2Z0C0, A2Z8S0, A4IG42, A4QP75, A6QQV6, A7YW45, B0JYW5, B0X4N1, B3DLB3, B3M1E1, B3MF31, B3NP10, B3P4N5, B4GA28, B4GZ20, B4HJC0, B4I8G2, B4P925, B4PVH6, B4QI55, B4QVW6, B5DZN7, D9IVE5, Q0J2C6, Q16NS8, Q29B63, Q3U3W5, Q5RGQ2, Q5U4E8, Q5VS72, Q5ZIB9, Q6NTR1, Q6NUA1, Q6P2P2, Q6PAK3, Q6PCI6, Q75G68

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

6 interactions.

A	Effect	B	Mechanism
PRMT1	up-regulates	TAF15	methylation
PRMT1	down-regulates	CNBP	methylation
RALY	“up-regulates quantity”	PRMT1	“post transcriptional regulation”
PRMT1	“down-regulates activity”	FUS	methylation
CSNK1A1	“up-regulates activity”	PRMT1	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 204 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
RHOBTB1 GTPase cycle	6	20.5×	3e-05
Transport of Mature Transcript to Cytoplasm	5	13.7×	2e-03
mRNA 3’-end processing	9	12.8×	4e-06
Transport of Mature mRNA derived from an Intron-Containing Transcript	10	10.9×	4e-06
Processing of Capped Intron-Containing Pre-mRNA	17	10.1×	6e-10
RNA Polymerase II Transcription Termination	6	9.5×	2e-03
mRNA Polyadenylation	12	7.6×	7e-06
PKR-mediated signaling	7	7.1×	3e-03

GO biological processes:

GO term	Partners	Fold	FDR
negative regulation of mRNA splicing, via spliceosome	5	20.7×	7e-04
stress granule assembly	6	19.5×	1e-04
mRNA stabilization	8	15.8×	1e-05
negative regulation of translation	11	11.7×	2e-06
translational initiation	5	9.7×	9e-03
mRNA export from nucleus	6	9.6×	3e-03
positive regulation of translation	7	8.6×	2e-03
mRNA transport	6	8.5×	5e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	21
Likely benign	1
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

1946 predictions. Top by Δscore:

Variant	Effect	Δscore
19:49677317:GT:G	donor_loss	1.0000
19:49679923:G:GT	donor_gain	1.0000
19:49679923:GAA:G	donor_gain	1.0000
19:49679926:G:GG	donor_gain	1.0000
19:49680482:CCCA:C	acceptor_loss	1.0000
19:49680484:CAGGT:C	acceptor_loss	1.0000
19:49680485:A:AG	acceptor_gain	1.0000
19:49680485:A:AT	acceptor_loss	1.0000
19:49680486:G:GG	acceptor_gain	1.0000
19:49680486:GGT:G	acceptor_gain	1.0000
19:49680587:AGG:A	donor_loss	1.0000
19:49680589:G:C	donor_loss	1.0000
19:49680590:T:G	donor_loss	1.0000
19:49681902:T:A	acceptor_gain	1.0000
19:49681905:CCTAG:C	acceptor_loss	1.0000
19:49681908:A:AC	acceptor_loss	1.0000
19:49681908:A:AG	acceptor_gain	1.0000
19:49681908:AG:A	acceptor_gain	1.0000
19:49681909:G:GC	acceptor_gain	1.0000
19:49681909:GG:G	acceptor_gain	1.0000
19:49681909:GGA:G	acceptor_gain	1.0000
19:49681909:GGAGA:G	acceptor_gain	1.0000
19:49682061:TCGGG:T	donor_gain	1.0000
19:49682063:GGG:G	donor_gain	1.0000
19:49682064:GG:G	donor_gain	1.0000
19:49682064:GGG:G	donor_gain	1.0000
19:49682065:GG:G	donor_gain	1.0000
19:49682066:G:GG	donor_gain	1.0000
19:49682066:G:T	donor_loss	1.0000
19:49682067:T:A	donor_loss	1.0000

AlphaMissense

2484 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:49680550:T:C	Y52H	1.000
19:49680553:T:C	Y53H	1.000
19:49680553:T:G	Y53D	1.000
19:49680554:A:G	Y53C	1.000
19:49680556:T:C	F54L	1.000
19:49680558:T:A	F54L	1.000
19:49680558:T:G	F54L	1.000
19:49680560:A:T	D55V	1.000
19:49680562:T:C	S56P	1.000
19:49680563:C:T	S56F	1.000
19:49680565:T:A	Y57N	1.000
19:49680565:T:C	Y57H	1.000
19:49680566:A:G	Y57C	1.000
19:49680568:G:C	A58P	1.000
19:49680571:C:G	H59D	1.000
19:49680573:C:A	H59Q	1.000
19:49680573:C:G	H59Q	1.000
19:49680574:T:C	F60L	1.000
19:49680576:T:A	F60L	1.000
19:49680576:T:G	F60L	1.000
19:49680577:G:C	G61R	1.000
19:49680578:G:A	G61D	1.000
19:49680581:T:A	I62N	1.000
19:49680581:T:C	I62T	1.000
19:49680581:T:G	I62S	1.000
19:49680583:C:A	H63N	1.000
19:49680583:C:G	H63D	1.000
19:49680583:C:T	H63Y	1.000
19:49680584:A:C	H63P	1.000
19:49680584:A:G	H63R	1.000

dbSNP variants (sampled 300 via entrez): RS1000096176 (19:49683508 G>A), RS1000163817 (19:49686890 C>T), RS1000196752 (19:49687133 C>T), RS1000295101 (19:49688085 C>A,G,T), RS1000491710 (19:49683722 A>G), RS1000569800 (19:49677130 T>C), RS1000590152 (19:49683875 G>A,C), RS1001195414 (19:49683041 T>C,G), RS1001246232 (19:49677481 G>A,T), RS1001301276 (19:49687051 A>G), RS1001695931 (19:49677674 G>A), RS1001894613 (19:49676306 C>G,T), RS1002036044 (19:49686300 C>G,T), RS1002379346 (19:49676600 C>A,T), RS1002501118 (19:49681511 G>GT)

Disease associations

OMIM: gene MIM:602950 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST006803_99	Schizophrenia	4.000000e-11

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5524 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

8 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 405,617 (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
CHEMBL1057	FLUORESCEIN	4	329,940
CHEMBL25105	HEXAMIDINE	4	5,666
CHEMBL55	PENTAMIDINE	4	27,049
CHEMBL1088977	ADEMETIONINE	3	1,522
CHEMBL265502	SURAMIN	3	36,848
CHEMBL1214186	SINEFUNGIN	2	2,165
CHEMBL1232461	MOLIBRESIB	2	1,538
CHEMBL142304	STILBAMIDINE	2	889

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 (4 total), top 4:

Ligand	Action	Affinity	Parameter
MS023	Inhibition	7.96	pKi
C21	Inhibition	5.74	pIC50
AMI-1	Inhibition	5.06	pIC50
RM65	Inhibition	4.26	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

413 potent at pChembl≥5 of 575 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.82	Ki	1.5	nM	CHEMBL5723346
8.77	IC50	1.7	nM	CHEMBL5559689
8.52	IC50	3	nM	CHEMBL5559689
8.52	IC50	3	nM	CHEMBL5612531
8.51	IC50	3.1	nM	CHEMBL5559689
8.51	IC50	3.1	nM	CHEMBL5723346
8.49	IC50	3.2	nM	CHEMBL5559689
8.40	IC50	4	nM	CHEMBL3589030
8.40	IC50	4	nM	CHEMBL3589026
8.40	IC50	4	nM	CHEMBL3901808
8.40	IC50	4	nM	CHEMBL5517922
8.40	IC50	4	nM	CHEMBL5527874
8.30	IC50	5	nM	CHEMBL3589031
8.30	IC50	5	nM	CHEMBL3589028
8.30	IC50	5	nM	CHEMBL5565736
8.30	IC50	5	nM	CHEMBL5633975
8.28	IC50	5.3	nM	CHEMBL4084293
8.23	IC50	5.9	nM	CHEMBL5532081
8.22	IC50	6	nM	CHEMBL6174061
8.15	IC50	7	nM	CHEMBL3589029
8.15	IC50	7	nM	CHEMBL3589027
8.10	IC50	8	nM	CHEMBL3589036
8.05	IC50	9	nM	CHEMBL3901808
8.05	IC50	9	nM	CHEMBL5542306
8.05	IC50	9	nM	CHEMBL5532462
8.00	IC50	10	nM	CHEMBL5559689
8.00	IC50	10	nM	CHEMBL5567635
7.96	IC50	11	nM	CHEMBL5566241
7.96	Ki	11	nM	CHEMBL3901808
7.89	IC50	13	nM	CHEMBL3589033
7.89	IC50	13	nM	CHEMBL3589913
7.85	IC50	14	nM	CHEMBL3589037
7.85	IC50	14	nM	CHEMBL3589032
7.85	IC50	14	nM	CHEMBL5560201
7.82	IC50	15	nM	CHEMBL5557453
7.80	IC50	16	nM	CHEMBL3589038
7.80	IC50	16	nM	CHEMBL5561358
7.80	IC50	16	nM	CHEMBL5558900
7.79	IC50	16.4	nM	CHEMBL5613785
7.79	IC50	16.4	nM	CHEMBL5612658
7.77	IC50	17	nM	CHEMBL5613916
7.75	IC50	18	nM	CHEMBL3589912
7.66	IC50	22	nM	CHEMBL6058181
7.66	IC50	22	nM	CHEMBL5741457
7.62	IC50	24	nM	CHEMBL5944391
7.62	IC50	24	nM	CHEMBL5901275
7.58	IC50	26	nM	CHEMBL3589042
7.57	IC50	27	nM	CHEMBL3589034
7.57	IC50	27	nM	CHEMBL5557488
7.57	IC50	27	nM	CHEMBL5770140

PubChem BioAssay actives

220 with measured affinity, of 1131 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	2069865: Inhibition of PRMT1 (unknown origin) 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’-[[5-(3,3-dimethyl-1-oxaspiro[4.5]decan-8-yl)-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	2126855: Inhibition of PRMT1 (unknown origin) by scintillation proximity assay	ic50	0.0030	uM
N’-[[5-(3-chloro-4-propan-2-yloxyphenyl)-1H-pyrazol-4-yl]methyl]-N’-methylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0040	uM
N’-[(2-cyclohexyloxyphenyl)methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0040	uM
N’-methyl-N’-[[2-[(1S,2R)-2-methylcyclohexyl]oxyphenyl]methyl]ethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0040	uM
N’-methyl-N’-[[5-(4-propan-2-yloxyphenyl)-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0040	uM
N’-methyl-N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine	1319862: Inhibition of human PRMT1 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation proximity assay	ic50	0.0040	uM
N’-methyl-N’-[[5-[4-(2-methylpropyl)phenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0050	uM
N’-[[5-(3-chloro-4-propan-2-yloxyphenyl)-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0050	uM
N’-[[3-(2-chlorophenyl)sulfanylphenyl]methyl]-N’-methylethane-1,2-diamine	2138388: Inhibition of PRMT1 (unknown origin)	ic50	0.0050	uM
N’-[[2-(4,4-dimethylcyclohexyl)oxyphenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0050	uM
N,N’-dimethyl-N’-[[5-(4-propan-2-yloxyphenyl)-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0070	uM
N’-methyl-N’-[[5-(4-phenoxyphenyl)-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0070	uM
N,N’-dimethyl-N’-[[5-[3-(2-phenylethoxy)-5-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]methyl]ethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0080	uM
N’-methyl-N’-[[2-[(1S,2S)-2-methylcyclohexyl]oxyphenyl]methyl]ethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0090	uM
N’-[(2-cyclohexyloxyphenyl)methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0090	uM
N’-[[2-[(3-chlorophenyl)methoxy]phenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0100	uM
N’-[[2-[(3-chlorophenyl)methoxy]phenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0110	uM
N’-[[5-(4-ethoxyphenyl)-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0130	uM
2-[4-[4-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-5-yl]phenoxy]butan-1-ol	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0130	uM
N’-[[5-[3-(2-cyclohexylethoxy)-5-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0140	uM
N’-[[5-(3-chloro-4-propan-2-yloxyphenyl)-1-methylpyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0140	uM
N’-[[2-[4,4-bis(methoxymethyl)cyclohexyl]oxyphenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0140	uM
N’-[[2-[4,4-bis(ethoxymethyl)cyclohexyl]oxyphenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0150	uM
4-methyl-2-[3-[4-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-5-yl]-5-(trifluoromethyl)phenoxy]pentan-1-ol	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0160	uM
N,N’-dimethyl-N’-[[2-[(1S,2R)-2-methylcyclohexyl]oxyphenyl]methyl]ethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0160	uM
N,N’-dimethyl-N’-[[2-[(1S,2S)-2-methylcyclohexyl]oxyphenyl]methyl]ethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0160	uM
2-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-1-(2-bromophenyl)guanidine	2127581: Inhibition of PRMT1 (unknown origin)	ic50	0.0164	uM
2-[3-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]-1-(2-bromophenyl)guanidine	2126856: Inhibition of PRMT1 (unknown origin) by fluorescence based analysis	ic50	0.0170	uM
N’-[[5-(4-fluorophenyl)-1H-pyrazol-4-yl]methyl]-N’-methylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0180	uM
N,N-dimethyl-3-[4-[4-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-5-yl]phenoxy]benzamide	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0260	uM
3-methyl-2-[4-[4-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-5-yl]phenoxy]butan-1-ol	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0270	uM
N’-[[2-(4-cyclohexylcyclohexyl)oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0270	uM
N’-[[2-[(4-chlorophenyl)methoxy]phenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0290	uM
N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine	2138388: Inhibition of PRMT1 (unknown origin)	ic50	0.0300	uM
(2R,3S,4R,5R)-2-[(R)-(4-chlorophenyl)-hydroxymethyl]-5-(5-hydroxy-3,6,8,10-tetrazatricyclo[7.3.0.02,6]dodeca-1(9),2,7,11-tetraen-10-yl)oxolane-3,4-diol	1510886: Inhibition of PRMT1 (unknown origin) by hotspot assay	ic50	0.0310	uM
N’-[[2-[4,4-bis(ethoxymethyl)cyclohexyl]oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0330	uM
N’-[[2-(4-cyclohexylcyclohexyl)oxyphenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0420	uM
N’-[[2-(4,4-dimethylcyclohexyl)oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0420	uM
N’-[[4-[3-chloro-4-propan-2-yloxy-5-(trifluoromethyl)phenyl]-1H-pyrazol-5-yl]methyl]-N’-methylethane-1,2-diamine	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0430	uM
N’-[[2-[(3,4-dichlorophenyl)methoxy]phenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0480	uM
N-methyl-2-[4-[5-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-4-yl]phenoxy]benzamide	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0500	uM
N’-methyl-N’-[[2-[[3-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]ethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0500	uM
(2S)-1-[[2-[4,4-bis(methoxymethyl)cyclohexyl]oxyphenyl]methyl-methylamino]-3-(methylamino)propan-2-ol	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0530	uM
(2S)-1-[[2-[4,4-bis(ethoxymethyl)cyclohexyl]oxyphenyl]methyl-methylamino]-3-(methylamino)propan-2-ol	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0560	uM
N’-[[2-[(4-chlorophenyl)methoxy]phenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0560	uM
N’-[[2-[4,4-bis(methoxymethyl)cyclohexyl]oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069832: Inhibition of PRMT1 (unknown origin) by AlphaLISA assay	ic50	0.0560	uM
N,N’-dimethyl-N’-[[2-[[3-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]ethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0590	uM
N,N-dimethyl-3-[4-[5-[[methyl-[2-(methylamino)ethyl]amino]methyl]-1H-pyrazol-4-yl]phenoxy]benzamide	1233973: Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix	ic50	0.0600	uM
N,N’-dimethyl-N’-[[2-[[4-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]ethane-1,2-diamine;dihydrochloride	2104083: Inhibition of PRMT1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0650	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, affects expression, increases methylation	6
Tretinoin	decreases expression, increases reaction, affects localization, affects binding, decreases reaction	5
sodium arsenite	decreases expression, decreases reaction, increases reaction, decreases response to substance, affects localization (+2 more)	4
Benzo(a)pyrene	increases methylation, decreases expression	3
bisphenol A	affects expression, decreases expression	2
Particulate Matter	decreases expression, increases expression	2
bisphenol F	affects cotreatment, decreases expression	1
deoxynivalenol	increases expression	1
beta-lapachone	increases expression	1
cobaltous chloride	decreases expression	1
2-bromopalmitate	decreases reaction, increases abundance, increases palmitoylation	1
di-n-butylphosphoric acid	affects expression	1
2,3,5-(triglutathion-S-yl)hydroquinone	increases ADP-ribosylation	1
CGP 52608	affects binding, increases reaction	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
obeticholic acid	increases activity, affects binding, increases reaction	1
nutlin 3	affects cotreatment, increases secretion	1
abrine	increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
2-(1H-indazol-4-yl)-6-(4-methanesulfonylpiperazin-1-ylmethyl)-4-morpholin-4-ylthieno(3,2-d)pyrimidine	decreases expression, increases response to substance	1
bisphenol AF	increases expression	1
Arsenic Trioxide	decreases expression	1
Acetaminophen	affects response to substance	1
Amiodarone	increases expression	1
Vehicle Emissions	increases expression	1
Benztropine	decreases expression	1
Berberine	decreases expression	1
Cadmium	decreases reaction, increases abundance, increases palmitoylation	1
Cisplatin	increases expression, affects reaction, decreases expression, decreases phosphorylation	1

ChEMBL screening assays

357 unique, capped per target: 344 binding, 12 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1023892	Binding	Inhibition of PRMT1	N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1). — Bioorg Med Chem Lett
CHEMBL4416349	ADMET	Inhibition of human PRMT1 expressed in Escherichia coli assessed as reduction in methylated histone H4 full length level using histone H4 full length as substrate in presence of [3H] SAM incubated for 20 mins by scintillation counting	High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). — J Med Chem
CHEMBL5444954	Functional	Affinity Phenotypic Cellular interaction: (Western Blot (inhibitor of H4R3 methylation in MCF-7 cells)) EUB0000261b PRMT1	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library

Clinical trials (associated diseases)

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