CARM1

Summary

CARM1 (coactivator associated arginine methyltransferase 1, HGNC:23393) is a protein-coding gene on chromosome 19p13.2, encoding Histone-arginine methyltransferase CARM1 (Q86X55). Methylates (mono- and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in several proteins involved in DNA packaging, transcription regulation, pre-mRNA splicing, and mRNA stability. It is a selective cancer dependency (DepMap: 22.5% of cell lines).

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 specifically on histones and other chromatin-associated proteins and is involved in regulation of gene expression. The enzyme may act in association with other proteins or within multi-protein complexes and may play a role in cell type-specific functions and cell lineage specification. A related pseudogene is located on chromosome 9.

Source: NCBI Gene 10498 — RefSeq curated summary.

At a glance

• GWAS associations: 5
• Clinical variants (ClinVar): 65 total — 1 pathogenic
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 22.5% of screened cell lines
• MANE Select transcript: NM_199141

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23393
Approved symbol	CARM1
Name	coactivator associated arginine methyltransferase 1
Location	19p13.2
Locus type	gene with protein product
Status	Approved
Aliases	PRMT4
Ensembl gene	ENSG00000142453
Ensembl biotype	protein_coding
OMIM	603934
Entrez	10498

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 5 protein_coding, 4 nonsense_mediated_decay, 2 retained_intron

ENST00000327064, ENST00000344150, ENST00000586221, ENST00000586298, ENST00000586508, ENST00000588947, ENST00000589693, ENST00000590039, ENST00000590699, ENST00000592516, ENST00000710361

RefSeq mRNA: 3 — MANE Select: NM_199141 NM_001370088, NM_001370089, NM_199141

CCDS: CCDS12250, CCDS92516

Canonical transcript exons

ENST00000327064 — 16 exons

Exon	Start	End
ENSE00001117485	10904951	10905076
ENSE00001117508	10908039	10908145
ENSE00001117512	10921615	10923075
ENSE00002890317	10871553	10871922
ENSE00003466443	10919595	10919680
ENSE00003490947	10919877	10919966
ENSE00003505946	10920659	10920748
ENSE00003515685	10916407	10916497
ENSE00003517646	10916696	10916777
ENSE00003544668	10921375	10921443
ENSE00003627200	10920834	10920946
ENSE00003637375	10920436	10920573
ENSE00003643396	10909103	10909207
ENSE00003659442	10921050	10921127
ENSE00003689737	10912184	10912294
ENSE00003692848	10913877	10914054

Expression profiles

Bgee: expression breadth ubiquitous, 279 present calls, max score 96.56.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 26.1415 / max 166.2906, expressed in 1811 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
173866	23.3329	1810
173867	1.2944	703
173873	0.9080	571
173865	0.4065	168
173864	0.1096	44
173868	0.0900	35

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
hindlimb stylopod muscle	UBERON:0004252	96.56	gold quality
gastrocnemius	UBERON:0001388	96.34	gold quality
endometrium epithelium	UBERON:0004811	96.24	gold quality
right testis	UBERON:0004534	95.93	gold quality
muscle of leg	UBERON:0001383	95.72	gold quality
left testis	UBERON:0004533	95.67	gold quality
stromal cell of endometrium	CL:0002255	95.28	gold quality
muscle organ	UBERON:0001630	94.57	gold quality
right hemisphere of cerebellum	UBERON:0014890	94.55	gold quality
testis	UBERON:0000473	93.97	gold quality
cerebellar hemisphere	UBERON:0002245	93.89	gold quality
cerebellar cortex	UBERON:0002129	93.80	gold quality
ectocervix	UBERON:0012249	93.46	gold quality
ganglionic eminence	UBERON:0004023	93.26	gold quality
endocervix	UBERON:0000458	93.20	gold quality
right uterine tube	UBERON:0001302	93.18	gold quality
cortical plate	UBERON:0005343	93.16	gold quality
lower esophagus mucosa	UBERON:0035834	93.11	gold quality
right frontal lobe	UBERON:0002810	92.94	gold quality
body of uterus	UBERON:0009853	92.88	gold quality
vastus lateralis	UBERON:0001379	92.69	gold quality
quadriceps femoris	UBERON:0001377	92.65	gold quality
Brodmann (1909) area 10	UBERON:0013541	92.52	gold quality
cerebellum	UBERON:0002037	92.22	gold quality
muscle layer of sigmoid colon	UBERON:0035805	92.07	gold quality
left uterine tube	UBERON:0001303	91.71	gold quality
prefrontal cortex	UBERON:0000451	91.70	gold quality
right ovary	UBERON:0002118	91.41	gold quality
esophagus mucosa	UBERON:0002469	91.40	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	91.23	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-MTAB-6386	no	47.65
E-ANND-3	no	3.26

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AR, ELF4, ESR1, EZH2, FOXN1, HIF1A, HNF4A, IRF6, JDP2, JUN, KAT7, NCOA1, NCOA2, NCOA3, NFKB1, NFKB, NR1H4, PAX7, RELA, SP1, TFAP2A, TP53, TP63, VSX2

miRNA regulators (miRDB)

92 targeting CARM1, 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-4262	100.00	73.26	3931
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-3925-3P	100.00	69.95	1237
HSA-MIR-188-3P	100.00	68.76	1240
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4650-5P	99.98	64.69	999
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-103A-3P	99.98	69.14	1595
HSA-MIR-107	99.98	69.14	1595
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6783-3P	99.89	67.92	2059
HSA-MIR-1343-3P	99.89	66.78	1815
HSA-MIR-548E-5P	99.89	72.73	4486
HSA-LET-7A-2-3P	99.87	70.53	1921
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-4447	99.85	67.81	2900

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 22.5% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• Methylates PAB1 and TARPP, suggesting a role in regulating transcription/translation. (PMID:11850402)
• The CBP/p300 acetylase and the CARM1 methyltransferase can positively regulate the expression of estrogen-responsive genes, there is a crosstalk between lysine acetylation and arginine methylation on chromatin (PMID:12498683)
• CARM1 plays a significant role in promoting the differentiation of early thymocyte progenitors, possibly through its direct action on TARPP. (PMID:15096520)
• overexpression of CARM1 is involved in the development of prostate carcinoma (PMID:15221992)
• results show that CARM1/PRMT4 is a novel transcriptional coactivator of NF-kappaB and functions as a promoter-specific regulator of NF-kappaB recruitment to chromatin (PMID:15616592)
• CARM1 affects pre-mRNA splicing in an isoform-specific manner (PMID:15944154)
• arginine methylation of CBP is required for IFN-gamma induction of MHC-II. A kinetic analysis shows that CIITA, CARM1, and H3-R17 methylation all precede CBP loading on the MHC-II promoter during IFN-gamma treatment. (PMID:16254053)
• CARM1 has a role in signal-dependent control of gluconeogenic key enzyme genes (PMID:16330542)
• CARM1 participates in NF-kappaB-mediated transcription through H3-R17 methylation and support a nonnuclear receptor-associated function for CARM1. (PMID:16497732)
• CARM1 is essential for androgen receptor (AR) function and may play a role in prostate cancer progression. (PMID:16705743)
• Results suggest that members of the SRC coactivator family, such as SRC-3, serve as substrates for the enzymatic coactivator coactivator-associated arginine methyltransferase 1 (CARM1). (PMID:16923966)
• our data provide evidence that CARM1 enhances Tax transactivation of the HTLV-1 LTR through a direct interaction between CARM1 and Tax and this binding promotes methylation of histone H3 (PMID:17005681)
• p/CIP/SRC-3 activity and stability are regulated by CARM1-dependent methylation (PMID:17043108)
• The identification of splicing factors that are methylated by CARM1, and protein-protein interactions that are regulated by CARM1, strongly implicates this enzyme in the regulation of alternative splicing. (PMID:17218272)
• phosphorylation of CARM1 serves as a unique mechanism for inactivating CARM1-regulated estrogen-dependent gene expression (PMID:17640894)
• the N-terminal and the C-terminal end of CARM1 catalytic module contain molecular switches that may determine how CARM1 regulates its biological activities by protein-protein interactions (PMID:17882262)
• CARM1 is a critical factor in the pathway of estrogen-stimulated breast cancer growth downstream of ERA and AIB1and upstream of the cell cycle regulatory transcription factor E2F1. (PMID:18172323)
• These results establish a role for CARM1 as an important regulator of chondrocyte proliferation during embryogenesis. (PMID:19725955)
• The physical interaction of CARM1 and PCAF is likely pivotal for the activation of PCAF in the downstream of CARM1 pathway for inducing myogenin under Tetradecanoylphorbol Acetate -induced differentiation. (PMID:20213728)
• phosphorylation of CARM1 by PKA at a single serine is necessary and sufficient for direct binding to the unliganded hormone-binding domain of ERalpha, and the interaction is necessary for cAMP activation of ERalpha (PMID:20360387)
• CARM1 was particularly overexpressed in colorectal cancers while CARM1 expression was not prevalent in prostate and breast cancers. (PMID:20462455)
• Findings suggest that coexpression of CARM1 and ERalpha may provide a better biomarker of well-differentiated breast cancer. (PMID:21282336)
• Signal transduction in cell death and survival involves a role for CARM1 in arginine methylation. (PMID:21445011)
• A coactivator role of CARM1 in the dysregulation of beta-catenin activity in colorectal cancer cell growth and gene expression (PMID:21478268)
• found that CARM1 facilitates Sox2-mediated transactivation and directly methylates Sox2 at arginine 113 (PMID:22046437)
• Findings indicate that expression of PRMT4/CARM1 and PRMT6 is deregulated in melanoma. (PMID:23265702)
• the miR-181c-CARM1 pathway has an important role in regulating the differentiation of human embryonic stem cells (PMID:23301034)
• Inhibition of CARM1 decreases PELP1 oncogenic activity. (PMID:23486015)
• These findings reveal an important and so far unknown connection between PRMT4 and the chromatin remodeller Mi2 in c-Myb signalling. (PMID:23505388)
• increased cytoplasmic CARM1, relative to nuclear levels, appear to be associated with self-identified African ethnicity and this result is being further investigated using quantified genetic ancestry measures. (PMID:23663560)
• Data show the transcriptional regulation of the human ferritin gene by coordinated regulation of Nrf2 and protein arginine methyltransferases PRMT1 and PRMT4. (PMID:23699174)
• CARM1 represses replicative senescence by methylating HuR. (PMID:23837869)
• CARM1 could be a potential marker of luminal class subclassification and for target therapy, particularly in the ER-positive luminal-like subgroup. (PMID:23887673)
• CARM1 overexpression was associated with poorly characterized clinicopathologic parameters and HER2 overexpression in invasive breast cancer. (PMID:23915145)
• Arginine 42 of histone H3 (H3R42), is dimethylated by the methyltransferases coactivator arginine methyltransferase 1 (CARM1) and protein arginine methyltransferase 6 (PRMT6) in vitro and in vivo. (PMID:23980157)
• CARM1 and PRMT1 are dysregulated in lung cancer; only CARM1 expression was found to be correlated with tumor differentiation and neither CARM1 nor PRMT1 expression was correlated with survival. (PMID:24211191)
• Overexpression of PRMT4 represses miR-223 via methylation of RUNX1 and blocks myeloid differentiation. (PMID:24332853)
• we identify BAF155 as a substrate for arginine methyltransferase CARM1. (PMID:24434208)
• PBMCs from patients with ACS showed higher levels of CARM1 mRNA and protein expression.CARM1 regulated the transcription of IP-10, IL-8, and MCP-1. miR-15a modulated CARM1 expression through targeted binding to CARM1 3’-UTR. (PMID:24530761)
• a noncoding variant in the CARM1-promoter functions as a regulator of gene transcription and homocysteine levels (PMID:25064859)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	carm1	ENSDARG00000018698
mus_musculus	Carm1	ENSMUSG00000032185
rattus_norvegicus	Carm1	ENSRNOG00000031129
drosophila_melanogaster	Art2	FBGN0031592
drosophila_melanogaster	Art4	FBGN0037770

Paralogs (7): PRMT8 (ENSG00000111218), PRMT1 (ENSG00000126457), PRMT7 (ENSG00000132600), PRMT2 (ENSG00000160310), PRMT9 (ENSG00000164169), PRMT3 (ENSG00000185238), PRMT6 (ENSG00000198890)

Protein

Protein identifiers

Histone-arginine methyltransferase CARM1 — Q86X55 (reviewed: Q86X55)

Alternative names: Coactivator-associated arginine methyltransferase 1, Protein arginine N-methyltransferase 4

All UniProt accessions (8): Q86X55, A0AA34QVH5, K7EIQ8, K7EK20, K7EPK1, K7EQA8, K7EQB9, K7ERM3

UniProt curated annotations — full annotation on UniProt →

Function. Methylates (mono- and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in several proteins involved in DNA packaging, transcription regulation, pre-mRNA splicing, and mRNA stability. Recruited to promoters upon gene activation together with histone acetyltransferases from EP300/P300 and p160 families, methylates histone H3 at ‘Arg-17’ (H3R17me), forming mainly asymmetric dimethylarginine (H3R17me2a), leading to activation of transcription via chromatin remodeling. During nuclear hormone receptor activation and TCF7L2/TCF4 activation, acts synergically with EP300/P300 and either one of the p160 histone acetyltransferases NCOA1/SRC1, NCOA2/GRIP1 and NCOA3/ACTR or CTNNB1/beta-catenin to activate transcription. During myogenic transcriptional activation, acts together with NCOA3/ACTR as a coactivator for MEF2C. During monocyte inflammatory stimulation, acts together with EP300/P300 as a coactivator for NF-kappa-B. Acts as a coactivator for PPARG, promotes adipocyte differentiation and the accumulation of brown fat tissue. Plays a role in the regulation of pre-mRNA alternative splicing by methylation of splicing factors. Also seems to be involved in p53/TP53 transcriptional activation. Methylates EP300/P300, both at ‘Arg-2142’, which may loosen its interaction with NCOA2/GRIP1, and at ‘Arg-580’ and ‘Arg-604’ in the KIX domain, which impairs its interaction with CREB and inhibits CREB-dependent transcriptional activation. Also methylates arginine residues in RNA-binding proteins PABPC1, ELAVL1 and ELAV4, which may affect their mRNA-stabilizing properties and the half-life of their target mRNAs. Acts as a transcriptional coactivator of ACACA/acetyl-CoA carboxylase by enriching H3R17 methylation at its promoter, thereby positively regulating fatty acid synthesis. Independently of its methyltransferase activity, involved in replication fork progression: promotes PARP1 recruitment to replication forks, leading to poly-ADP-ribosylation of chromatin at replication forks and reduced fork speed.

Subunit / interactions. Homodimer. Interacts with NR1H4. Interacts with SNRPC. Interacts with the C-terminus of NCOA2/GRIP1, NCO3/ACTR and NCOA1/SRC1. Part of a complex consisting of CARM1, EP300/P300 and NCOA2/GRIP1. Interacts with FLII, TP53, myogenic factor MEF2, EP300/P300, TRIM24, CREBBP and CTNNB1. Interacts with RELA. Identified in a complex containing CARM1, TRIM24 and NCOA2/GRIP1. Interacts with NCOA3/SRC3. Interacts with SKP2. Interacts (via PH domain-like fold) with C9orf72. Interacts with PARP1; promoting PARP1 recruimtent to replication forks. (Microbial infection) Interacts with HTLV-1 protein Tax.

Subcellular location. Nucleus. Cytoplasm. Chromosome.

Tissue specificity. Overexpressed in prostate adenocarcinomas and high-grade prostatic intraepithelial neoplasia.

Post-translational modifications. Auto-methylated on Arg-550. Methylation enhances transcription coactivator activity. Methylation is required for its role in the regulation of pre-mRNA alternative splicing. Phosphorylation at Ser-216 is strongly increased during mitosis, and decreases rapidly to a very low, basal level after entry into the G1 phase of the cell cycle. Phosphorylation at Ser-216 may promote location in the cytosol. Phosphorylation at Ser-216 interferes with S-adenosyl-L-methionine binding and strongly reduces methyltransferase activity. Ubiquitinated by E3 ubiquitin-protein ligase complex containing FBXO9 at Lys-227; leading to proteasomal degradation.

Activity regulation. Methylation of H3R17 (H3R17me) by CARM1 is stimulated by preacetylation of H3 ‘Lys-18’ (H3K18ac) H3 ‘Lys-23’ (H3K23ac) by EP300 and blocked by citrullination of H3 ‘Arg-17’ (H3R17ci) by PADI4.

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

Isoforms (3)

UniProt ID	Names	Canonical?
Q86X55-3	3	yes
Q86X55-1	1
Q86X55-2	2

RefSeq proteins (3): NP_001357017, NP_001357018, NP_954592* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR011993	PH-like_dom_sf	Homologous_superfamily
IPR025799	Arg_MeTrfase	Family
IPR029063	SAM-dependent_MTases_sf	Homologous_superfamily
IPR055135	PRMT_dom	Domain

Pfam: PF06325, PF11531, 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), 1 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)

UniProt features (57 total): helix 15, strand 15, binding site 6, turn 6, modified residue 3, splice variant 3, region of interest 3, mutagenesis site 2, initiator methionine 1, chain 1, cross-link 1, domain 1

Structure

Experimental structures (PDB)

33 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
8G2H	X-RAY DIFFRACTION	1.49
6DVR	X-RAY DIFFRACTION	1.54
8SIG	X-RAY DIFFRACTION	1.78
6S7A	X-RAY DIFFRACTION	1.86
8UQH	X-RAY DIFFRACTION	1.87
5U4X	X-RAY DIFFRACTION	1.88
6ARJ	X-RAY DIFFRACTION	1.92
5DX1	X-RAY DIFFRACTION	1.93
5DX8	X-RAY DIFFRACTION	1.94
5DXJ	X-RAY DIFFRACTION	1.95
9O6H	X-RAY DIFFRACTION	1.97
4IKP	X-RAY DIFFRACTION	2
6ARV	X-RAY DIFFRACTION	2
6D2L	X-RAY DIFFRACTION	2
7U9I	X-RAY DIFFRACTION	2
5DX0	X-RAY DIFFRACTION	2.05
6S71	X-RAY DIFFRACTION	2.06
5DXA	X-RAY DIFFRACTION	2.07
7FAI	X-RAY DIFFRACTION	2.1
2Y1W	X-RAY DIFFRACTION	2.1
6S74	X-RAY DIFFRACTION	2.1
6S79	X-RAY DIFFRACTION	2.1
9O37	X-RAY DIFFRACTION	2.11
6S77	X-RAY DIFFRACTION	2.12
8G2I	X-RAY DIFFRACTION	2.17
7FAJ	X-RAY DIFFRACTION	2.25
6S70	X-RAY DIFFRACTION	2.3
6S7C	X-RAY DIFFRACTION	2.3
8SIH	X-RAY DIFFRACTION	2.35
5DWQ	X-RAY DIFFRACTION	2.36

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q86X55-F1	80.20	0.60

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (6): 243; 271; 159; 168; 192; 214

Post-translational modifications (4): 2, 216, 550, 227

Mutagenesis-validated functional residues (2):

Position	Phenotype
168	loss of protein methyltransferase activity without affecting ability to regulate replication fork progression.
227	loss of fbxo9-mediated ubiquitination and subsequent proteasomal degradation.

Function

Pathways and Gene Ontology

Reactome pathways

36 pathways

ID	Pathway
R-HSA-1368108	BMAL1:CLOCK,NPAS2 activates circadian expression
R-HSA-1989781	PPARA activates gene expression
R-HSA-2151201	Transcriptional activation of mitochondrial biogenesis
R-HSA-2426168	Activation of gene expression by SREBF (SREBP)
R-HSA-3214858	RMTs methylate histone arginines
R-HSA-381340	Transcriptional regulation of white adipocyte differentiation
R-HSA-400206	Regulation of lipid metabolism by PPARalpha
R-HSA-6804114	TP53 Regulates Transcription of Genes Involved in G2 Cell Cycle Arrest
R-HSA-9018519	Estrogen-dependent gene expression
R-HSA-9707564	Cytoprotection by HMOX1
R-HSA-9707616	Heme signaling
R-HSA-9931509	Expression of BMAL (ARNTL), CLOCK, and NPAS2
R-HSA-9933387	RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression
R-HSA-1266738	Developmental Biology
R-HSA-1368082
R-HSA-1430728	Metabolism
R-HSA-1592230	Mitochondrial biogenesis
R-HSA-162582	Signal Transduction
R-HSA-1655829	Regulation of cholesterol biosynthesis by SREBP (SREBF)
R-HSA-1852241	Organelle biogenesis and maintenance
R-HSA-212436	Generic Transcription Pathway
R-HSA-2262752	Cellular responses to stress
R-HSA-3247509	Chromatin modifying enzymes
R-HSA-3700989	Transcriptional Regulation by TP53
R-HSA-400253
R-HSA-4839726	Chromatin organization
R-HSA-556833	Metabolism of lipids
R-HSA-6791312	TP53 Regulates Transcription of Cell Cycle Genes
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 242 (showing top): GOBP_DNA_TEMPLATED_DNA_REPLICATION_MAINTENANCE_OF_FIDELITY, REACTOME_TRANSCRIPTIONAL_REGULATION_OF_WHITE_ADIPOCYTE_DIFFERENTIATION, GOBP_DENDRITE_DEVELOPMENT, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_EPITHELIAL_CELL_APOPTOTIC_PROCESS, TGCTGCT_MIR15A_MIR16_MIR15B_MIR195_MIR424_MIR497, GOBP_CELLULAR_RESPONSE_TO_LIPID, PAL_PRMT5_TARGETS_UP, GOBP_POSITIVE_REGULATION_OF_FAT_CELL_DIFFERENTIATION, STARK_PREFRONTAL_CORTEX_22Q11_DELETION_DN, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_REGULATION_OF_INTRACELLULAR_STEROID_HORMONE_RECEPTOR_SIGNALING_PATHWAY, GOBP_NEUROGENESIS, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION

GO Biological Process (14): chromatin remodeling (GO:0006338), regulation of DNA-templated transcription (GO:0006355), positive regulation of cell population proliferation (GO:0008284), methylation (GO:0032259), regulation of intracellular estrogen receptor signaling pathway (GO:0033146), positive regulation of fat cell differentiation (GO:0045600), positive regulation of transcription by RNA polymerase I (GO:0045943), response to cAMP (GO:0051591), replication fork reversal (GO:0071932), positive regulation of epithelial cell apoptotic process (GO:1904037), negative regulation of dendrite development (GO:2000171), chromatin organization (GO:0006325), apoptotic process (GO:0006915), peptidyl-arginine methylation (GO:0018216)

GO Molecular Function (14): transcription cis-regulatory region binding (GO:0000976), transcription coactivator activity (GO:0003713), beta-catenin binding (GO:0008013), protein methyltransferase activity (GO:0008276), protein-arginine N-methyltransferase activity (GO:0016274), protein-arginine omega-N asymmetric methyltransferase activity (GO:0035242), histone H3R17 methyltransferase activity (GO:0035642), histone methyltransferase activity (GO:0042054), histone H3R2 methyltransferase activity (GO:0070611), DNA-binding transcription factor binding (GO:0140297), protein binding (GO:0005515), methyltransferase activity (GO:0008168), obsolete histone arginine N-methyltransferase activity (GO:0008469), transferase activity (GO:0016740)

GO Cellular Component (6): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), nuclear replication fork (GO:0043596), chromosome (GO:0005694)

Reactome top-level categories

Rollup of top-13 pathways:

Category	Pathways
Circadian clock	3
Regulation of lipid metabolism by PPARalpha	1
Mitochondrial biogenesis	1
Regulation of cholesterol biosynthesis by SREBP (SREBF)	1
Chromatin modifying enzymes	1
Adipogenesis	1
Metabolism of lipids	1
TP53 Regulates Transcription of Cell Cycle Genes	1
ESR-mediated signaling	1
Cellular response to chemical stress	1
Cellular responses to stress	1
Organelle biogenesis and maintenance	1
Metabolism of steroids	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
protein-arginine N-methyltransferase activity	3
cellular anatomical structure	3
positive regulation of DNA-templated transcription	2
protein methyltransferase activity	2
histone H3 methyltransferase activity	2
chromatin organization	1
DNA-templated transcription	1
regulation of gene expression	1
regulation of RNA biosynthetic process	1
cell population proliferation	1
regulation of cell population proliferation	1
positive regulation of cellular process	1
metabolic process	1
estrogen receptor signaling pathway	1
regulation of intracellular steroid hormone receptor signaling pathway	1
fat cell differentiation	1
positive regulation of cell differentiation	1
regulation of fat cell differentiation	1
regulation of transcription by RNA polymerase I	1
transcription by RNA polymerase I	1
response to purine-containing compound	1
response to organophosphorus	1
response to oxygen-containing compound	1
replication fork processing	1
positive regulation of apoptotic process	1
epithelial cell apoptotic process	1
regulation of epithelial cell apoptotic process	1
negative regulation of neuron projection development	1
dendrite development	1
regulation of dendrite development	1
negative regulation of developmental process	1
cellular component organization	1
programmed cell death	1
apoptotic signaling pathway	1
execution phase of apoptosis	1
protein methylation	1
peptidyl-arginine modification	1
transcription regulatory region nucleic acid binding	1
sequence-specific double-stranded DNA binding	1
transcription coregulator activity	1

Protein interactions and networks

STRING

2952 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
CARM1	EP300	Q09472	980
CARM1	NCOA2	Q15596	980
CARM1	APOE	P02649	948
CARM1	NCOA1	Q15788	923
CARM1	PRMT1	Q99873	894
CARM1	NCOA3	Q9Y6Q9	883
CARM1	CREBBP	Q92793	881
CARM1	KAT2B	Q92831	790
CARM1	PRMT3	O60678	790
CARM1	SNRPC	P09234	776
CARM1	TP53	P04637	767
CARM1	EZH2	Q15910	749
CARM1	TDRD3	Q9H7E2	738
CARM1	ELAVL1	Q15717	732
CARM1	H3-4	Q16695	727
CARM1	H3-7	Q5TEC6	727

IntAct

155 interactions, top by confidence:

A	B	Type	Score
RELA	NFKB1	psi-mi:“MI:0914”(association)	0.920
CDK7	ERCC2	psi-mi:“MI:0914”(association)	0.890
CAMK2G	CAMK2D	psi-mi:“MI:0914”(association)	0.810
CLK3	PSME3	psi-mi:“MI:0914”(association)	0.730
EIF4EBP1	EIF4E1B	psi-mi:“MI:0914”(association)	0.670
USE1	NBAS	psi-mi:“MI:0914”(association)	0.640
DPYSL5	DPYSL4	psi-mi:“MI:0914”(association)	0.640
PCYT2	INPPL1	psi-mi:“MI:0914”(association)	0.640
NCOA3	CARM1	psi-mi:“MI:0914”(association)	0.620
NCOA3	CARM1	psi-mi:“MI:0915”(physical association)	0.620
SMARCC1	CARM1	psi-mi:“MI:0213”(methylation reaction)	0.610
SMARCC1	CARM1	psi-mi:“MI:0915”(physical association)	0.610
CARM1	SMARCC1	psi-mi:“MI:0407”(direct interaction)	0.610
CARM1	CEBPB	psi-mi:“MI:0915”(physical association)	0.600
CARM1	CEBPB	psi-mi:“MI:0407”(direct interaction)	0.600
GLI2	KIF7	psi-mi:“MI:0914”(association)	0.570
ORF	EIF3D	psi-mi:“MI:0914”(association)	0.560

BioGRID (473): CARM1 (Affinity Capture-Western), KAT2B (Affinity Capture-Western), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Affinity Capture-MS), CARM1 (Co-fractionation), CARM1 (Co-fractionation), CARM1 (Co-fractionation), CARM1 (Co-fractionation), CTBP1 (Co-fractionation)

ESM2 similar proteins: A0JMF8, A2RSY1, A6QLW9, B1WAV2, B2GV50, O60271, O75069, O77627, P05412, P05627, P0C090, P17325, P22670, P48377, P48378, P48379, P48380, P48381, P56432, Q0V989, Q0V9K5, Q16656, Q32NR3, Q3KR73, Q499B3, Q49GP3, Q4R3I8, Q4R3Z4, Q4V872, Q4VGL6, Q58A65, Q5EAP5, Q5EY87, Q5RDR2, Q5RJA1, Q5TC82, Q62739, Q66IV1, Q6NRE7, Q6NUC6

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

11 interactions.

A	Effect	B	Mechanism
CARM1	up-regulates	PAX7	methylation
CARM1	“up-regulates activity”	SMARCC1	methylation
CARM1	“down-regulates activity”	RUNX1	methylation
CARM1	down-regulates	Differentiation
hsa-mir-223	“down-regulates quantity by repression”	CARM1	“post transcriptional regulation”
CARM1	“down-regulates activity”	MDH1	acetylation
KRAS	“down-regulates activity”	CARM1
MAPK12	“down-regulates activity”	CARM1	phosphorylation
CARM1	up-regulates	MEF2A	methylation
CARM1	“form complex”	MAPK12/CARM1	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 168 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
CD209 (DC-SIGN) signaling	5	21.3×	1e-03
Activation of NF-kappaB in B cells	6	9.7×	7e-03
Downstream TCR signaling	7	7.4×	7e-03

GO biological processes:

GO term	Partners	Fold	FDR
intrinsic apoptotic signaling pathway	6	14.0×	1e-03
mitophagy	6	12.4×	2e-03
negative regulation of translation	7	8.9×	3e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	44
Likely benign	4
Benign	1

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
3248377	NC_000019.9:g.(?10828919)(11222335_?)del	Pathogenic

SpliceAI

2846 predictions. Top by Δscore:

Variant	Effect	Δscore
19:10871920:GCC:G	donor_gain	1.0000
19:10871923:G:GG	donor_gain	1.0000
19:10871927:G:GG	donor_gain	1.0000
19:10904947:GTA:G	acceptor_loss	1.0000
19:10904948:TAGAT:T	acceptor_loss	1.0000
19:10904949:A:AC	acceptor_loss	1.0000
19:10904949:A:AG	acceptor_gain	1.0000
19:10904950:G:GT	acceptor_gain	1.0000
19:10904950:GAT:G	acceptor_gain	1.0000
19:10905073:AACG:A	donor_gain	1.0000
19:10905073:AACGG:A	donor_loss	1.0000
19:10905074:ACG:A	donor_gain	1.0000
19:10905074:ACGGT:A	donor_loss	1.0000
19:10905075:CG:C	donor_gain	1.0000
19:10905076:GG:G	donor_gain	1.0000
19:10905077:G:GG	donor_gain	1.0000
19:10905077:G:T	donor_loss	1.0000
19:10908034:TCCAG:T	acceptor_loss	1.0000
19:10908035:CCA:C	acceptor_loss	1.0000
19:10908036:CA:C	acceptor_loss	1.0000
19:10908037:A:AG	acceptor_gain	1.0000
19:10908037:A:C	acceptor_loss	1.0000
19:10908038:G:GC	acceptor_loss	1.0000
19:10908038:G:GG	acceptor_gain	1.0000
19:10909101:A:AG	acceptor_gain	1.0000
19:10909102:G:GA	acceptor_gain	1.0000
19:10909102:GTT:G	acceptor_gain	1.0000
19:10909102:GTTTT:G	acceptor_gain	1.0000
19:10909205:AAGGT:A	donor_loss	1.0000
19:10909206:AGGT:A	donor_loss	1.0000

AlphaMissense

4004 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
19:10905019:T:C	S97P	1.000
19:10905046:A:C	S106R	1.000
19:10905048:C:A	S106R	1.000
19:10905048:C:G	S106R	1.000
19:10905053:T:C	L108P	1.000
19:10905062:T:C	F111S	1.000
19:10908101:T:C	F137L	1.000
19:10908102:T:C	F137S	1.000
19:10908102:T:G	F137C	1.000
19:10908103:C:A	F137L	1.000
19:10908103:C:G	F137L	1.000
19:10908125:T:C	S145P	1.000
19:10908126:C:T	S145F	1.000
19:10908128:G:C	A146P	1.000
19:10908129:C:A	A146D	1.000
19:10908137:T:C	Y149H	1.000
19:10908137:T:G	Y149D	1.000
19:10908138:A:G	Y149C	1.000
19:10908140:T:A	F150I	1.000
19:10908140:T:C	F150L	1.000
19:10908140:T:G	F150V	1.000
19:10908141:T:C	F150S	1.000
19:10908141:T:G	F150C	1.000
19:10908142:C:A	F150L	1.000
19:10908142:C:G	F150L	1.000
19:10909103:T:A	F152I	1.000
19:10909103:T:C	F152L	1.000
19:10909103:T:G	F152V	1.000
19:10909104:T:C	F152S	1.000
19:10909104:T:G	F152C	1.000

dbSNP variants (sampled 300 via entrez): RS1000004367 (19:10877923 C>T), RS1000022008 (19:10892978 A>C,G), RS1000077821 (19:10881048 C>T), RS1000105798 (19:10918954 T>G), RS1000235539 (19:10880867 A>G), RS1000255921 (19:10888913 CTG>C), RS1000261162 (19:10886485 C>T), RS1000292949 (19:10922976 T>C), RS1000349609 (19:10893773 C>T), RS1000400634 (19:10896127 T>G), RS1000435164 (19:10891476 G>T), RS1000499554 (19:10922280 C>T), RS1000522060 (19:10885492 T>C), RS1000564413 (19:10882223 ACCT>A), RS1000590395 (19:10886759 C>T)

Disease associations

OMIM: gene MIM:603934 | disease phenotypes: MIM:143890

GenCC curated gene-disease

Mondo (2): familial hypercholesterolemia (MONDO:0005439), neurodevelopmental disorder (MONDO:0700092)

Orphanet (0):

HPO phenotypes

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

GWAS associations

5 associations (top):

Study	Trait	p-value
GCST002738_5	Psoriasis	3.000000e-07
GCST003268_37	Psoriasis vulgaris	8.000000e-07
GCST003678_4	C-reactive protein levels or total cholesterol levels (pleiotropy)	3.000000e-08
GCST003679_17	C-reactive protein levels or LDL-cholesterol levels (pleiotropy)	2.000000e-08
GCST005527_36	Psoriasis	3.000000e-17

EFO canonical traits (4, from GWAS)

EFO ID	Trait name
EFO:1001494	psoriasis vulgaris
EFO:0004458	C-reactive protein measurement
EFO:0004574	total cholesterol measurement
EFO:0004611	low density lipoprotein cholesterol measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D065886	Neurodevelopmental Disorders	F03.625

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL5406 (SINGLE PROTEIN), CHEMBL5465233 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 28,373 (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
CHEMBL1214186	SINEFUNGIN	2	2,165
CHEMBL1232461	MOLIBRESIB	2	1,538
CHEMBL6246	ELLAGIC ACID	2	23,148

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 (8 total), top 8:

Ligand	Action	Affinity	Parameter
BIIB021	Inhibition	8.0	pIC50
MS023	Inhibition	7.64	pKi
BMS pyrazole inhibitor 7f	Inhibition	7.4	pIC50
SGC2085	Inhibition	7.3	pIC50
compound 17f [PMID: 19632837]	Inhibition	7.15	pIC50
MS049	Inhibition	7.0	pKd
compound 43 [PMID: 34781683]	Inhibition	5.43	pIC50
iCARM1	Inhibition	4.91	pIC50

Binding affinities (BindingDB)

14 measured of 29 human assays (29 total across all organisms); most potent 14 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
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
1-(methylamino)-3-[3-[5-methyl-4-[[(3R)-oxolan-3-yl]amino]-6-(1H-pyrazol-5-yl)pyrimidin-2-yl]phenoxy]propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
5-[2-[3-[2-hydroxy-3-(methylamino)propoxy]phenyl]-5-methyl-6-[[(3R)-oxolan-3-yl]amino]pyrimidin-4-yl]-5H-pyrimidin-2-one	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
3-[2-[3-[2-hydroxy-3-(methylamino)propoxy]phenyl]-5-methyl-6-[[(3R)-oxolan-3-yl]amino]pyrimidin-4-yl]-3H-pyridin-6-one	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-6-[methyl(oxan-4-yl)amino]pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(1H-imidazol-2-yl)-6-[methyl(oxan-4-yl)amino]pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(1H-imidazol-5-yl)-6-[methyl(oxan-4-yl)amino]pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-chloro-5-[4-(1H-indol-3-yl)-5-methyl-6-[methyl(oxan-4-yl)amino]pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-5-methyl-6-(oxan-4-ylamino)pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(3,5-dimethyl-1H-pyrazol-4-yl)-6-(oxan-4-ylamino)pyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	550 nM	US-10633389: CARM1 inhibitors and uses thereof
1-[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-6-(3,5-dimethyl-1H-pyrazol-4-yl)-5-methylpyrimidin-2-yl]phenoxy]-3-(methylamino)propan-2-ol	IC50	2000 nM	US-10633389: CARM1 inhibitors and uses thereof
3-[2-[3-[2-hydroxy-3-(methylamino)propoxy]phenyl]-5-methyl-6-[[(3R)-oxolan-3-yl]amino]pyrimidin-4-yl]-3H-pyridin-2-one	IC50	2000 nM	US-10633389: CARM1 inhibitors and uses thereof
1-(methylamino)-3-[3-[4-(5-methyl-1H-imidazol-4-yl)-6-[methyl(oxan-4-yl)amino]pyrimidin-2-yl]phenoxy]propan-2-ol	IC50	2000 nM	US-10633389: CARM1 inhibitors and uses thereof

ChEMBL bioactivities

402 potent at pChembl≥5 of 443 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.30	IC50	0.05	nM	CHEMBL4436627
10.15	IC50	0.07	nM	CHEMBL584335
9.92	IC50	0.12	nM	CHEMBL571829
9.59	IC50	0.26	nM	CHEMBL571639
9.39	IC50	0.41	nM	CHEMBL572103
9.19	IC50	0.65	nM	CHEMBL5272699
9.15	IC50	0.7	nM	CHEMBL571431
9.11	IC50	0.78	nM	CHEMBL5270700
9.08	IC50	0.84	nM	CHEMBL572102
9.04	IC50	0.92	nM	CHEMBL5274219
8.96	IC50	1.1	nM	CHEMBL5291238
8.95	IC50	1.13	nM	CHEMBL5271782
8.92	IC50	1.2	nM	CHEMBL5613749
8.92	IC50	1.2	nM	CHEMBL569225
8.79	IC50	1.63	nM	CHEMBL5288947
8.77	IC50	1.7	nM	CHEMBL5559689
8.70	IC50	2	nM	CHEMBL5566004
8.64	IC50	2.3	nM	CHEMBL5283756
8.61	IC50	2.46	nM	CHEMBL5287824
8.55	IC50	2.8	nM	CHEMBL5283866
8.55	IC50	2.8	nM	CHEMBL5559161
8.55	IC50	2.8	nM	CHEMBL5560909
8.55	IC50	2.8	nM	CHEMBL5613744
8.55	IC50	2.8	nM	CHEMBL6103457
8.55	IC50	2.8	nM	ADEMETIONINE
8.54	IC50	2.9	nM	CHEMBL571640
8.53	IC50	2.94	nM	CHEMBL5271800
8.52	IC50	3	nM	CHEMBL5523577
8.52	IC50	3	nM	CHEMBL5564369
8.52	IC50	3	nM	CHEMBL5574920
8.49	IC50	3.2	nM	CHEMBL5173678
8.43	IC50	3.76	nM	CHEMBL5274712
8.43	IC50	3.68	nM	CHEMBL5289496
8.43	IC50	3.7	nM	CHEMBL5266562
8.43	IC50	3.71	nM	CHEMBL5557446
8.42	IC50	3.78	nM	CHEMBL5289683
8.42	IC50	3.84	nM	CHEMBL5284876
8.40	IC50	4	nM	CHEMBL3901808
8.40	IC50	4	nM	CHEMBL5274712
8.37	IC50	4.29	nM	CHEMBL5274541
8.37	IC50	4.24	nM	CHEMBL5268692
8.36	IC50	4.37	nM	CHEMBL5277620
8.34	IC50	4.6	nM	CHEMBL567298
8.30	IC50	5	nM	CHEMBL5569914
8.30	IC50	5.05	nM	CHEMBL5613785
8.30	IC50	5	nM	CHEMBL5631342
8.30	IC50	5.05	nM	CHEMBL5612658
8.29	IC50	5.13	nM	CHEMBL5273938
8.28	IC50	5.2	nM	CHEMBL5279093
8.22	IC50	6	nM	CHEMBL5274712

PubChem BioAssay actives

361 with measured affinity, of 917 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
(2S)-2-amino-N-[[3-[5-[5-(1,3-benzothiazol-7-yl)-1,3,4-oxadiazol-2-yl]-3-(trifluoromethyl)pyrazol-1-yl]phenyl]methyl]propanamide	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	<0.0001	uM
2-[4-[2-(2,6-dimethoxyphenyl)-7-methyl-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0001	uM
2-[4-[2-(2-fluoro-6-methoxyphenyl)-7-methyl-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0001	uM
2-[4-[2-(4-fluoro-2-methoxyphenyl)-7-methyl-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0003	uM
2-[4-[2-(2-methoxyphenyl)-7-methyl-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0004	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-(1,3,5-trimethylpyrazol-4-yl)pyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0006	uM
2-[4-[2-(2-methoxy-3-pyridinyl)-1H-imidazo[4,5-b]pyridin-6-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0007	uM
N’-[[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methyl-6-(4-methylsulfonylpiperazin-1-yl)pyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0008	uM
2-[4-[2-(2-methoxy-3-pyridinyl)-7-methyl-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0008	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-pyridin-3-ylpyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0009	uM
(2R,3R,4S,5S)-2-(6-aminopurin-9-yl)-5-[2-[(3-bromophenyl)methylamino]ethylsulfanylmethyl]oxolane-3,4-diol	2127546: Inhibition of human PRMT4 using histone H3 as substrate and SAM as cofactor by radiometric HotSpot assay	ic50	0.0010	uM
N’-[[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methyl-6-morpholin-4-ylpyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0011	uM
N’-[[3-[4-(5,7-dihydropyrrolo[3,4-b]pyridin-6-yl)-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0011	uM
2-[4-[2-(2-methoxy-3-pyridinyl)-3H-benzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0012	uM
(2R,3R,4S,5S)-2-(6-aminopurin-9-yl)-5-[2-[[3-(furan-3-yl)phenyl]methylamino]ethylsulfanylmethyl]oxolane-3,4-diol	2127546: Inhibition of human PRMT4 using histone H3 as substrate and SAM as cofactor by radiometric HotSpot assay	ic50	0.0012	uM
N’-[[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methyl-6-(oxan-4-ylamino)pyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0016	uM
N’-[[5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl]methyl]-N,N’-dimethylethane-1,2-diamine	2069867: Inhibition of N-terminal FLAG tagged human PRMT4 (2 to end residues) expressed in FreeStyle 293-F cells using SAM and rHistone H3.1 as substrate preincubated for 60 mins followed by substrate addition and measured after 40 mins by Topcount reader based analysis	ic50	0.0017	uM
(2S)-1-[[2-[[3-chloro-4-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl-methylamino]-3-(methylamino)propan-2-ol	2104082: Inhibition of CARM1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0020	uM
4-[5-methyl-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-6-(oxan-4-ylamino)pyrimidin-4-yl]phenol	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0023	uM
N’-[[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-6-(1,1-dioxo-1,4-thiazinan-4-yl)-5-methylpyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0025	uM
(2S)-2-amino-N-[2-[[(2R)-1-amino-4-[[amino-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethylamino]methylidene]amino]-1-oxobutan-2-yl]amino]-2-oxoethyl]-5-(diaminomethylideneamino)pentanamide	1946285: Inhibition of human PRMT4 by fluorescence-based SAHH-coupled assay	ic50	0.0028	uM
(2S)-5-amino-N-[(2R)-1-amino-5-[[N’-[3-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]carbamimidoyl]amino]-1-oxopentan-2-yl]-2-[[2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]pentanamide	2073631: Inhibition of PRMT4 (unknown origin) by HotSpot profiling analysis	ic50	0.0028	uM
(2S)-2-amino-N-[2-[[(2S)-1-amino-4-[[N’-[3-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]carbamimidoyl]amino]-1-oxobutan-2-yl]amino]-2-oxoethyl]-5-(diaminomethylideneamino)pentanamide	2074342: Inhibition of PRMT4 (unknown origin)	ic50	0.0028	uM
(2S)-2-[[(2S)-5-amino-2-[[2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]pentanoyl]amino]-5-[[N’-[3-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]propyl]carbamimidoyl]amino]pentanoic acid	2127546: Inhibition of human PRMT4 using histone H3 as substrate and SAM as cofactor by radiometric HotSpot assay	ic50	0.0028	uM
N-methyl-N’-[[3-[5-methyl-4-(2-methylpyrazol-3-yl)-6-(oxan-4-ylamino)pyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0029	uM
2-[4-[2-(2-methoxy-3-pyridinyl)-1-methylbenzimidazol-5-yl]piperidin-1-yl]-N-methylethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0029	uM
(2R)-1-[3-[4-[2-(azetidin-1-yl)-5,7-dihydropyrrolo[3,4-d]pyrimidin-6-yl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-2-yl]-4-chlorophenoxy]-3-(methylamino)propan-2-ol	2074347: Inhibition of flag-tagged PRMT4 (2 to 585 residues) (unknown origin) expressed in HEK293F cells preincubated for 30 mins followed by biotinylated substrate and SAM addition by Topcount reader assay	ic50	0.0030	uM
(2R)-1-(methylamino)-3-[methyl-[[2-[[3-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]amino]propan-2-ol	2104082: Inhibition of CARM1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0030	uM
N’-[[2-[[3-chloro-4-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2104082: Inhibition of CARM1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0030	uM
methyl 6-[4-[[N’-[(E)-3-[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]prop-2-enyl]carbamimidoyl]amino]butylcarbamoylamino]-4-hydroxynaphthalene-2-carboxylate	1883071: Inhibition of human full length recombinant GST-tagged PRMT4 (2 to 608 residues) using histone H3 as substrate incubated for 20 mins in presence of [3H]-SAM by radioisotope-based filter assay	ic50	0.0032	uM
N’-[[3-[4-anilino-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0037	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-pyridin-4-ylpyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0037	uM
N-hydroxy-7-[3-[[5-methyl-2-[3-[[2-(methylamino)ethylamino]methyl]phenyl]-6-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-4-yl]amino]phenoxy]heptanamide	2069870: Inhibition of human recombinant CARM1 using biotinylated peptide and [3H]SAM as substrates preincubated for 30 mins followed by [3H]SAM addition by Topcount reader based analysis	ic50	0.0037	uM
N’-[[3-[4-(1,3-dimethylpyrazol-4-yl)-5-methyl-6-(oxan-4-ylamino)pyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0038	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-(1H-pyrrolo[2,3-b]pyridin-4-yl)pyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0038	uM
methyl 2-[2-[2-chloro-5-[(2R)-2-hydroxy-3-(methylamino)propoxy]phenyl]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methylpyrimidin-4-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylate	1934144: Inhibition of FLAG-tagged CARM1 (unknown origin) (2 to 585 residues) using biotin-aminohexanoate-PRKQLATKAARMeKSAP-amide peptide as substrate preincubated for 30 mins followed by substrate addition in presence of SAM by topcount reader analysis	ic50	0.0038	uM
N’-methyl-N’-[[4-(4-propan-2-yloxyphenyl)-1H-pyrrol-3-yl]methyl]ethane-1,2-diamine	1319864: Inhibition of human PRMT4 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation proximity assay	ic50	0.0040	uM
N’-[[3-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-5-methyl-6-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0042	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-pyrimidin-5-ylpyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0043	uM
N’-[[3-[4-isoquinolin-5-yl-5-methyl-6-(oxan-4-ylamino)pyrimidin-2-yl]phenyl]methyl]-N-methylethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0044	uM
N-methyl-2-[4-(7-methyl-2-phenyl-3H-benzimidazol-5-yl)piperidin-1-yl]ethanamine	447190: Inhibition of human CARM1 assessed as inhibition of histone3 methylation	ic50	0.0046	uM
N-[(2-methoxyphenyl)methyl]-1-[3-[2-(methylamino)ethylamino]phenyl]-3-(trifluoromethyl)pyrazole-5-carboxamide	2138375: Inhibition of PRMT4 (unknown origin)	ic50	0.0050	uM
2-[2-[[(2S,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]ethyl]-1-(2-bromophenyl)guanidine	2127583: Inhibition of PRMT4 (unknown origin)	ic50	0.0050	uM
(2S)-1-(methylamino)-3-[methyl-[[2-[[3-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]amino]propan-2-ol	2104082: Inhibition of CARM1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0050	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-[4-(trifluoromethoxy)phenyl]pyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0051	uM
N-methyl-N’-[[3-[5-methyl-4-(4-methylsulfonylphenyl)-6-(oxan-4-ylamino)pyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0052	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-quinolin-5-ylpyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0061	uM
N-methyl-N’-[[3-[5-methyl-4-(oxan-4-ylamino)-6-pyridin-2-ylpyrimidin-2-yl]phenyl]methyl]ethane-1,2-diamine	1934145: Inhibition of human CARM1 (140 to 480 residues) incubated for 15 mins measured after 60 min by AlphaLISA assay	ic50	0.0062	uM
N’-[[2-[[3-chloro-4-(1,3-thiazol-2-yl)phenyl]methoxy]phenyl]methyl]-N’-methylethane-1,2-diamine;dihydrochloride	2104082: Inhibition of CARM1 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLISA assay	ic50	0.0070	uM
N’-[[2-[4,4-bis(methoxymethyl)cyclohexyl]oxyphenyl]methyl]-N,N’-dimethylethane-1,2-diamine;dihydrochloride	2069833: Inhibition of CARM1 (unknown origin) using histone H3 (21 to 44 residues) and SAM as substrates by AlphaLISA assay	ic50	0.0070	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects cotreatment, increases expression, decreases expression, decreases reaction, increases reaction (+2 more)	3
Estradiol	decreases reaction, increases expression, affects binding, increases reaction, decreases expression	3
methylmercuric chloride	increases expression, affects cotreatment	2
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	2
Doxorubicin	affects binding, increases reaction, decreases expression	2
bisphenol A	decreases expression	1
arsenite	increases expression, decreases expression, decreases reaction	1
cobaltous chloride	decreases expression	1
ochratoxin A	increases expression	1
benzo(e)pyrene	increases methylation	1
testosterone-3-carboxymethyloxime-bovine serum albumin conjugate	increases expression	1
CGP 52608	affects binding, increases reaction	1
dorsomorphin	affects cotreatment, increases expression	1
LDN 193189	affects cotreatment, increases expression	1
(+)-JQ1 compound	decreases expression	1
Arsenic Trioxide	increases expression	1
Fulvestrant	decreases reaction, increases expression	1
Acetaminophen	decreases expression	1
Cyclic AMP	increases activity, increases reaction, increases expression, affects binding, increases phosphorylation	1
Atrazine	increases expression	1
Vehicle Emissions	increases abundance, increases expression	1
Benzo(a)pyrene	increases expression	1
Cadmium	decreases reaction, increases expression, decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Ethyl Methanesulfonate	decreases expression	1
Ivermectin	decreases expression	1
Lead	affects expression	1
Methapyrilene	increases methylation	1
Methyl Methanesulfonate	decreases expression	1
Ribavirin	affects binding, decreases reaction, decreases expression	1

ChEMBL screening assays

371 unique, capped per target: 363 binding, 8 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1037272	Binding	Inhibition of human CARM1 assessed as inhibition of histone3 methylation	Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)–Hit to Lead studies. — Bioorg Med Chem Lett
CHEMBL5445896	Functional	Affinity Phenotypic Cellular interaction: (Cell viability assay (CellTiter-Glo assay in NCI-H929 cells)) EUB0000230b CARM1	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library

Cellosaurus cell lines

12 cell lines: 8 cancer cell line, 3 embryonic stem cell, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_A0K4	SEES3-1V human CARM1, clone1	Embryonic stem cell	Male
CVCL_A0K5	SEES3-1V human CARM1, clone2	Embryonic stem cell	Male
CVCL_A0K6	SEES3-1V human CARM1, clone3	Embryonic stem cell	Male
CVCL_B2TH	Abcam HEK293T CARM1 KO	Transformed cell line	Female
CVCL_B8CF	Abcam HCT 116 CARM1 KO	Cancer cell line	Male
CVCL_B8TA	Abcam MCF-7 CARM1 KO	Cancer cell line	Female
CVCL_B9EL	Abcam A-549 CARM1 KO	Cancer cell line	Male
CVCL_D7LQ	Ubigene A-549 CARM1 KO	Cancer cell line	Male
CVCL_D8IG	Ubigene HCT 116 CARM1 KO	Cancer cell line	Male
CVCL_SG82	HAP1 CARM1 (-) 1	Cancer cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT00655265	PHASE4	COMPLETED	A Study of the Safety and Efficacy of Patients With Familial Hypercholesterolaemia Taking Colesevelam as add-on Therapy to Their Existing Medication
NCT00916643	PHASE4	COMPLETED	Low-Density Lipoprotein (LDL) Apheresis Using H.E.L.P. Therapy
NCT03331666	PHASE4	TERMINATED	Impact of LDL-cholesterol Lowering on Platelet Activation
NCT05465278	PHASE4	COMPLETED	Alirocumab and Plaque Burden In Familial Hypercholesterolaemia
NCT04586348	PHASE4	UNKNOWN	Prenatal Iodine Supplementation and Early Childhood Neurodevelopment
NCT04873115	PHASE4	UNKNOWN	Double-blind, Placebo-controlled, Randomized Clinical Trial Comparing the Efficacy and Safety of Sialanar Plus orAl rehabiLitation Against Placebo Plus Oral Rehabilitation for chIldren and Adolescents With seVere Sialorrhoea and Neurodisabilties,
NCT00355615	PHASE3	COMPLETED	PLUTO: Pediatric Lipid-redUction Trial of rOsuvastatin
NCT00552097	PHASE3	COMPLETED	Effect of Ezetimibe Plus Simvastatin Versus Simvastatin Alone on Atherosclerosis in the Carotid Artery (ENHANCE)(P02578)
NCT00607373	PHASE3	COMPLETED	Study to Assess the Safety and Efficacy of ISIS 301012 (Mipomersen) in Homozygous Familial Hypercholesterolemia
NCT00694109	PHASE3	COMPLETED	An Open-label Extension Study to Assess the Long-term Safety and Efficacy of ISIS 301012 (Mipomersen) in Patients With Familial Hypercholesterolemia or Severe-Hypercholesterolemia
NCT00827606	PHASE3	COMPLETED	Atorvastatin Three Year Pediatric Study
NCT00943306	PHASE3	COMPLETED	Long Term, Follow-on Study of Lomitapide in Patients With Homozygous Familial Hypercholesterolemia
NCT01524289	PHASE3	COMPLETED	Study to Assess the Tolerability and Efficacy of Anacetrapib (MK-0859) Co-Administered With Statin in Participants With Heterozygous Familial Hypercholesterolemia (MK-0859-020)
NCT01813006	PHASE3	COMPLETED	Effect of Omega-3 Fatty Acid on Endothelial Function
NCT01841684	PHASE3	TERMINATED	Efficacy and Tolerability of Anacetrapib Added to Ongoing Lipid-Lowering Therapy in Adult Participants With Homozygous Familial Hypercholesterolemia (HoFH) (MK-0859-042)
NCT02624869	PHASE3	COMPLETED	Safety, Tolerability and Efficacy of Evolocumab (AMG 145) in Children With Inherited Elevated Low-density Lipoprotein Cholesterol (Familial Hypercholesterolemia)
NCT02748057	PHASE3	COMPLETED	A Clinical Trial to Assess the Long Term Safety and Tolerability of MK-0653H in Japanese Participants With Hypercholesterolemia (MK-0653H-833)
NCT03884452	PHASE3	COMPLETED	Ezetimibe (SCH 58235) Taken With Either Atorvastatin or Simvastatin in Participants With Familial Hypercholesterolemia (MK-0653-018)
NCT04798430	PHASE3	ENROLLING_BY_INVITATION	Long-term Efficacy and Safety of OLE LIB003 in HoFH, HeFH, and High-risk CVD Patients Requiring Further LDL-C Reduction
NCT05142722	PHASE3	COMPLETED	Randomized Study to Evaluate the Effect of Obicetrapib on Top of Maximum Tolerated Lipid-Modifying Therapies
NCT05238519	PHASE3	ACTIVE_NOT_RECRUITING	Improved Diagnosis of Familial Hypercholesterolemia Across the Northland (ID-FH)
NCT05425745	PHASE3	COMPLETED	Evaluate the Effect of Obicetrapib in Patients With HeFH on Top of Maximum Tolerated Lipid-Modifying Therapies.
NCT05952856	PHASE3	COMPLETED	A Study of Enlicitide Decanoate (MK-0616 Oral PCSK9 Inhibitor) in Adults With Hypercholesterolemia (MK-0616-013) CORALreef Lipids
NCT05952869	PHASE3	COMPLETED	A Study of Enlicitide Decanoate (MK-0616 Oral PCSK9 Inhibitor) in Adults With Heterozygous Familial Hypercholesterolemia (MK-0616-017/CORALreef HeFH)
NCT06005597	PHASE3	COMPLETED	Study of Obicetrapib & Ezetimibe Fixed Dose Combination on Top of Maximum Tolerated Lipid-Modifying Therapies
NCT02559102	PHASE3	COMPLETED	Dexmedetomidine Sedation Versus General Anaesthesia for Inguinal Hernia Surgery in Infants
NCT02757079	PHASE3	COMPLETED	Study of the Efficacy and Safety of NPC-15 for Sleep Disorders of Children With Neurodevelopmental Disorders
NCT06915480	PHASE3	RECRUITING	Reducing Missed Appointments
NCT07377032	PHASE3	RECRUITING	TAP-GRIN: Interventional Study on Patients With GRIN-related Neurodevelopmental Disorders
NCT00079846	PHASE2	TERMINATED	Implitapide in Patients With Homozygous Familial Hypercholesterolemia (HoFH) on Maximal Concurrent Lipid-Lowering Therapy
NCT00079859	PHASE2	TERMINATED	Implitapide in Patients With Heterozygous Familial Hypercholesterolemia (HeFH) on Maximal Concurrent Lipid-Lowering Therapy
NCT00477594	PHASE2	COMPLETED	Open Label Extension of ISIS 301012 (Mipomersen) to Treat Familial Hypercholesterolemia
NCT00751608	PHASE2	WITHDRAWN	Effect of APL180 on Endothelial Function in Familial Hypercholesterolemia Patients
NCT02597127	PHASE2	COMPLETED	Trial to Evaluate the Effect of ALN-PCSSC Treatment on Low Density Lipoprotein Cholesterol (LDL-C)
NCT03060577	PHASE2	COMPLETED	An Extension Trial of Inclisiran in Participants With Cardiovascular Disease and High Cholesterol
NCT04455581	PHASE2	UNKNOWN	A Study to Determine the Safety, Tolerability, and Efficacy of SHR-1209 in Patients With Familial Hypercholesterolemia
NCT04941599	PHASE2	RECRUITING	2-Hydroxybenzylamine (2-HOBA) to Reduce HDL Modification and Improve HDL Function in Familial Hypercholesterolemia (FH)
NCT05261126	PHASE2	COMPLETED	A Study of the Efficacy and Safety of Enclitide Chloride (MK-0616 Oral PCSK9 Inhibitor) in Adults With Hypercholesterolemia (MK-0616-008)
NCT02909959	PHASE2	COMPLETED	Sulforaphane for the Treatment of Young Men With Autism Spectrum Disorder
NCT06081348	PHASE2	RECRUITING	Sertraline vs. Placebo in the Treatment of Anxiety in Children and AdoLescents With NeurodevelopMental Disorders