L3MBTL3

Summary

L3MBTL3 (L3MBTL histone methyl-lysine binding protein 3, HGNC:23035) is a protein-coding gene on chromosome 6q23.1, encoding Lethal(3)malignant brain tumor-like protein 3 (Q96JM7). Is a negative regulator of Notch target genes expression, required for RBPJ-mediated transcriptional repression.

This gene encodes a member of the malignant brain tumor (MBT) family of chromatin interacting transcriptional repressors. Members of this family function as methyl-lysine readers, which recognize methylated lysine residues on histone protein tails, and are associated with the repression of gene expression. The encoded protein may regulate hematopoiesis. Homozygous deletion of this gene has been observed in human patients with medulloblastoma.

Source: NCBI Gene 84456 — RefSeq curated summary.

At a glance

• GWAS associations: 92
• Clinical variants (ClinVar): 121 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_032438

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23035
Approved symbol	L3MBTL3
Name	L3MBTL histone methyl-lysine binding protein 3
Location	6q23.1
Locus type	gene with protein product
Status	Approved
Aliases	KIAA1798
Ensembl gene	ENSG00000198945
Ensembl biotype	protein_coding
OMIM	618844
Entrez	84456

Gene structure

Transcript identifiers

Ensembl transcripts: 24 — 22 protein_coding, 2 retained_intron

ENST00000361794, ENST00000368136, ENST00000368139, ENST00000526019, ENST00000526087, ENST00000528385, ENST00000531313, ENST00000533560, ENST00000533890, ENST00000674039, ENST00000858923, ENST00000858924, ENST00000858925, ENST00000858926, ENST00000858927, ENST00000858928, ENST00000858929, ENST00000858930, ENST00000858931, ENST00000858932, ENST00000858933, ENST00000858934, ENST00000966136, ENST00000966137

RefSeq mRNA: 4 — MANE Select: NM_032438 NM_001007102, NM_001346550, NM_001346551, NM_032438

CCDS: CCDS34537, CCDS34538

Canonical transcript exons

ENST00000361794 — 23 exons

Exon	Start	End
ENSE00000975595	130049282	130049393
ENSE00000975596	130051249	130051408
ENSE00000975597	130052859	130052991
ENSE00000975598	130055171	130055255
ENSE00001084666	130049756	130049830
ENSE00001409294	130022227	130022305
ENSE00001411632	130042685	130042801
ENSE00001427560	130139610	130141438
ENSE00003459377	130133452	130133621
ENSE00003475057	130066353	130066488
ENSE00003476175	130078558	130078634
ENSE00003497801	130083620	130083705
ENSE00003513360	130060036	130060140
ENSE00003518768	130068330	130068421
ENSE00003520949	130070976	130071127
ENSE00003523957	130092745	130092859
ENSE00003529613	130104426	130104575
ENSE00003609961	130094265	130094367
ENSE00003626157	130086140	130086250
ENSE00003648718	130133843	130133905
ENSE00003677658	130057406	130057497
ENSE00003693197	130120879	130120958
ENSE00003897320	130018581	130018664

Expression profiles

Bgee: expression breadth ubiquitous, 213 present calls, max score 90.78.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 8.6047 / max 186.5970, expressed in 1600 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
69749	8.2515	1594
69750	0.3532	142

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	90.78	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	90.01	gold quality
stromal cell of endometrium	CL:0002255	88.54	gold quality
sural nerve	UBERON:0015488	85.43	gold quality
right adrenal gland cortex	UBERON:0035827	85.33	gold quality
monocyte	CL:0000576	84.90	gold quality
leukocyte	CL:0000738	84.68	gold quality
secondary oocyte	CL:0000655	84.11	gold quality
right adrenal gland	UBERON:0001233	83.90	gold quality
left adrenal gland	UBERON:0001234	83.74	gold quality
vermiform appendix	UBERON:0001154	83.68	gold quality
cortical plate	UBERON:0005343	83.62	gold quality
left adrenal gland cortex	UBERON:0035825	83.58	gold quality
adrenal gland	UBERON:0002369	83.00	gold quality
adrenal cortex	UBERON:0001235	82.88	gold quality
adrenal tissue	UBERON:0018303	82.84	gold quality
bone marrow cell	CL:0002092	82.74	gold quality
tibia	UBERON:0000979	81.85	gold quality
colonic epithelium	UBERON:0000397	81.05	gold quality
endocervix	UBERON:0000458	80.69	gold quality
smooth muscle tissue	UBERON:0001135	80.61	gold quality
spleen	UBERON:0002106	80.35	gold quality
lymph node	UBERON:0000029	79.84	gold quality
body of uterus	UBERON:0009853	79.36	gold quality
ganglionic eminence	UBERON:0004023	79.10	gold quality
blood	UBERON:0000178	79.06	gold quality
left ovary	UBERON:0002119	78.94	gold quality
right coronary artery	UBERON:0001625	78.79	gold quality
ventricular zone	UBERON:0003053	78.23	gold quality
ovary	UBERON:0000992	78.16	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	6.69

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

133 targeting L3MBTL3, 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-190A-3P	100.00	80.35	5520
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-4803	99.98	71.99	3117
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-8075	99.97	67.20	962
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548Y	99.94	71.28	3514
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AR-5P	99.94	71.28	3515

Literature-anchored findings (GeneRIF, showing 9)

• The mouse MBT-1 protein influences myelopoiesis by transiently enhancing p57(KIP2) expression levels. (PMID:15889154)
• Mutation in L3MBTL3 gene is associated with insulin-resistant cardiometabolic disease. (PMID:27841877)
• RBPJ interacts with L3MBTL3 to promote repression of Notch signaling via histone demethylase KDM1A. (PMID:29030483)
• The direct binding of L3MBTL3 to the methylated SOX2 protein leads to the recruitment of the CRL4(DCAF5) ubiquitin E3 ligase to target SOX2 protein for ubiquitin-dependent proteolysis. (PMID:30442713)
• L3MBTL3 rs4364506 was found neither as a predisposing nor a protective variant against multiple sclerosis (PMID:30456721)
• Effect of L3MBTL3/PTPN9 polymorphisms on risk to alcohol-induced ONFH in Chinese Han population. (PMID:34373992)
• Identification of the genetic mechanism that associates L3MBTL3 to multiple sclerosis. (PMID:35088080)
• The structure, binding and function of a Notch transcription complex involving RBPJ and the epigenetic reader protein L3MBTL3. (PMID:36477367)
• Association of the L3MBTL3 rs1125970 and rs4897367 Gene Polymorphisms With Coronary Heart Disease Susceptibility in the Chinese Population: A Case-Control Study. (PMID:37523690)

Cross-species orthologs

8 orthologs

Organism	Symbol	Gene ID
danio_rerio	l3mbtl3	ENSDARG00000025983
mus_musculus	L3mbtl3	ENSMUSG00000039089
rattus_norvegicus	L3mbtl3	ENSRNOG00000011720
drosophila_melanogaster	l(3)mbt	FBGN0002441
drosophila_melanogaster	Scm	FBGN0003334
drosophila_melanogaster	Sfmbt	FBGN0032475
caenorhabditis_elegans	lin-61	WBGENE00003041
caenorhabditis_elegans	mbtr-1	WBGENE00021661

Paralogs (18): SCMH1 (ENSG00000010803), MBTD1 (ENSG00000011258), SCML1 (ENSG00000047634), L3MBTL2 (ENSG00000100395), SCML2 (ENSG00000102098), PHC1 (ENSG00000111752), THAP10 (ENSG00000129028), PHC2 (ENSG00000134686), SAMD1 (ENSG00000141858), SCML4 (ENSG00000146285), L3MBTL4 (ENSG00000154655), SFMBT1 (ENSG00000163935), PHC3 (ENSG00000173889), L3MBTL1 (ENSG00000185513), SAMD7 (ENSG00000187033), SAMD11 (ENSG00000187634), SFMBT2 (ENSG00000198879), SAMD13 (ENSG00000203943)

Protein

Protein identifiers

Lethal(3)malignant brain tumor-like protein 3 — Q96JM7 (reviewed: Q96JM7)

Alternative names: MBT-1

All UniProt accessions (4): Q96JM7, A0A669KAX0, E9PI01, E9PLL7

UniProt curated annotations — full annotation on UniProt →

Function. Is a negative regulator of Notch target genes expression, required for RBPJ-mediated transcriptional repression. It recruits KDM1A to Notch-responsive elements and promotes KDM1A-mediated H3K4me demethylation. Involved in the regulation of ubiquitin-dependent degradation of a set of methylated non-histone proteins, including SOX2, DNMT1 and E2F1. It acts as an adapter recruiting the CRL4-DCAF5 E3 ubiquitin ligase complex to methylated target proteins. Required for normal maturation of myeloid progenitor cells.

Subunit / interactions. Interacts with RNF2. Interacts (via SAM domain) with SAMD1 (via SAM domain); the interaction mediates L3MBTL3 binding to chromatin. Interacts with RBPJ; the interaction is required for L3MBTL3 localization to chromatin and is impaired by Notch-derived peptides containing the intracellular domain (NICD). Interacts (via SAM domain) with KDM1A. Interacts with DCAF5. Interacts with DNMT1. Interacts with E2F1. Interacts with SOX2. Interacts with SFMBT1.

Subcellular location. Nucleus.

Isoforms (2)

UniProt ID	Names	Canonical?
Q96JM7-1	1	yes
Q96JM7-2	2

RefSeq proteins (4): NP_001007103, NP_001333479, NP_001333480, NP_115814* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001660	SAM	Domain
IPR002515	Znf_C2H2C	Repeat
IPR004092	Mbt	Domain
IPR013761	SAM/pointed_sf	Homologous_superfamily
IPR050548	PcG_chromatin_remod_factors	Family

Pfam: PF00536, PF02820

UniProt features (59 total): helix 20, strand 16, turn 4, region of interest 4, repeat 3, compositionally biased region 3, cross-link 2, chain 1, modified residue 1, splice variant 1, sequence variant 1, mutagenesis site 1, domain 1, zinc finger region 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
8Y77	X-RAY DIFFRACTION	1.5
8Y76	X-RAY DIFFRACTION	1.99
3UT1	X-RAY DIFFRACTION	2.05
7RTI	X-RAY DIFFRACTION	2.05
7RTE	X-RAY DIFFRACTION	2.06
4L59	X-RAY DIFFRACTION	2.29
4FL6	X-RAY DIFFRACTION	2.55
1WJQ	SOLUTION NMR
1WJS	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96JM7-F1	72.73	0.43

Functional residue map

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

Post-translational modifications (3): 608, 637, 704

Mutagenesis-validated functional residues (1):

Position	Phenotype
381	loss of interaction with dnmt1.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 191 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GOBP_MYELOID_CELL_HOMEOSTASIS, GOBP_MYELOID_CELL_DEVELOPMENT, TGCACTT_MIR519C_MIR519B_MIR519A, GOBP_ERYTHROCYTE_HOMEOSTASIS, GOBP_MACROMOLECULE_CATABOLIC_PROCESS, GOBP_MYELOID_LEUKOCYTE_DIFFERENTIATION, CACCAGC_MIR138, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, GOBP_ANATOMICAL_STRUCTURE_MATURATION, GOBP_REGULATION_OF_CATABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_CATABOLIC_PROCESS, GOBP_CELL_MATURATION, GOBP_ERYTHROCYTE_MATURATION, SCHAEFFER_PROSTATE_DEVELOPMENT_6HR_DN

GO Biological Process (10): chromatin organization (GO:0006325), macrophage differentiation (GO:0030225), granulocyte differentiation (GO:0030851), erythrocyte maturation (GO:0043249), negative regulation of DNA-templated transcription (GO:0045892), negative regulation of transcription initiation-coupled chromatin remodeling (GO:0160217), positive regulation of ubiquitin-dependent protein catabolic process (GO:2000060), regulation of DNA-templated transcription (GO:0006355), myeloid cell differentiation (GO:0030099), regulation of ubiquitin-dependent protein catabolic process (GO:2000058)

GO Molecular Function (7): chromatin binding (GO:0003682), zinc ion binding (GO:0008270), histone binding (GO:0042393), identical protein binding (GO:0042802), methylation-dependent protein binding (GO:0140034), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (3): nucleus (GO:0005634), nucleoplasm (GO:0005654), nucleolus (GO:0005730)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
myeloid leukocyte differentiation	2
DNA-templated transcription	2
regulation of gene expression	2
ubiquitin-dependent protein catabolic process	2
binding	2
protein binding	2
nuclear lumen	2
cellular component organization	1
mononuclear cell differentiation	1
cell maturation	1
erythrocyte development	1
regulation of DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
transcription initiation-coupled chromatin remodeling	1
negative regulation of chromatin organization	1
positive regulation of protein catabolic process	1
regulation of ubiquitin-dependent protein catabolic process	1
regulation of RNA biosynthetic process	1
hemopoiesis	1
cell differentiation	1
regulation of protein catabolic process	1
transition metal ion binding	1
modification-dependent protein binding	1
cation binding	1
intracellular membrane-bounded organelle	1
cellular anatomical structure	1
intracellular membraneless organelle	1

Protein interactions and networks

STRING

792 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
L3MBTL3	BCLAF1	Q9NYF8	724
L3MBTL3	DCAF5	Q96JK2	719
L3MBTL3	RNF2	Q99496	579
L3MBTL3	MAML1	Q92585	549
L3MBTL3	BMI1	P35226	515
L3MBTL3	PHF20L1	A8MW92	511
L3MBTL3	R4GMX3	R4GMX3	510
L3MBTL3	RBPJ	Q06330	500
L3MBTL3	DNMT1	P26358	495
L3MBTL3	SFMBT1	Q9UHJ3	475
L3MBTL3	NOTCH2	Q04721	411
L3MBTL3	NCOR1	O75376	407
L3MBTL3	ZNF404	Q494X3	398
L3MBTL3	L3MBTL1	Q9Y468	386
L3MBTL3	MSL3	Q8N5Y2	385

IntAct

156 interactions, top by confidence:

A	B	Type	Score
PHC2	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.670
L3MBTL3	BANP	psi-mi:“MI:0915”(physical association)	0.670
L3MBTL3	PHC2	psi-mi:“MI:0915”(physical association)	0.670
L3MBTL3	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.670
BANP	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.670
L3MBTL3	DNMT1	psi-mi:“MI:0915”(physical association)	0.670
DNMT1	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.670
DNMT1	L3MBTL3	psi-mi:“MI:0407”(direct interaction)	0.670
L3MBTL3	DNMT1	psi-mi:“MI:0914”(association)	0.670
L3MBTL3	SAMD13	psi-mi:“MI:0914”(association)	0.640
E2F1	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.590
L3MBTL3	E2F1	psi-mi:“MI:0915”(physical association)	0.590
DCAF5	L3MBTL3	psi-mi:“MI:0915”(physical association)	0.580
L3MBTL3	DCAF5	psi-mi:“MI:0915”(physical association)	0.580
L3MBTL3	THRA	psi-mi:“MI:0915”(physical association)	0.560

BioGRID (179): L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid), L3MBTL3 (Two-hybrid)

ESM2 similar proteins: A0SQM0, A8WP66, B1H2Q2, B2D6M2, G5ECC7, G5EDT1, O17514, O17828, O62301, O75164, P0C5E7, P34344, P34607, Q09291, Q09293, Q10122, Q11193, Q17388, Q20500, Q21209, Q21988, Q22670, Q23541, Q24592, Q28Z18, Q32KD2, Q4IEV4, Q4R381, Q5RD88, Q5U595, Q5VVW2, Q61T02, Q621Q3, Q6C710, Q6FPH9, Q6NUB7, Q75BY2, Q86ME2, Q8BW72, Q8IQA2

Diamond homologs: A2A5N8, B1B1A0, D3YUG0, D3YXK1, D3ZWK4, E1C2V1, O02274, O60284, O95251, P39769, P59178, P70047, P70475, P78364, P97500, Q01538, Q05BQ5, Q1JQD9, Q1RNF8, Q29L50, Q32N90, Q3MIF2, Q4V7W5, Q5DTW2, Q5R737, Q5SVQ0, Q5VUG0, Q5VXD3, Q64028, Q6DIN3, Q6P5G3, Q6SPE9, Q6SPF0, Q7Z3H4, Q80TY4, Q810T5, Q8BLB7, Q8C8Y5, Q8CFC2, Q8CHP6

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 104 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
Negative Regulation of CDH1 Gene Transcription	7	11.7×	4e-04
ERCC6 (CSB) and EHMT2 (G9a) positively regulate rRNA expression	5	10.6×	5e-03
Pre-NOTCH Transcription and Translation	6	10.2×	2e-03
NoRC negatively regulates rRNA expression	7	10.2×	7e-04
Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)	5	10.2×	5e-03
Oxidative Stress Induced Senescence	8	10.1×	3e-04
HDACs deacetylate histones	6	10.0×	2e-03
NuRD complex assembly	5	9.8×	6e-03

GO biological processes:

GO term	Partners	Fold	FDR
regulation of circadian rhythm	5	13.7×	3e-03
rhythmic process	5	13.2×	3e-03
glucose homeostasis	6	8.2×	5e-03
chromatin organization	7	7.3×	3e-03
transcription by RNA polymerase II	9	6.7×	7e-04
chromatin remodeling	8	6.1×	3e-03
positive regulation of gene expression	13	5.3×	2e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	96
Likely benign	2
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

4105 predictions. Top by Δscore:

Variant	Effect	Δscore
6:130016225:GATA:G	acceptor_gain	1.0000
6:130022214:A:AG	acceptor_gain	1.0000
6:130022215:A:G	acceptor_gain	1.0000
6:130022216:A:AG	acceptor_gain	1.0000
6:130022217:C:G	acceptor_gain	1.0000
6:130022219:A:AG	acceptor_gain	1.0000
6:130022219:AAT:A	acceptor_gain	1.0000
6:130022220:A:G	acceptor_gain	1.0000
6:130022221:T:TA	acceptor_gain	1.0000
6:130022222:GCTA:G	acceptor_loss	1.0000
6:130022224:TAG:T	acceptor_loss	1.0000
6:130022225:A:AG	acceptor_gain	1.0000
6:130022225:A:AT	acceptor_loss	1.0000
6:130022226:G:GG	acceptor_gain	1.0000
6:130022226:G:T	acceptor_loss	1.0000
6:130022226:GA:G	acceptor_gain	1.0000
6:130022303:AAGGT:A	donor_loss	1.0000
6:130022305:GGT:G	donor_loss	1.0000
6:130022306:G:GA	donor_loss	1.0000
6:130022307:T:G	donor_loss	1.0000
6:130042681:TCAGG:T	acceptor_loss	1.0000
6:130042682:CAGGT:C	acceptor_loss	1.0000
6:130042683:A:AC	acceptor_loss	1.0000
6:130042683:A:AG	acceptor_gain	1.0000
6:130042683:AG:A	acceptor_gain	1.0000
6:130042684:G:GA	acceptor_gain	1.0000
6:130042684:GG:G	acceptor_gain	1.0000
6:130042684:GGTT:G	acceptor_gain	1.0000
6:130042684:GGTTA:G	acceptor_gain	1.0000
6:130042788:G:GT	donor_gain	1.0000

AlphaMissense

5198 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
6:130042760:T:A	W21R	1.000
6:130042760:T:C	W21R	1.000
6:130042761:G:C	W21S	1.000
6:130042762:G:C	W21C	1.000
6:130042762:G:T	W21C	1.000
6:130042776:G:A	G26D	1.000
6:130042782:T:C	L28S	1.000
6:130049282:T:C	F35L	1.000
6:130049283:T:C	F35S	1.000
6:130049284:T:A	F35L	1.000
6:130049284:T:G	F35L	1.000
6:130060133:T:A	V286D	1.000
6:130068353:T:A	W342R	1.000
6:130068353:T:C	W342R	1.000
6:130068390:C:A	A354D	1.000
6:130071013:T:C	L377P	1.000
6:130083646:T:A	W450R	1.000
6:130083646:T:C	W450R	1.000
6:130083648:G:C	W450C	1.000
6:130083648:G:T	W450C	1.000
6:130083683:C:A	A462D	1.000
6:130133607:T:A	W708R	1.000
6:130133607:T:C	W708R	1.000
6:130133608:G:C	W708S	1.000
6:130133609:G:C	W708C	1.000
6:130133609:G:T	W708C	1.000
6:130133852:T:C	F716L	1.000
6:130133853:T:C	F716S	1.000
6:130133854:T:A	F716L	1.000
6:130133854:T:G	F716L	1.000

dbSNP variants (sampled 300 via entrez): RS1000015997 (6:130019068 G>A,C,T), RS1000020125 (6:130072557 TAC>T), RS1000050296 (6:130098925 G>A), RS1000089962 (6:130026909 A>G), RS1000091294 (6:130075181 A>T), RS1000115279 (6:130114325 A>G), RS1000143116 (6:130051808 A>G), RS1000160988 (6:130107756 C>T), RS1000165063 (6:130123948 G>A), RS1000203675 (6:130066719 A>C,G), RS1000214386 (6:130108002 A>G), RS1000224869 (6:130126895 G>A), RS1000243569 (6:130097405 A>G), RS1000277048 (6:130127271 G>A), RS1000293735 (6:130021167 A>C)

Disease associations

OMIM: gene MIM:618844 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

92 associations (top):

Study	Trait	p-value
GCST000175_31	Height	6.000000e-06
GCST000817_44	Height	1.000000e-21
GCST001956_61	Height	5.000000e-13
GCST002647_60	Height	3.000000e-36
GCST002702_57	Height	1.000000e-24
GCST002783_149	Body mass index	3.000000e-06
GCST002783_202	Body mass index	2.000000e-06
GCST002783_607	Body mass index	5.000000e-06
GCST003124_14	Mild influenza (H1N1) infection	3.000000e-12
GCST003125_2	Influenza A (H1N1) infection	3.000000e-08
GCST003566_1	Multiple sclerosis	2.000000e-06
GCST004066_36	Hip circumference	1.000000e-09
GCST004066_89	Hip circumference	7.000000e-12
GCST004067_116	Hip circumference adjusted for BMI	7.000000e-13
GCST004067_154	Hip circumference adjusted for BMI	5.000000e-09
GCST004067_47	Hip circumference adjusted for BMI	2.000000e-06
GCST004604_114	Hematocrit	2.000000e-09
GCST004627_33	Lymphocyte count	2.000000e-10
GCST004988_665	Breast cancer	3.000000e-12
GCST005076_13	Breast cancer (estrogen-receptor negative)	4.000000e-08
GCST005077_2	Breast cancer	8.000000e-10
GCST005146_18	Birth weight	4.000000e-11
GCST006288_460	Heel bone mineral density	4.000000e-10
GCST006288_556	Heel bone mineral density	4.000000e-14
GCST006291_73	Spherical equivalent or myopia (age of diagnosis)	5.000000e-10
GCST006979_388	Heel bone mineral density	2.000000e-14
GCST006979_389	Heel bone mineral density	5.000000e-15
GCST007614_45	C-reactive protein levels	2.000000e-11
GCST007615_22	C-reactive protein levels	1.000000e-08
GCST008058_120	Estimated glomerular filtration rate	8.000000e-17

EFO canonical traits (25, from GWAS)

EFO ID	Trait name
EFO:0004340	body mass index
EFO:1001488	influenza A (H1N1)
EFO:0008039	BMI-adjusted hip circumference
EFO:0004348	hematocrit
EFO:0004587	lymphocyte count
EFO:0004344	birth weight
EFO:0009270	heel bone mineral density
EFO:0004847	age at onset
EFO:0004458	C-reactive protein measurement
EFO:0004338	body weight
EFO:0005939	parental genotype effect measurement
EFO:0004509	hemoglobin measurement
EFO:0004530	triglyceride measurement
EFO:0004611	low density lipoprotein cholesterol measurement
EFO:0004615	apolipoprotein B measurement
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0007789	BMI-adjusted waist circumference
EFO:0004980	appendicular lean mass
EFO:0005090	basophil count
EFO:0007992	basophil percentage of leukocytes
EFO:0007986	reticulocyte count
EFO:0004305	erythrocyte count
EFO:0004736	aspartate aminotransferase measurement
EFO:0004533	alkaline phosphatase measurement
EFO:0004532	serum gamma-glutamyl transferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1287623 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 40,315 (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
CHEMBL505	CHLORPHENIRAMINE	4	40,315

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Methyllysine reader proteins

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
UNC1215	Agonist	6.92	pKd

ChEMBL bioactivities

171 potent at pChembl≥5 of 186 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.62	IC50	24	nM	CHEMBL2426364
7.43	IC50	37	nM	CHEMBL3134130
7.41	IC50	39	nM	CHEMBL2426365
7.40	IC50	40	nM	CHEMBL2426364
7.37	IC50	43	nM	CHEMBL2426360
7.32	IC50	48	nM	CHEMBL2426366
7.32	IC50	48	nM	CHEMBL2426498
7.32	IC50	48	nM	CHEMBL3134144
7.31	IC50	49	nM	CHEMBL2426364
7.30	IC50	50	nM	CHEMBL2426365
7.30	IC50	50	nM	CHEMBL2426364
7.29	IC50	51	nM	CHEMBL2426366
7.28	IC50	53	nM	CHEMBL2426367
7.24	IC50	58	nM	CHEMBL2426367
7.23	IC50	59	nM	CHEMBL3134146
7.21	IC50	61	nM	CHEMBL2426368
7.21	IC50	61	nM	CHEMBL2424678
7.21	IC50	62	nM	CHEMBL3134131
7.19	IC50	64	nM	CHEMBL2426364
7.18	IC50	66	nM	CHEMBL2426368
7.17	IC50	68	nM	CHEMBL2426363
7.16	IC50	70	nM	CHEMBL3134134
7.15	IC50	71	nM	CHEMBL2426498
7.14	IC50	72	nM	CHEMBL2426360
7.13	IC50	74	nM	CHEMBL2426476
7.13	IC50	74	nM	CHEMBL2426496
7.10	IC50	80	nM	CHEMBL3134126
7.09	IC50	81	nM	CHEMBL2426489
7.06	IC50	88	nM	CHEMBL2426477
7.04	IC50	92	nM	CHEMBL2426495
7.04	IC50	92	nM	CHEMBL2426490
7.02	IC50	96	nM	CHEMBL2426363
7.02	IC50	96	nM	CHEMBL2426496
7.01	IC50	97	nM	CHEMBL2426481
7.00	IC50	99	nM	CHEMBL2426481
7.00	IC50	100	nM	CHEMBL3134125
6.96	IC50	110	nM	CHEMBL2424678
6.96	IC50	110	nM	CHEMBL2426469
6.96	IC50	110	nM	CHEMBL2426480
6.92	IC50	120	nM	CHEMBL2426476
6.92	IC50	120	nM	CHEMBL2426490
6.92	IC50	120	nM	CHEMBL2426480
6.92	Kd	120	nM	CHEMBL2426364
6.92	IC50	120	nM	CHEMBL3134136
6.92	IC50	120	nM	CHEMBL3134135
6.89	IC50	130	nM	CHEMBL2424677
6.89	IC50	130	nM	CHEMBL2426358
6.89	IC50	130	nM	CHEMBL2426483
6.85	IC50	140	nM	CHEMBL2426489
6.85	IC50	140	nM	CHEMBL2426483

PubChem BioAssay actives

156 with measured affinity, of 249 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
[3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0240	uM
1-[3-chloro-4-(2-pyrrolidin-1-ylethyl)phenyl]-4-pyrrolidin-1-ylpiperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0370	uM
[3-(benzylamino)-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771620: Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay	ic50	0.0390	uM
[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)naphthalen-1-yl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0430	uM
[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0480	uM
[3-benzyl-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771620: Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay	ic50	0.0480	uM
1-[4-[2-(azetidin-1-yl)ethyl]phenyl]-4-pyrrolidin-1-ylpiperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0480	uM
[3-phenoxy-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0530	uM
[3-(hydroxymethyl)-1-[2-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]ethyl]azetidin-3-yl]methanol	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0590	uM
[3-phenyl-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0610	uM
[6-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)-3-pyridinyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0610	uM
4-pyrrolidin-1-yl-1-[4-(2-pyrrolidin-1-ylethyl)phenyl]piperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0620	uM
[5-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)thiophen-2-yl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0680	uM
4-pyrrolidin-1-yl-1-[4-(3-pyrrolidin-1-ylpropyl)phenyl]piperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0700	uM
(4-pyrrolidin-1-ylazepan-1-yl)-[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0740	uM
[3-bromo-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0740	uM
1-[4-(2-piperidin-1-ylethyl)phenyl]-4-pyrrolidin-1-ylpiperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.0800	uM
[4-[4-(1-methylpyrrolidin-1-ium-1-yl)piperidine-1-carbonyl]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0810	uM
[3-nitro-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0880	uM
[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-2-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0920	uM
[4-(8-pyrrolidin-1-yl-3-azabicyclo[3.2.1]octane-3-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0920	uM
(4-pyrrolidin-1-ylpiperidin-1-yl)-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)sulfonylphenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.0970	uM
1-[2-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]ethyl]azepane	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.1000	uM
[3,4-bis(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1100	uM
[4-(4-pyrrolidin-1-ylazepane-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylazepan-1-yl)methanone	771620: Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay	ic50	0.1100	uM
4-pyrrolidin-1-yl-1-[3-(2-pyrrolidin-1-ylethyl)phenyl]piperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.1200	uM
4-pyrrolidin-1-yl-1-[3-(pyrrolidin-1-ylmethyl)phenyl]piperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.1200	uM
3-anilino-N-(2-ethyl-1,3-dihydroisoindol-5-yl)-4-(4-pyrrolidin-2-ylpiperidine-1-carbonyl)benzamide	771620: Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay	ic50	0.1300	uM
(4-pyrrolidin-1-ylpiperidin-1-yl)-[4-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1300	uM
(4-pyrrolidin-1-ylpiperidin-1-yl)-[2,3,5,6-tetrafluoro-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1300	uM
(4-pyrrolidin-1-ylpiperidin-1-yl)-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1500	uM
N-(2-ethyl-1,3-dihydroisoindol-5-yl)-4-(8-pyrrolidin-1-yl-3-azabicyclo[3.2.1]octane-3-carbonyl)benzamide	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1500	uM
2-anilino-N-(2-ethyl-1,3-dihydroisoindol-5-yl)-4-(4-pyrrolidin-2-ylpiperidine-1-carbonyl)benzamide	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1600	uM
N-(2-ethyl-1,3-dihydroisoindol-5-yl)-4-(4-pyrrolidin-2-ylpiperidine-1-carbonyl)benzamide	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1600	uM
(4-piperidin-1-ylpiperidin-1-yl)-[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1600	uM
[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.1800	uM
[4-(azepan-1-yl)piperidin-1-yl]-[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2100	uM
[2,5-dimethyl-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771620: Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay	ic50	0.2100	uM
(4-pyrrolidin-1-ylpiperidin-1-yl)-[4-(3-pyrrolidin-1-ylpyrrolidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2200	uM
[3-amino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2200	uM
[4-[1-(4-methylpiperazin-1-yl)ethyl]piperidin-1-yl]-[4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2500	uM
6-[2-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]ethyl]-2-oxa-6-azaspiro[3.3]heptane	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.2700	uM
[4-(8-pyrrolidin-1-yl-3-azabicyclo[3.2.1]octane-3-carbonyl)phenyl]-(8-pyrrolidin-1-yl-3-azabicyclo[3.2.1]octan-3-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2800	uM
[3-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.2900	uM
[4-(3-pyrrolidin-1-ylazetidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.3000	uM
[5-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)furan-2-yl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.3100	uM
4-pyrrolidin-1-yl-1-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]piperidine	1077877: Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay	ic50	0.3200	uM
4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)-N-(3-pyrrolidin-1-ylpropyl)benzamide	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.3400	uM
N-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]-4-[2,5-bis(4-pyrrolidin-1-ylpiperidine-1-carbonyl)anilino]benzamide	2189726: Binding affinity to L3MBTL3 (unknown origin) by ITC assay	kd	0.3500	uM
N-(2-ethyl-1,3-dihydroisoindol-5-yl)-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)benzamide	771621: Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay	ic50	0.3500	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, decreases expression, increases expression, increases methylation	4
bisphenol A	decreases expression, increases expression, affects cotreatment	3
(+)-JQ1 compound	decreases expression	2
FR900359	increases phosphorylation	1
triphenyl phosphate	affects expression	1
trichostatin A	increases expression	1
sodium arsenite	decreases expression	1
cobaltous chloride	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases expression, affects cotreatment	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
abrine	decreases expression	1
gardiquimod	increases expression, decreases reaction	1
MT19c compound	increases expression	1
UNC1215	affects binding, decreases activity, decreases reaction	1
Zoledronic Acid	decreases expression	1
Acetaminophen	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Benzo(a)pyrene	affects methylation	1
Calcitriol	decreases expression	1
Dexamethasone	increases expression, affects cotreatment	1
Indomethacin	affects cotreatment, increases expression	1
Lipopolysaccharides	affects cotreatment, decreases expression	1
Methyl Methanesulfonate	decreases expression	1
Dihydrotestosterone	increases expression	1
Tobacco Smoke Pollution	increases expression	1
Urethane	decreases expression	1
1-Methyl-3-isobutylxanthine	affects cotreatment, increases expression	1
8-Bromo Cyclic Adenosine Monophosphate	decreases expression	1
Cadmium Chloride	decreases expression	1

ChEMBL screening assays

50 unique, capped per target: 49 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1286364	Binding	Inhibition of L3MBTL3 by alpha-screening	Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds. — J Med Chem
CHEMBL5210085	Functional	Affinity Phenotypic Cellular interaction (Foci formation of GFP-3MBT in HEK293 cells) EUB0000214b L3MBTL3	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3

Cellosaurus cell lines

1 cell lines: 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B2ZZ	Abcam HEK293T L3MBTL3 KO	Transformed cell line	Female

Clinical trials (associated diseases)

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