AEBP2

gene

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Also known as MGC17922

Summary

AEBP2 (AE binding protein 2, HGNC:24051) is a protein-coding gene on chromosome 12p12.3, encoding Zinc finger protein AEBP2 (Q6ZN18). Acts as an accessory subunit for the core Polycomb repressive complex 2 (PRC2), which mediates histone H3K27 (H3K27me3) trimethylation on chromatin leading to transcriptional repression of the affected target gene.

Predicted to enable DNA binding activity; transcription coregulator activity; and zinc ion binding activity. Predicted to be involved in regulation of transcription by RNA polymerase II. Predicted to act upstream of or within regulation of DNA-templated transcription. Located in nucleoplasm. Part of ESC/E(Z) complex.

Source: NCBI Gene 121536 — RefSeq curated summary.

At a glance

GWAS associations: 12
Clinical variants (ClinVar): 77 total
Druggable target: yes — 1 molecules with ChEMBL bioactivity
MANE Select transcript: NM_153207

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:24051
Approved symbol	AEBP2
Name	AE binding protein 2
Location	12p12.3
Locus type	gene with protein product
Status	Approved
Aliases	MGC17922
Ensembl gene	ENSG00000139154
Ensembl biotype	protein_coding
OMIM	617934
Entrez	121536

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 9 protein_coding

ENST00000266508, ENST00000360995, ENST00000398731, ENST00000398864, ENST00000512223, ENST00000538425, ENST00000541908, ENST00000673644, ENST00000673824

RefSeq mRNA: 4 — MANE Select: NM_153207 NM_001114176, NM_001267043, NM_001363736, NM_153207

CCDS: CCDS44841, CCDS44842, CCDS58215

Canonical transcript exons

ENST00000266508 — 8 exons

Exon	Start	End
ENSE00001617769	19514671	19514784
ENSE00001682922	19493800	19493986
ENSE00001685772	19500097	19500221
ENSE00001711103	19473248	19473355
ENSE00001730378	19512398	19512465
ENSE00002224438	19518087	19522227
ENSE00002282085	19439492	19440370
ENSE00003642446	19462510	19462717

Expression profiles

Bgee: expression breadth ubiquitous, 259 present calls, max score 95.93.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 31.8704 / max 780.5477, expressed in 1817 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
124594	12.7401	1777
124591	12.5228	1710
124592	1.9643	1114
124601	1.7738	941
124593	0.8217	405
124595	0.7091	364
124596	0.6925	326
124589	0.3885	25
124588	0.2151	28
124587	0.0424	18

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	95.93	gold quality
pigmented layer of retina	UBERON:0001782	94.58	gold quality
upper arm skin	UBERON:0004263	94.55	gold quality
caput epididymis	UBERON:0004358	94.32	gold quality
epithelial cell of pancreas	CL:0000083	94.25	gold quality
eye	UBERON:0000970	93.89	gold quality
buccal mucosa cell	CL:0002336	93.78	gold quality
palpebral conjunctiva	UBERON:0001812	93.68	gold quality
esophagus squamous epithelium	UBERON:0006920	93.27	gold quality
epithelium of nasopharynx	UBERON:0001951	93.19	gold quality
cauda epididymis	UBERON:0004360	92.98	gold quality
gingival epithelium	UBERON:0001949	92.86	gold quality
parietal pleura	UBERON:0002400	92.86	gold quality
gingiva	UBERON:0001828	92.52	gold quality
popliteal artery	UBERON:0002250	92.51	gold quality
tibial artery	UBERON:0007610	92.51	gold quality
smooth muscle tissue	UBERON:0001135	92.48	gold quality
saphenous vein	UBERON:0007318	92.34	gold quality
tonsil	UBERON:0002372	92.33	gold quality
placenta	UBERON:0001987	92.30	gold quality
sural nerve	UBERON:0015488	92.16	gold quality
mammary duct	UBERON:0001765	92.07	gold quality
epithelium of mammary gland	UBERON:0003244	92.07	gold quality
germinal epithelium of ovary	UBERON:0001304	92.04	gold quality
visceral pleura	UBERON:0002401	92.03	gold quality
seminal vesicle	UBERON:0000998	92.01	gold quality
adrenal tissue	UBERON:0018303	92.00	gold quality
artery	UBERON:0001637	91.91	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	91.86	gold quality
ventricular zone	UBERON:0003053	91.38	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-GEOD-110499	no	1000.28
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
FABP4	Repression

miRNA regulators (miRDB)

302 targeting AEBP2, 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-1277-5P	100.00	73.95	5056
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-513A-5P	100.00	69.77	2465
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-511-3P	99.99	68.85	1467
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-4775	99.98	75.00	6394
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-12136	99.98	72.81	5713
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-499A-5P	99.98	70.79	1323
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-1185-1-3P	99.98	71.04	2593
HSA-MIR-1185-2-3P	99.98	71.04	2593

Literature-anchored findings (GeneRIF, showing 5)

The first three-dimensional structure of the human polycomb repressive complex 2 complex bound to its cofactor AEBP2 has been presented. (PMID:23110252)
retrotransposons as promoter, which display partial DNA methylation pattern of allelic- or non-allelic origin during different stages of development (PMID:25915901)
The binding interface between AEBP and RBBP4 is relatively small compared with PHF6, histone H3 and FOG-1, indicating that AEBP may not have been the only region that participates in RBBP4 recognition. (PMID:29134516)
beta-TRCP-mediated AEBP2 ubiquitination and destruction controls cisplatin resistance in ovarian cancer. (PMID:31864706)
JARID2 and AEBP2 regulate PRC2 in the presence of H2AK119ub1 and other histone modifications. (PMID:33479123)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	aebp2	ENSDARG00000006038
mus_musculus	Aebp2	ENSMUSG00000030232
rattus_norvegicus	Aebp2	ENSRNOG00000008929

Paralogs (14): ZIC2 (ENSG00000043355), ZXDC (ENSG00000070476), GLI2 (ENSG00000074047), GLI3 (ENSG00000106571), GLIS3 (ENSG00000107249), GLI1 (ENSG00000111087), GLIS2 (ENSG00000126603), ZIC5 (ENSG00000139800), ZIC1 (ENSG00000152977), ZIC3 (ENSG00000156925), GLIS1 (ENSG00000174332), ZIC4 (ENSG00000174963), ZXDA (ENSG00000198205), ZXDB (ENSG00000198455)

Protein

Protein identifiers

Zinc finger protein AEBP2 — Q6ZN18 (reviewed: Q6ZN18)

Alternative names: Adipocyte enhancer-binding protein 2

All UniProt accessions (7): Q6ZN18, A0A669KBC9, A0A669KBL4, F5GZR7, G5EA50, H0YH08, H7BYT4

UniProt curated annotations — full annotation on UniProt →

Function. Acts as an accessory subunit for the core Polycomb repressive complex 2 (PRC2), which mediates histone H3K27 (H3K27me3) trimethylation on chromatin leading to transcriptional repression of the affected target gene. Plays a role in nucleosome localization of the PRC2 complex.

Subunit / interactions. Self-associates. Associates with the PRC2 complex, which consists of the core components EED, EZH1 or EZH2, SUZ12, and RBBP4, and various combinations of accessory subunits including AEBP2, JARID2, PHF19, MTF2 and EPOP. Found in a monomeric PRC2.2 (class 2) complex consisting of at least SUZ12, RBBP4, AEBP2 and JARID2. Within the PRC2 complex, interacts directly with SUZ12; competes with PHF19 for SUZ12 binding. Interacts with EED, EZH2, and RBBP4. May also interact with RBBP7.

Subcellular location. Nucleus.

Similarity. Belongs to the AEBP2/jing C2H2-type zinc-finger family.

Isoforms (3)

UniProt ID	Names	Canonical?
Q6ZN18-1	1	yes
Q6ZN18-2	2
Q6ZN18-3	3

RefSeq proteins (4): NP_001107648, NP_001253972, NP_001350665, NP_694939* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR013087	Znf_C2H2_type	Domain
IPR036236	Znf_C2H2_sf	Homologous_superfamily
IPR052130	AEBP2/jing_C2H2-Znf	Family
IPR059034	SH3_AEBP2_C	Domain

Pfam: PF26014

UniProt features (51 total): strand 10, helix 10, compositionally biased region 9, modified residue 8, region of interest 5, zinc finger region 3, splice variant 3, initiator methionine 1, chain 1, turn 1

Structure

Experimental structures (PDB)

18 structures.

PDB	Method	Resolution (Å)
5Y1U	X-RAY DIFFRACTION	2.14
5WAI	X-RAY DIFFRACTION	2.9
8VMI	ELECTRON MICROSCOPY	3.1
8VNV	ELECTRON MICROSCOPY	3.1
9C8U	ELECTRON MICROSCOPY	3.1
8FYH	ELECTRON MICROSCOPY	3.4
9DCH	ELECTRON MICROSCOPY	3.4
6C24	ELECTRON MICROSCOPY	3.5
6WKR	ELECTRON MICROSCOPY	3.5
8VML	ELECTRON MICROSCOPY	3.5
8VNZ	ELECTRON MICROSCOPY	3.5
8EQV	ELECTRON MICROSCOPY	3.64
6C23	ELECTRON MICROSCOPY	3.9
7KSO	ELECTRON MICROSCOPY	3.9
8TB9	ELECTRON MICROSCOPY	4
8TAS	ELECTRON MICROSCOPY	4.1
8T9G	ELECTRON MICROSCOPY	6.2
5Y0U	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q6ZN18-F1	63.62	0.06

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 (8): 2, 18, 24, 141, 206, 210, 211, 390

Function

Pathways and Gene Ontology

Reactome pathways

6 pathways

ID	Pathway
R-HSA-212300	PRC2 methylates histones and DNA
R-HSA-3214841	PKMTs methylate histone lysines
R-HSA-212165	Epigenetic regulation of gene expression
R-HSA-3247509	Chromatin modifying enzymes
R-HSA-4839726	Chromatin organization
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 273 (showing top): GCACCTT_MIR18A_MIR18B, CMYB_01, AAGCCAT_MIR135A_MIR135B, AGTCTTA_MIR499, GOBP_NEGATIVE_REGULATION_OF_GENE_EXPRESSION_EPIGENETIC, FOSTER_TOLERANT_MACROPHAGE_UP, KMCATNNWGGA_UNKNOWN, GATA1_01, TGIF_01, ZIC1_01, NKX22_01, CDPCR3HD_01, ZHANG_BREAST_CANCER_PROGENITORS_UP, GRYDER_PAX3FOXO1_ENHANCERS_IN_TADS, GOBP_CHROMATIN_REMODELING

GO Biological Process (4): negative regulation of transcription by RNA polymerase II (GO:0000122), chromatin organization (GO:0006325), regulation of transcription by RNA polymerase II (GO:0006357), regulation of DNA-templated transcription (GO:0006355)

GO Molecular Function (5): DNA binding (GO:0003677), transcription coregulator activity (GO:0003712), zinc ion binding (GO:0008270), protein binding (GO:0005515), metal ion binding (GO:0046872)

GO Cellular Component (4): chromatin (GO:0000785), nucleoplasm (GO:0005654), ESC/E(Z) complex (GO:0035098), nucleus (GO:0005634)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Epigenetic regulation of gene expression	1
Chromatin modifying enzymes	1
Gene expression (Transcription)	1
Chromatin organization	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transcription by RNA polymerase II	2
cellular anatomical structure	2
regulation of transcription by RNA polymerase II	1
negative regulation of DNA-templated transcription	1
cellular component organization	1
regulation of DNA-templated transcription	1
DNA-templated transcription	1
regulation of gene expression	1
regulation of RNA biosynthetic process	1
nucleic acid binding	1
transcription regulator activity	1
transition metal ion binding	1
binding	1
cation binding	1
chromosome	1
nuclear lumen	1
PcG protein complex	1
histone methyltransferase complex	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1002 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
AEBP2	SUZ12	Q15022	997
AEBP2	JARID2	Q92833	997
AEBP2	RBBP4	P31149	997
AEBP2	EZH2	Q15910	995
AEBP2	RBBP7	Q16576	994
AEBP2	EED	O75530	952
AEBP2	PHF1	O43189	942
AEBP2	MTF2	Q9Y483	926
AEBP2	EZH1	Q92800	893
AEBP2	PHF19	Q5T6S3	870
AEBP2	EPOP	A6NHQ4	866
AEBP2	LCOR	Q96JN0	726
AEBP2	H2AC20	Q16777	704
AEBP2	H2AC19	P20670	704
AEBP2	ARID2	Q68CP9	603

IntAct

41 interactions, top by confidence:

A	B	Type	Score
EZH2	EED	psi-mi:“MI:0914”(association)	0.930
SUZ12	EED	psi-mi:“MI:0914”(association)	0.910
EZH2	PHF1	psi-mi:“MI:0914”(association)	0.900
RBBP7	CDK2AP1	psi-mi:“MI:0914”(association)	0.840
RBBP4	CDK2AP1	psi-mi:“MI:0914”(association)	0.790
EZH2	EPOP	psi-mi:“MI:0914”(association)	0.730
AEBP2	EED	psi-mi:“MI:0915”(physical association)	0.650
AEBP2	EED	psi-mi:“MI:0914”(association)	0.650
JARID2	EED	psi-mi:“MI:0914”(association)	0.640
SUZ12	EPOP	psi-mi:“MI:0914”(association)	0.640
AEBP2	LDOC1	psi-mi:“MI:0915”(physical association)	0.550
LDOC1	AEBP2	psi-mi:“MI:0915”(physical association)	0.550
RBBP7	EPOP	psi-mi:“MI:0914”(association)	0.530
EZH1	EPOP	psi-mi:“MI:0914”(association)	0.530
EED	EPOP	psi-mi:“MI:0914”(association)	0.530
JARID2	EED	psi-mi:“MI:0914”(association)	0.500
AEBP2	TTC9C	psi-mi:“MI:0915”(physical association)	0.400
AEBP2	PHB2	psi-mi:“MI:0915”(physical association)	0.400

BioGRID (112): AEBP2 (Affinity Capture-MS), AEBP2 (Two-hybrid), AEBP2 (Affinity Capture-MS), AEBP2 (Affinity Capture-MS), AEBP2 (Affinity Capture-MS), AEBP2 (Affinity Capture-MS), RBBP7 (Affinity Capture-MS), EED (Affinity Capture-MS), EZH2 (Affinity Capture-MS), JARID2 (Affinity Capture-MS), ATXN3 (Affinity Capture-MS), KBTBD7 (Affinity Capture-MS), SUZ12 (Affinity Capture-MS), AEBP2 (Two-hybrid), RALYL (Two-hybrid)

ESM2 similar proteins: A2AFR3, A4FV57, B3KU38, F1LXF1, G3V9M2, O00287, O09112, O88450, P0C6S7, P11274, P22681, P22682, P49797, Q03353, Q03354, Q03355, Q13387, Q14CM0, Q3UR85, Q5RDF5, Q5T6S3, Q68FF6, Q69Z61, Q6GR30, Q6PAJ1, Q6ZMZ0, Q6ZN18, Q6ZWB6, Q7SXV2, Q7Z6G8, Q80ZQ5, Q86VZ6, Q8BIE6, Q8BIZ1, Q8CE64, Q8R3B7, Q8TEK3, Q8WXI2, Q96N64, Q9CXG9

Diamond homologs: A0A5K4F1D0, A0JC51, A4FV57, O57311, O60481, O73689, O95409, P08151, P10070, P10071, P19538, P34708, P39768, P46684, P47806, P55878, P55879, Q0VGT2, Q15915, Q17308, Q5IS56, Q61467, Q61602, Q62520, Q62521, Q6DJQ6, Q6GR30, Q6XP49, Q6ZN18, Q7JNM3, Q7K0S9, Q7SXV2, Q7TQ40, Q8JJC0, Q8K1M4, Q8N9L1, Q8NBF1, Q8NEA6, Q8SV95, Q8VDL9

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
AEBP2	“form complex”	“Polycomb repressive complex 2”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 24 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
Transcriptional Regulation by E2F6	6	92.5×	2e-09
PRC2 methylates histones and DNA	9	72.1×	2e-13
Regulation of PTEN gene transcription	6	56.4×	3e-08
PKMTs methylate histone lysines	6	50.8×	4e-08
Defective pyroptosis	6	49.4×	4e-08
Negative Regulation of CDH1 Gene Transcription	6	38.0×	2e-07
Regulation of PD-L1(CD274) transcription	6	34.4×	3e-07
Activation of anterior HOX genes in hindbrain development during early embryogenesis	6	28.9×	6e-07

GO biological processes:

GO term	Partners	Fold	FDR
chromatin remodeling	5	16.6×	2e-04

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	65
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1858 predictions. Top by Δscore:

Variant	Effect	Δscore
12:19462508:A:AG	acceptor_gain	1.0000
12:19462509:G:GG	acceptor_gain	1.0000
12:19462587:G:GT	donor_gain	1.0000
12:19462713:G:GT	donor_gain	1.0000
12:19462715:GGG:G	donor_gain	1.0000
12:19462716:GGG:G	donor_gain	1.0000
12:19466851:G:GG	donor_gain	1.0000
12:19473245:CA:C	acceptor_loss	1.0000
12:19473247:GGT:G	acceptor_gain	1.0000
12:19473354:AGG:A	donor_loss	1.0000
12:19473356:GTA:G	donor_loss	1.0000
12:19493797:TA:T	acceptor_loss	1.0000
12:19493798:A:AG	acceptor_gain	1.0000
12:19493798:AGT:A	acceptor_gain	1.0000
12:19493798:AGTGT:A	acceptor_gain	1.0000
12:19493799:G:GA	acceptor_gain	1.0000
12:19493799:G:T	acceptor_loss	1.0000
12:19493799:GT:G	acceptor_gain	1.0000
12:19493799:GTG:G	acceptor_gain	1.0000
12:19493799:GTGT:G	acceptor_gain	1.0000
12:19493799:GTGTG:G	acceptor_gain	1.0000
12:19493982:ATTAC:A	donor_gain	1.0000
12:19493983:TTAC:T	donor_gain	1.0000
12:19493985:AC:A	donor_gain	1.0000
12:19493985:ACGT:A	donor_loss	1.0000
12:19493986:CG:C	donor_loss	1.0000
12:19493987:G:GG	donor_gain	1.0000
12:19493987:GTAAG:G	donor_loss	1.0000
12:19493988:T:A	donor_loss	1.0000
12:19500095:A:AG	acceptor_gain	1.0000

AlphaMissense

3336 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:19462625:T:A	C263S	1.000
12:19462625:T:C	C263R	1.000
12:19462626:G:A	C263Y	1.000
12:19462626:G:C	C263S	1.000
12:19462627:T:G	C263W	1.000
12:19462631:T:A	W265R	1.000
12:19462631:T:C	W265R	1.000
12:19462632:G:C	W265S	1.000
12:19462633:G:C	W265C	1.000
12:19462633:G:T	W265C	1.000
12:19462640:T:C	C268R	1.000
12:19462642:C:G	C268W	1.000
12:19462671:T:C	L278P	1.000
12:19462680:A:C	H281P	1.000
12:19462681:C:A	H281Q	1.000
12:19462681:C:G	H281Q	1.000
12:19462683:T:A	I282N	1.000
12:19462694:C:A	H286N	1.000
12:19462694:C:G	H286D	1.000
12:19462696:T:A	H286Q	1.000
12:19462696:T:G	H286Q	1.000
12:19473251:T:C	F295L	1.000
12:19473253:T:A	F295L	1.000
12:19473253:T:G	F295L	1.000
12:19473255:T:A	V296D	1.000
12:19473257:T:A	C297S	1.000
12:19473257:T:C	C297R	1.000
12:19473257:T:G	C297G	1.000
12:19473258:G:A	C297Y	1.000
12:19473258:G:C	C297S	1.000

dbSNP variants (sampled 300 via entrez): RS1000021437 (12:19454819 C>T), RS1000029055 (12:19444505 G>A), RS1000057995 (12:19440899 T>A), RS1000084170 (12:19513291 C>A,G,T), RS1000088618 (12:19440746 T>C,G), RS1000108005 (12:19460405 T>G), RS1000115127 (12:19513550 G>A), RS1000133555 (12:19477574 G>C), RS1000255379 (12:19472361 C>G,T), RS1000289523 (12:19472171 A>G), RS1000297580 (12:19487647 G>A), RS1000303645 (12:19475617 G>C), RS1000344233 (12:19427179 C>A,T), RS1000349991 (12:19445628 G>A), RS1000445522 (12:19470454 G>A,C)

Disease associations

OMIM: gene MIM:617934 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

12 associations (top):

Study	Trait	p-value
GCST001248_2	Pulmonary function	8.000000e-06
GCST001762_904	Obesity-related traits	2.000000e-06
GCST002932_35	Manganese levels	4.000000e-06
GCST003486_1	Response to fenofibrate (LDL cholesterol levels)	7.000000e-07
GCST006479_92	Diverticular disease	2.000000e-06
GCST006627_40	Diastolic blood pressure	1.000000e-11
GCST007431_14	Lung function (FEV1/FVC)	2.000000e-12
GCST008163_221	Height	3.000000e-07
GCST008708_3	Chronic mountain sickness	5.000000e-09
GCST009796_5	Opioid use cessation	3.000000e-06
GCST010989_36	Body size at age 10	3.000000e-08
GCST012297_5	Schizophrenia, bipolar disorder or major depressive disorder	6.000000e-06

EFO canonical traits (9, from GWAS)

EFO ID	Trait name
EFO:0003892	pulmonary function measurement
EFO:0004713	FEV/FVC ratio
EFO:0003940	physical activity
EFO:0007804	LDL cholesterol change measurement
EFO:0009959	diverticular disease
EFO:0006336	diastolic blood pressure
EFO:0010143	chronic mountain sickness
EFO:0009937	Opioid use measurement
EFO:0009819	comparative body size at age 10, self-reported

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL3137287 (PROTEIN COMPLEX), CHEMBL6066550 (PROTEIN COMPLEX), CHEMBL6066551 (PROTEIN COMPLEX)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,869 (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
CHEMBL3414621	TAZEMETOSTAT	4	1,869

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

Binding affinities (BindingDB)

89 measured of 144 human assays (144 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-[(E)-1-(4-aminocyclohexyl)prop-1-enyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	13 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(((cis)-4-(dimethylamino)cyclohexyl)(ethyl)amino)-4-methylthiophene-3-carboxamide (Example 7) and N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(((trans)-4-(dimethylamino)cyclohexyl)(ethyl)amino)-4-methylthiophene-3-carboxamide (Example 8)	IC50	13 nM	US-9790212: Enhancer of zeste homolog 2 inhibitors
5-Bromo-3-(sec-butoxy)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methylbenzamide	IC50	13 nM	US-10478426: Enhancer of Zeste Homolog 2 inhibitors
4-[[4-(dimethylamino)cyclohexyl]-ethylamino]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-3-methylthiophene-2-carboxamide	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
tert-butyl 4-[[4-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methylcarbamoyl]-3-methylthiophen-2-yl]-ethylamino]piperidine-1-carboxylate	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[1-(4-aminocyclohexyl)propyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
2-chloro-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl-[4-[ethyl(methyl)amino]cyclohexyl]amino]-4-methylthiophene-3-carboxamide	IC50	16 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[1-[4-(dimethylamino)piperidin-1-yl]propyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	19 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(piperidin-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
2-bromo-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-(1-piperidin-4-ylpropyl)thiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[(1S)-1-[4-(dimethylamino)piperidin-1-yl]propyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[1-[4-(dimethylamino)cyclohexyl]propyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
2-bromo-5-[[4-(dimethylamino)cyclohexyl]-ethylamino]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl-(3-fluoropiperidin-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	20 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
2-cyano-5-[[4-(dimethylamino)cyclohexyl]-ethylamino]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	25 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-2-(furan-3-yl)-4-methylthiophene-3-carboxamide	IC50	25 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[1-[4-(dimethylamino)piperidin-1-yl]ethyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	31 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
4-[[4-(dimethylamino)cyclohexyl]-ethylamino]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-3-methylthiophene-2-carboxamide	IC50	32 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-2,4-dimethylthiophene-3-carboxamide	IC50	32 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-2-(furan-2-yl)-4-methylthiophene-3-carboxamide	IC50	32 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[[4-(dimethylamino)cyclohexyl]-ethylamino]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-2-(furan-3-yl)-4-methylthiophene-3-carboxamide	IC50	32 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[[4-(dimethylamino)cyclohexyl]-ethylamino]-4-methyl-N-[(1,4,6-trimethyl-2-oxo-3-pyridinyl)methyl]thiophene-3-carboxamide	IC50	50 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
tert-butyl 4-[1-[4-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methylcarbamoyl]-3-methylthiophen-2-yl]propyl]piperidine-1-carboxylate	IC50	50 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl-(1-propan-2-ylpiperidin-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	63 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
2-cyano-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methylthiophene-3-carboxamide	IC50	79 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-(2-piperidin-4-ylpyrrolidin-1-yl)thiophene-3-carboxamide	IC50	79 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-chloro-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-[ethyl(oxan-4-yl)amino]-3-methylthiophene-2-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[hydroxy(piperidin-4-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-(2-methylpyrrolidin-1-yl)thiophene-3-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[ethyl(oxan-4-yl)amino]-4-methyl-N-[(1,4,6-trimethyl-2-oxo-3-pyridinyl)methyl]thiophene-3-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
tert-butyl N-[4-[(E)-1-[4-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methylcarbamoyl]-3-methylthiophen-2-yl]prop-1-enyl]cyclohexyl]carbamate	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-(1,2,3,4-tetrahydroisoquinolin-5-yl)thiophene-3-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methyl-2-(1-methylpyrazol-4-yl)thiophene-3-carboxamide	IC50	100 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(hydroxy(piperidin-4-yl)methyl)-4-methylthiophene-3-carboxamide	IC50	100 nM	US-9790212: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-(1-piperidin-4-ylethenyl)thiophene-3-carboxamide	IC50	126 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methyl-5-[6-(4-methylpiperazin-1-yl)hexan-3-yl]thiophene-3-carboxamide	IC50	126 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
tert-butyl 4-[hydroxy-(4-methoxycarbonyl-3-methylthiophen-2-yl)methyl]piperidine-1-carboxylate	IC50	158 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[[4-(dimethylamino)cyclohexyl]-hydroxymethyl]-N-[(4,6-dimethyl-2-oxo-3H-pyridin-3-yl)methyl]-4-methylthiophene-3-carboxamide	IC50	158 nM	US-9505745: Enhancer of zeste homolog 2 inhibitors
5-[5-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]pyrido[3,4-d]pyridazin-8-yl]-N,N,4-trimethylpyridine-2-carboxamide	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
4-[5-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]pyrido[3,4-d]pyridazin-8-yl]-N,N-dimethylbenzamide	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(4-((methylamino)methyl)phenyl)pyrido[3,4-d]pyridazin-5-amine	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
N-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methyl]-4-(2-methyl-4-methylsulfonylphenyl)-2,7-naphthyridin-1-amine	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
5-(1-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-2,7-naphthyridin-4-yl)-N,N,1-trimethyl-1H-pyrazol-e-3-carboxamide	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
4-(1,3-dimethyl-1H-pyrazol-5-yl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-6-methoxy-2,7-naphthyridin-1-amine	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
8-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-5-[4-(pyrrolidin-1-ylmethyl)phenyl]-2H-2,7-naphthyridin-3-one	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
5-[4-[(dimethylamino)methyl]phenyl]-8-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-2H-2,7-naphthyridin-3-one	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors
8-[(5-fluoro-2,3-dihydro-1-benzofuran-4-yl)methylamino]-5-(2-methyl-4-methylsulfonylphenyl)-2H-2,7-naphthyridin-3-one	IC50	175 nM	US-12421228: Naphthyridine derivatives as PRC2 inhibitors

ChEMBL bioactivities

496 potent at pChembl≥5 of 501 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.00	IC50	0.1	nM	CHEMBL4159112
9.40	IC50	0.4	nM	CHEMBL4161265
9.30	IC50	0.5	nM	CHEMBL4165937
9.22	IC50	0.6	nM	CHEMBL4160111
9.10	IC50	0.8	nM	CHEMBL4172576
8.67	IC50	2.15	nM	CHEMBL6052145
8.58	IC50	2.65	nM	CHEMBL6024531
8.57	IC50	2.7	nM	CHEMBL4164687
8.54	IC50	2.9	nM	CHEMBL4170327
8.51	IC50	3.1	nM	CHEMBL5951235
8.48	IC50	3.3	nM	CHEMBL4162316
8.42	IC50	3.8	nM	CHEMBL4177454
8.40	IC50	4	nM	CHEMBL4162499
8.40	IC50	4	nM	CHEMBL4170753
8.40	IC50	4	nM	CHEMBL4174176
8.40	IC50	4	nM	TAZEMETOSTAT
8.39	IC50	4.1	nM	CHEMBL4169191
8.34	IC50	4.6	nM	CHEMBL4169368
8.34	IC50	4.6	nM	CHEMBL4162406
8.23	IC50	5.9	nM	CHEMBL4169598
8.22	IC50	6	nM	CHEMBL4167587
8.21	IC50	6.1	nM	CHEMBL4169762
8.19	IC50	6.5	nM	CHEMBL4176373
8.19	IC50	6.4	nM	CHEMBL4161444
8.11	IC50	7.8	nM	CHEMBL4176554
7.89	IC50	13	nM	CHEMBL5893972
7.89	IC50	13	nM	CHEMBL5900858
7.89	IC50	13	nM	CHEMBL5876110
7.89	IC50	13	nM	CHEMBL5877767
7.89	IC50	13	nM	CHEMBL5917099
7.80	IC50	16	nM	CHEMBL5915007
7.80	IC50	16	nM	CHEMBL6007399
7.80	IC50	16	nM	CHEMBL5766410
7.80	IC50	16	nM	CHEMBL5953012
7.80	IC50	16	nM	CHEMBL5969797
7.80	IC50	16	nM	CHEMBL6019885
7.72	IC50	19	nM	CHEMBL5778578
7.70	IC50	20	nM	CHEMBL3770000
7.70	IC50	20	nM	CHEMBL5893972
7.70	IC50	20	nM	CHEMBL5766410
7.70	IC50	20	nM	CHEMBL5752900
7.70	IC50	20	nM	CHEMBL5827347
7.70	IC50	20	nM	CHEMBL6008235
7.70	IC50	20	nM	CHEMBL5779095
7.70	IC50	20	nM	CHEMBL6014189
7.70	IC50	20	nM	CHEMBL5930741
7.70	IC50	20	nM	CHEMBL5918559
7.60	IC50	25	nM	CHEMBL5915007
7.60	IC50	25	nM	CHEMBL5976294
7.60	IC50	25	nM	CHEMBL6050278

PubChem BioAssay actives

32 with measured affinity, of 33 total; 29 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
5-ethyl-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-[(4-methylpiperazin-1-yl)methyl]-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0001	uM
2-chloro-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0004	uM
2-cyclopropyl-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0005	uM
N-[(4-ethyl-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[ethyl(oxan-4-yl)amino]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0006	uM
2-cyano-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0008	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-2-(trifluoromethyl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0027	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2,5-dimethyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0029	uM
5-ethyl-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0033	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[ethyl(oxan-4-yl)amino]-2,5-dimethyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0038	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(1-propan-2-ylpiperidin-4-yl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0040	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0040	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[ethyl(oxan-4-yl)amino]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0040	uM
Tazemetostat	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0040	uM
6-[ethyl(oxan-4-yl)amino]-2-fluoro-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-methyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0041	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(morpholin-4-ylmethyl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0046	uM
6-[ethyl(oxan-4-yl)amino]-5-methyl-N-[[6-methyl-2-oxo-4-(trifluoromethyl)-1H-pyridin-3-yl]methyl]-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0046	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-3,5-dimethyl-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0059	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[ethyl(oxan-4-yl)amino]-5-methyl-1-benzothiophene-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0060	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-ethyl-6-[ethyl(oxan-4-yl)amino]-2-(1-methylpiperidin-4-yl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0061	uM
5-ethyl-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-(piperidin-1-ylmethyl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0064	uM
5-chloro-6-[ethyl(oxan-4-yl)amino]-N-[(6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0065	uM
5-ethyl-6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-(morpholin-4-ylmethyl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0078	uM
N-(furan-2-ylmethyl)-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine	1802691: HMT Assay from Article 10.1038/nchembio.2304: “An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.”	ic50	0.0200	uM
5-bromo-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methylbenzamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.0200	uM
N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)-3-pyridinyl]-1-propan-2-ylindazole-4-carboxamide	711406: Inhibition of PRC2 complex of EZH1, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr by SPA	ic50	0.1000	uM
N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)-4-pyridinyl]-1-propan-2-ylindazole-4-carboxamide	711406: Inhibition of PRC2 complex of EZH1, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr by SPA	ic50	0.2400	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	0.3310	uM
6-[ethyl(oxan-4-yl)amino]-N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-5-(trifluoromethyl)-1-benzofuran-4-carboxamide	1350244: Inhibition of human N-terminal His-tagged EZH2/flag-tagged EED/SUZ12/AEBP2/RBAP48 A677G mutant (2 to end residues) expressed in baculovirus infected Sf9 insect cells using histone H3 (1 to 50 residues)-GGK as substrate after 2 hrs in presence of SAM by fluorescence assay	ic50	2.0000	uM
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)-3-pyridinyl]-1-propan-2-ylindazole-4-carboxamide	711406: Inhibition of PRC2 complex of EZH1, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr by SPA	ic50	2.5000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	decreases expression, increases expression	3
Valproic Acid	decreases expression, increases methylation	3
sodium arsenite	increases expression, decreases expression	2
Phenylmercuric Acetate	decreases expression, affects cotreatment	2
Cyclosporine	decreases expression, increases expression	2
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
trichostatin A	affects expression	1
benzo(e)pyrene	increases methylation	1
coumarin	increases phosphorylation	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
ICG 001	increases expression	1
abrine	increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
jinfukang	decreases expression	1
Sunitinib	increases expression	1
Air Pollutants	decreases expression, increases abundance	1
Arbutin	increases expression	1
Caffeine	decreases phosphorylation	1
Dimethyl Sulfoxide	increases expression	1
Indomethacin	decreases expression	1
Ketoconazole	decreases expression	1
Methapyrilene	increases methylation	1
Selenium	decreases methylation	1
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression	1
Aflatoxin B1	increases methylation	1
Asbestos, Crocidolite	decreases expression	1
Cadmium Chloride	decreases expression	1
Palmitic Acid	increases phosphorylation	1

ChEMBL screening assays

10 unique, capped per target: 10 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2209120	Binding	Inhibition of PRC2 complex of EZH1, EED, SUZ12, AEBP2 and RbAp48 using histone H3 peptide (21 to 44) as substrate and [3H]SAM after 1 hr by SPA	Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. — ACS Med Chem Lett

Cellosaurus cell lines

5 cell lines: 4 cancer cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_HC69	HEK293 eGFP-AEBP2	Transformed cell line	Female
CVCL_SB85	HAP1 AEBP2 (-) 1	Cancer cell line	Male
CVCL_SB86	HAP1 AEBP2 (-) 2	Cancer cell line	Male
CVCL_SB87	HAP1 AEBP2 (-) 3	Cancer cell line	Male
CVCL_SB88	HAP1 AEBP2 (-) 4	Cancer cell line	Male

Clinical trials (associated diseases)

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

No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.