ENY2

Summary

ENY2 (ENY2 transcription and export complex 2 subunit, HGNC:24449) is a protein-coding gene on chromosome 8q23.1, encoding Transcription and mRNA export factor ENY2 (Q9NPA8). Involved in mRNA export coupled transcription activation by association with both the TREX-2 and the SAGA complexes. It is a selective cancer dependency (DepMap: 14.9% of cell lines).

Enables transcription coactivator activity. Involved in poly(A)+ mRNA export from nucleus; positive regulation of DNA-templated transcription; and regulation of transcription by RNA polymerase II. Located in mitochondrion and nucleoplasm. Part of SAGA complex and nucleus.

Source: NCBI Gene 56943 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 16 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 14.9% of screened cell lines
• MANE Select transcript: NM_020189

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:24449
Approved symbol	ENY2
Name	ENY2 transcription and export complex 2 subunit
Location	8q23.1
Locus type	gene with protein product
Status	Approved
Aliases	DC6, FLJ20480, Sus1
Ensembl gene	ENSG00000120533
Ensembl biotype	protein_coding
OMIM	619015
Entrez	56943

Gene structure

Transcript identifiers

Ensembl transcripts: 16 — 7 retained_intron, 4 nonsense_mediated_decay, 3 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000339942, ENST00000517311, ENST00000517350, ENST00000517756, ENST00000518118, ENST00000518584, ENST00000519754, ENST00000520147, ENST00000521619, ENST00000521662, ENST00000521688, ENST00000522407, ENST00000522632, ENST00000522766, ENST00000523335, ENST00000523707

RefSeq mRNA: 2 — MANE Select: NM_020189 NM_001193557, NM_020189

CCDS: CCDS43762, CCDS55270

Canonical transcript exons

ENST00000521688 — 5 exons

Exon	Start	End
ENSE00002131803	109334347	109334474
ENSE00003573333	109340489	109340563
ENSE00003596719	109339320	109339390
ENSE00003640464	109343405	109345954
ENSE00003683129	109336128	109336204

Expression profiles

Bgee: expression breadth ubiquitous, 288 present calls, max score 99.10.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 100.1814 / max 2326.7786, expressed in 1825 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
90255	99.2422	1825
90254	0.6289	377
205289	0.3104	128

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
tendon of biceps brachii	UBERON:0008188	99.10	gold quality
oocyte	CL:0000023	99.02	gold quality
monocyte	CL:0000576	98.45	gold quality
mononuclear cell	CL:0000842	98.40	gold quality
leukocyte	CL:0000738	98.26	gold quality
tendon	UBERON:0000043	97.92	gold quality
secondary oocyte	CL:0000655	97.89	gold quality
omental fat pad	UBERON:0010414	97.55	gold quality
peritoneum	UBERON:0002358	97.54	gold quality
right atrium auricular region	UBERON:0006631	97.53	gold quality
right adrenal gland cortex	UBERON:0035827	97.49	gold quality
left adrenal gland	UBERON:0001234	97.48	gold quality
calcaneal tendon	UBERON:0003701	97.45	gold quality
right adrenal gland	UBERON:0001233	97.43	gold quality
left adrenal gland cortex	UBERON:0035825	97.43	gold quality
right lobe of liver	UBERON:0001114	97.42	gold quality
adipose tissue of abdominal region	UBERON:0007808	97.40	gold quality
embryo	UBERON:0000922	97.32	gold quality
body of pancreas	UBERON:0001150	97.30	gold quality
ganglionic eminence	UBERON:0004023	97.30	gold quality
left coronary artery	UBERON:0001626	97.29	gold quality
mucosa of transverse colon	UBERON:0004991	97.24	gold quality
muscle layer of sigmoid colon	UBERON:0035805	97.23	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	97.20	gold quality
lower esophagus muscularis layer	UBERON:0035833	97.19	gold quality
bone marrow	UBERON:0002371	97.18	gold quality
lower esophagus	UBERON:0013473	97.17	gold quality
popliteal artery	UBERON:0002250	97.16	gold quality
tibial artery	UBERON:0007610	97.16	gold quality
rectum	UBERON:0001052	97.14	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-MTAB-11011	no	265.17
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

134 targeting ENY2, 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-450A-1-3P	100.00	69.33	1837
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-6740-5P	100.00	65.64	932
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-485-3P	99.98	70.68	1585
HSA-MIR-539-3P	99.98	70.74	1616
HSA-MIR-433-3P	99.98	69.37	1203
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-101-3P	99.94	75.03	2230
HSA-MIR-144-3P	99.94	73.98	2698
HSA-MIR-4525	99.94	64.38	675
HSA-MIR-5010-5P	99.94	64.11	705
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-6772-5P	99.94	67.01	577
HSA-MIR-335-3P	99.93	73.36	4958
HSA-MIR-539-5P	99.93	70.30	2855
HSA-MIR-10523-5P	99.91	69.22	2038
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-124-3P	99.89	73.74	3043
HSA-MIR-506-3P	99.89	73.55	3057

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 14.9% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 2)

• ATXN7L3, USP22, & ENY2 are required cofactors for full transcriptional activity by nuclear receptors. The deubiquitinase activity of TFTC/STAGA HAT counteracts heterochromatin silencing & is a positive cofactor for in vivo nuclear receptor activation. (PMID:18206972)
• ATXN7L3 and ENY2 orchestrate activities of multiple deubiquitinating enzymes, including USP27x and USP51, and that imbalances in these activities likely potentiate human diseases including cancer. (PMID:27132940)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	eny2	ENSDARG00000070046
mus_musculus	Eny2	ENSMUSG00000022338
rattus_norvegicus	Eny2	ENSRNOG00000004681
drosophila_melanogaster	e(y)2	FBGN0000618

Protein

Protein identifiers

Transcription and mRNA export factor ENY2 — Q9NPA8 (reviewed: Q9NPA8)

Alternative names: Enhancer of yellow 2 transcription factor homolog

All UniProt accessions (6): Q9NPA8, E5RHT9, E5RHX8, E5RI00, E5RJ84, J3KNT2

UniProt curated annotations — full annotation on UniProt →

Function. Involved in mRNA export coupled transcription activation by association with both the TREX-2 and the SAGA complexes. The transcription regulatory histone acetylation (HAT) complex SAGA is a multiprotein complex that activates transcription by remodeling chromatin and mediating histone acetylation and deubiquitination. Within the SAGA complex, participates in a subcomplex that specifically deubiquitinates both histones H2A and H2B. The SAGA complex is recruited to specific gene promoters by activators such as MYC, where it is required for transcription. Required for nuclear receptor-mediated transactivation. As a component of the TREX-2 complex, involved in the export of mRNAs to the cytoplasm through the nuclear pores.

Subunit / interactions. Component of the nuclear pore complex (NPC)-associated TREX-2 complex (transcription and export complex 2), composed of at least ENY2, the isoform GANP of the MCM3AP gene, PCID2, SEM1, and either centrin CETN2 or CETN3. TREX-2 contains 2 ENY2 chains. The TREX-2 complex also associates with ALYREF/ALY and with the nucleoporin NUP153. Component of some SAGA transcription coactivator-HAT complexes, at least composed of ATXN7, ATXN7L3, ENY2, GCN5L2, SUPT3H/SPT3, TAF10, TRRAP and USP22. Within the SAGA complex, ENY2, ATXN7, ATXN7L3, and USP22 form an additional subcomplex of SAGA called the DUB module (deubiquitination module). Interacts with RNA polymerase II subunit POLR2A. Interacts with ATXN7L3B.

Subcellular location. Nucleus. Nucleoplasm.

Similarity. Belongs to the ENY2 family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9NPA8-1	1	yes
Q9NPA8-2	2

RefSeq proteins (2): NP_001180486, NP_064574* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR018783	TF_ENY2	Family
IPR038212	TF_EnY2_sf	Homologous_superfamily

Pfam: PF10163

UniProt features (10 total): helix 5, chain 1, cross-link 1, splice variant 1, turn 1, modified residue 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
4DHX	X-RAY DIFFRACTION	2.1

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NPA8-F1	93.74	0.88

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 (2): 74, 1

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-3214847	HATs acetylate histones

MSigDB gene sets: 196 (showing top): GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, HORIUCHI_WTAP_TARGETS_DN, GOBP_REGULATION_OF_DNA_REPAIR, GOBP_NUCLEAR_TRANSPORT, MARTORIATI_MDM4_TARGETS_NEUROEPITHELIUM_DN, ONKEN_UVEAL_MELANOMA_UP, MODULE_206, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, GOBP_NUCLEOBASE_CONTAINING_COMPOUND_TRANSPORT, GOBP_RNA_SPLICING, GOBP_DNA_DAMAGE_RESPONSE, GUO_HEX_TARGETS_UP, DODD_NASOPHARYNGEAL_CARCINOMA_UP, GOCC_RNA_POLYMERASE_COMPLEX, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_STRESS

GO Biological Process (11): regulation of DNA repair (GO:0006282), chromatin organization (GO:0006325), regulation of transcription by RNA polymerase II (GO:0006357), transcription elongation by RNA polymerase II (GO:0006368), protein transport (GO:0015031), poly(A)+ mRNA export from nucleus (GO:0016973), regulation of RNA splicing (GO:0043484), positive regulation of DNA-templated transcription (GO:0045893), negative regulation of insulin secretion involved in cellular response to glucose stimulus (GO:0061179), mRNA export from nucleus (GO:0006406), mRNA transport (GO:0051028)

GO Molecular Function (3): chromatin binding (GO:0003682), transcription coactivator activity (GO:0003713), protein binding (GO:0005515)

GO Cellular Component (9): SAGA complex (GO:0000124), nucleoplasm (GO:0005654), mitochondrion (GO:0005739), transcription factor TFTC complex (GO:0033276), nuclear pore nuclear basket (GO:0044615), transcription export complex 2 (GO:0070390), DUBm complex (GO:0071819), nucleus (GO:0005634), nuclear pore (GO:0005643)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Chromatin modifying enzymes	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
nuclear protein-containing complex	4
regulation of DNA-templated transcription	2
transcription by RNA polymerase II	2
binding	2
SAGA-type complex	2
intracellular membrane-bounded organelle	2
DNA repair	1
regulation of DNA metabolic process	1
regulation of cellular response to stress	1
cellular component organization	1
DNA-templated transcription elongation	1
transport	1
intracellular protein localization	1
establishment of protein localization	1
mRNA export from nucleus	1
RNA splicing	1
regulation of gene expression	1
regulation of primary metabolic process	1
DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
insulin secretion involved in cellular response to glucose stimulus	1
negative regulation of insulin secretion	1
negative regulation of response to stimulus	1
regulation of insulin secretion involved in cellular response to glucose stimulus	1
RNA export from nucleus	1
gene expression	1
mRNA transport	1
RNA transport	1
transcription coregulator activity	1
positive regulation of DNA-templated transcription	1
DUBm complex	1
peptidase complex	1
nuclear lumen	1
cellular anatomical structure	1
cytoplasm	1
RNA polymerase II, holoenzyme	1
RNA polymerase II transcription regulator complex	1
nuclear pore	1
nuclear envelope	1

Protein interactions and networks

STRING

2545 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ENY2	ATXN7	O15265	997
ENY2	ATXN7L3	Q14CW9	995
ENY2	SEM1	Q6ZVN7	992
ENY2	PCID2	Q5JVF3	991
ENY2	MCM3AP	O60318	980
ENY2	CETN2	P41208	977
ENY2	USP22	Q9UPT9	973
ENY2	CETN3	O15182	899
ENY2	USP51	Q70EK9	887
ENY2	USP27X	A6NNY8	885
ENY2	ATXN7L2	Q5T6C5	884
ENY2	ATXN7L1	Q9ULK2	881
ENY2	TADA3	O75528	850
ENY2	SGF29	Q96ES7	829
ENY2	AWAT2	Q6E213	821

IntAct

57 interactions, top by confidence:

A	B	Type	Score
ATXN7L3	ENY2	psi-mi:“MI:0915”(physical association)	0.840
TRRAP	ATXN7	psi-mi:“MI:0914”(association)	0.740
ATXN7L3	USP27X	psi-mi:“MI:0914”(association)	0.640
CETN1	SFI1	psi-mi:“MI:0914”(association)	0.640
CSTPP1	ENY2	psi-mi:“MI:0915”(physical association)	0.560
HNRNPA2B1	ENY2	psi-mi:“MI:0915”(physical association)	0.560
KSR2	POLR3A	psi-mi:“MI:0914”(association)	0.530
NS1	PIK3R2	psi-mi:“MI:0914”(association)	0.530
EPB41L3	AP3B1	psi-mi:“MI:0914”(association)	0.530
LYG1	ENY2	psi-mi:“MI:0915”(physical association)	0.400
ENY2		psi-mi:“MI:0915”(physical association)	0.370
Kifc5b	KPNA3	psi-mi:“MI:0914”(association)	0.350
Naa10	MYO9A	psi-mi:“MI:0914”(association)	0.350
PCDHB15	HLA-A	psi-mi:“MI:0914”(association)	0.350
Rock1		psi-mi:“MI:0914”(association)	0.350
NEIL3	SF3B2	psi-mi:“MI:0914”(association)	0.350
Smo	METTL8	psi-mi:“MI:0914”(association)	0.350
NS1	SAC3D1	psi-mi:“MI:0914”(association)	0.350
KSR1	FBLL1	psi-mi:“MI:0914”(association)	0.350
KSR1		psi-mi:“MI:0914”(association)	0.350
DND1	RPSA2	psi-mi:“MI:0914”(association)	0.350
Prdm16	ESYT2	psi-mi:“MI:0914”(association)	0.350
OASL	LARP1	psi-mi:“MI:0914”(association)	0.350
ATXN7L3	USP27X	psi-mi:“MI:0914”(association)	0.350
USP22	CNOT1	psi-mi:“MI:0914”(association)	0.350
MED23	PGRMC1	psi-mi:“MI:0914”(association)	0.350

BioGRID (242): ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), H2AFX (Co-fractionation), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS), ENY2 (Affinity Capture-MS)

ESM2 similar proteins: A0JN61, A4QNE0, O35427, O60763, O60941, O70585, O75575, O88597, O95453, P11029, P11497, P13984, P41541, P41542, P69341, Q01750, Q05B58, Q0JNK5, Q13085, Q13901, Q14457, Q28559, Q2T9L9, Q32PE4, Q3ZBJ0, Q4A1L4, Q4A1L5, Q5R4J9, Q5R660, Q5R878, Q5RBU4, Q5SWU9, Q5ZHS3, Q5ZKS6, Q60482, Q6NRL4, Q80UM3, Q8BWQ6, Q8L5Y9, Q8NE86

Diamond homologs: B0WG73, B2RYZ5, B3MQ24, B3NUB6, B4H2S0, B4IK33, B4JLC3, B4L1Z8, B4M6M6, B4N1G8, B4NUB3, B4PY93, B4UN38, B5FZ63, B5XC71, B5XGH3, P0CS72, P0CS73, Q17MZ8, Q29IN4, Q3KPT5, Q3ZBJ0, Q4H3N8, Q6DH42, Q75BB0, Q7LL15, Q9JIX0, Q9NPA8, Q9VI60, Q9VYX1, Q54HB4, Q6NQ54, A5DG59, A6ZL57, B3LN41, Q6WNK7, Q5ADP6

SIGNOR signaling

1 interactions.

A	Effect	B	Mechanism
ENY2	“form complex”	“SAGA complex”	binding

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 60 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.

GO biological processes:

GO term	Partners	Fold	FDR
regulation of DNA repair	6	33.8×	8e-06
regulation of RNA splicing	6	26.8×	2e-05

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	6
Likely benign	0
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

956 predictions. Top by Δscore:

Variant	Effect	Δscore
8:109340475:T:TA	acceptor_gain	1.0000
8:109340481:T:A	acceptor_gain	1.0000
8:109340484:A:AG	acceptor_gain	1.0000
8:109340485:T:G	acceptor_gain	1.0000
8:109340487:A:G	acceptor_gain	1.0000
8:109342603:GCT:G	donor_gain	1.0000
8:109343403:A:AG	acceptor_gain	1.0000
8:109343404:G:GG	acceptor_gain	1.0000
8:109339318:A:AG	acceptor_gain	0.9900
8:109339319:G:GG	acceptor_gain	0.9900
8:109340486:A:AG	acceptor_gain	0.9900
8:109340486:AAGAG:A	acceptor_gain	0.9900
8:109340559:CAGAG:C	donor_loss	0.9900
8:109340560:AGAG:A	donor_loss	0.9900
8:109340561:GAG:G	donor_gain	0.9900
8:109340562:AG:A	donor_loss	0.9900
8:109340563:GGTAA:G	donor_loss	0.9900
8:109340564:G:C	donor_loss	0.9900
8:109340565:TAA:T	donor_loss	0.9900
8:109341673:GAGAA:G	donor_gain	0.9900
8:109341675:G:GT	donor_gain	0.9900
8:109343399:TTTCA:T	acceptor_loss	0.9900
8:109343400:TTCA:T	acceptor_loss	0.9900
8:109343401:TCAG:T	acceptor_loss	0.9900
8:109343402:CA:C	acceptor_loss	0.9900
8:109343403:A:G	acceptor_loss	0.9900
8:109343404:GC:G	acceptor_gain	0.9900
8:109343404:GCC:G	acceptor_gain	0.9900
8:109343404:GCCC:G	acceptor_gain	0.9900
8:109343404:GCCCT:G	acceptor_gain	0.9900

AlphaMissense

664 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:109339346:T:C	L37S	1.000
8:109339360:T:A	W42R	1.000
8:109339360:T:C	W42R	1.000
8:109339362:G:C	W42C	1.000
8:109339362:G:T	W42C	1.000
8:109336180:T:C	L20S	0.999
8:109339361:G:C	W42S	0.999
8:109340557:G:C	G75R	0.999
8:109340558:G:A	G75D	0.999
8:109343427:G:C	K84N	0.999
8:109343427:G:T	K84N	0.999
8:109343435:T:C	L87P	0.999
8:109339358:G:T	G41V	0.998
8:109340534:T:C	L67S	0.998
8:109343411:T:A	V79E	0.998
8:109336192:G:T	G24V	0.997
8:109339322:T:C	L29P	0.997
8:109339361:G:T	W42L	0.997
8:109339385:G:A	C50Y	0.997
8:109339386:T:G	C50W	0.997
8:109340562:A:C	R76S	0.997
8:109340562:A:T	R76S	0.997
8:109343426:A:T	K84M	0.997
8:109343438:T:C	L88P	0.997
8:109343455:T:C	F94L	0.997
8:109343457:C:A	F94L	0.997
8:109343457:C:G	F94L	0.997
8:109339334:T:A	L33Q	0.996
8:109339334:T:C	L33P	0.996
8:109339373:T:C	L46S	0.996

dbSNP variants (sampled 300 via entrez): RS1000028157 (8:109346440 G>A,C), RS1000510377 (8:109339917 A>G), RS1000669718 (8:109335154 G>A), RS1000932965 (8:109335363 A>G,T), RS1001113404 (8:109341608 G>A,C), RS1001361635 (8:109342565 G>A,C), RS1001541581 (8:109341915 T>C), RS1001572425 (8:109332896 C>A), RS1001658444 (8:109333203 T>C), RS1001680973 (8:109336512 T>A), RS1001734991 (8:109336858 T>C), RS1001774965 (8:109338194 C>A), RS1001923219 (8:109345122 A>C), RS1001954461 (8:109345355 G>T), RS1003094214 (8:109337942 CTT>C,CTTT)

Disease associations

OMIM: gene MIM:619015 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST003542_207	Night sleep phenotypes	5.000000e-06
GCST003783_8	Multiple system atrophy (pathologically confirmed)	1.000000e-06
GCST009391_414	Metabolite levels	6.000000e-06

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0010387	phosphatidylcholine 38:5 measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL5725124 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,538 (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
CHEMBL1232461	MOLIBRESIB	2	1,538

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

ChEMBL bioactivities

2 potent at pChembl≥5 of 2 total, top 2 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.13	Kd	74	nM	MOLIBRESIB
7.05	IC50	90	nM	MOLIBRESIB

PubChem BioAssay actives

2 with measured affinity, of 7 total; 1 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
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2179182: Binding affinity against ENY2 (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.0740	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
trichostatin A	affects cotreatment, decreases expression	2
Valproic Acid	affects expression, decreases expression	2
Cyclosporine	decreases expression	2
dicrotophos	decreases expression	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression	1
beta-lapachone	decreases expression, increases expression	1
arsenite	affects binding, increases reaction	1
methylparaben	increases expression	1
sodium arsenite	decreases expression	1
beta-methylcholine	affects expression	1
di-n-butylphosphoric acid	affects expression	1
chloropicrin	increases 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	decreases expression	1
abrine	decreases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
STA 9090	decreases expression	1
bisphenol S	affects cotreatment, increases expression	1
NSC 689534	decreases expression, affects binding	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	decreases expression	1
Vorinostat	increases expression	1
Air Pollutants	increases abundance, decreases expression	1
Cannabidiol	decreases expression	1
Carbamazepine	affects expression	1
Copper	affects binding, decreases expression	1
Dexamethasone	affects cotreatment, increases expression	1
Doxorubicin	decreases expression	1
Ethinyl Estradiol	decreases expression	1

ChEMBL screening assays

7 unique, capped per target: 7 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL5697338	Binding	Inhibition of ENY2 (unknown origin) assessed as fold change at 10 uM incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. — Nature

Clinical trials (associated diseases)

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