RCOR3

Summary

RCOR3 (REST corepressor 3, HGNC:25594) is a protein-coding gene on chromosome 1q32.2-q32.3, encoding REST corepressor 3 (Q9P2K3). May act as a component of a corepressor complex that represses transcription.

Predicted to enable enzyme binding activity and transcription corepressor activity. Predicted to be involved in negative regulation of DNA-templated transcription and regulation of transcription by RNA polymerase II. Located in cytosol and nucleoplasm.

Source: NCBI Gene 55758 — RefSeq curated summary.

At a glance

• GWAS associations: 1
• Clinical variants (ClinVar): 72 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001136223

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:25594
Approved symbol	RCOR3
Name	REST corepressor 3
Location	1q32.2-q32.3
Locus type	gene with protein product
Status	Approved
Aliases	FLJ10876
Ensembl gene	ENSG00000117625
Ensembl biotype	protein_coding
OMIM	620464
Entrez	55758

Gene structure

Transcript identifiers

Ensembl transcripts: 28 — 20 protein_coding, 3 nonsense_mediated_decay, 3 retained_intron, 2 protein_coding_CDS_not_defined

ENST00000367005, ENST00000367006, ENST00000419091, ENST00000452621, ENST00000472734, ENST00000485186, ENST00000486666, ENST00000526255, ENST00000528066, ENST00000528408, ENST00000528926, ENST00000529572, ENST00000529763, ENST00000533469, ENST00000534460, ENST00000534478, ENST00000905991, ENST00000905992, ENST00000905993, ENST00000905994, ENST00000905995, ENST00000905996, ENST00000905997, ENST00000905998, ENST00000905999, ENST00000906000, ENST00000942863, ENST00000942864

RefSeq mRNA: 6 — MANE Select: NM_001136223 NM_001136223, NM_001136224, NM_001136225, NM_001350069, NM_001350070, NM_018254

CCDS: CCDS31016, CCDS44312, CCDS44313, CCDS44314

Canonical transcript exons

ENST00000419091 — 12 exons

Exon	Start	End
ENSE00000960298	211289178	211289396
ENSE00001167269	211279238	211279316
ENSE00001197300	211271232	211271309
ENSE00001694980	211313424	211316385
ENSE00002140488	211259366	211259726
ENSE00003475295	211260108	211260164
ENSE00003551446	211276257	211276418
ENSE00003563034	211274210	211274262
ENSE00003586194	211304083	211304140
ENSE00003601146	211312720	211312961
ENSE00003675757	211278117	211278241
ENSE00003688517	211295676	211295753

Expression profiles

Bgee: expression breadth ubiquitous, 284 present calls, max score 97.48.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 29.8531 / max 218.2078, expressed in 1815 samples.

FANTOM5 promoters (13 alternative TSS)

Promoter ID	TPM avg	Samples expressed
8405	19.9750	1803
8413	2.7289	1204
8408	1.8269	1029
8411	1.7428	904
8412	1.3228	820
8403	0.6669	369
8406	0.4729	229
8410	0.4483	237
8407	0.2746	104
8409	0.2177	72

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sperm	CL:0000019	97.48	gold quality
right testis	UBERON:0004534	97.39	gold quality
left testis	UBERON:0004533	97.37	gold quality
hindlimb stylopod muscle	UBERON:0004252	96.90	gold quality
gastrocnemius	UBERON:0001388	96.81	gold quality
muscle of leg	UBERON:0001383	96.59	gold quality
tibia	UBERON:0000979	96.54	gold quality
mucosa of stomach	UBERON:0001199	96.44	gold quality
testis	UBERON:0000473	96.26	gold quality
right lobe of thyroid gland	UBERON:0001119	95.47	gold quality
left lobe of thyroid gland	UBERON:0001120	95.38	gold quality
right uterine tube	UBERON:0001302	95.33	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	95.28	gold quality
thyroid gland	UBERON:0002046	95.19	gold quality
ventricular zone	UBERON:0003053	95.08	gold quality
calcaneal tendon	UBERON:0003701	95.03	gold quality
male germ cell	CL:0000015	94.94	gold quality
biceps brachii	UBERON:0001507	94.91	gold quality
seminal vesicle	UBERON:0000998	94.76	gold quality
body of pancreas	UBERON:0001150	94.75	gold quality
minor salivary gland	UBERON:0001830	94.64	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	94.62	gold quality
metanephros cortex	UBERON:0010533	94.47	gold quality
skin of leg	UBERON:0001511	94.44	gold quality
secondary oocyte	CL:0000655	94.43	gold quality
caput epididymis	UBERON:0004358	94.43	gold quality
muscle organ	UBERON:0001630	94.41	gold quality
skin of abdomen	UBERON:0001416	94.40	gold quality
small intestine Peyer’s patch	UBERON:0003454	94.39	gold quality
left ovary	UBERON:0002119	94.36	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-GEOD-109979	yes	456.64
E-ANND-3	yes	7.30

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

114 targeting RCOR3, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-126-5P	100.00	72.71	3180
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4282	99.99	75.36	6408
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-4803	99.98	71.99	3117
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-551B-5P	99.96	71.28	3493
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-3119	99.92	71.34	2390
HSA-MIR-6508-5P	99.92	70.67	2465
HSA-MIR-1305	99.91	71.43	3443
HSA-MIR-5680	99.91	69.83	3421

Literature-anchored findings (GeneRIF, showing 1)

• The serum RCOR3 levels in SHB, cirrhosis and liver cancer patients were significantly lower than those in the patients with moderate chronic hepatitis B and with mild chronic hepatitis B. (PMID:21765449)

Cross-species orthologs

8 orthologs

Organism	Symbol	Gene ID
danio_rerio	rcor3	ENSDARG00000004502
mus_musculus	Rcor3	ENSMUSG00000037395
rattus_norvegicus	Rcor3	ENSRNOG00000046445
drosophila_melanogaster	CoRest	FBGN0261573
caenorhabditis_elegans		WBGENE00005006
caenorhabditis_elegans		WBGENE00009224
caenorhabditis_elegans		WBGENE00013632
caenorhabditis_elegans	rcor-1	WBGENE00022278

Paralogs (5): RCOR1 (ENSG00000089902), ZNF541 (ENSG00000118156), TRERF1 (ENSG00000124496), MIDEAS (ENSG00000156030), RCOR2 (ENSG00000167771)

Protein

Protein identifiers

REST corepressor 3 — Q9P2K3 (reviewed: Q9P2K3)

All UniProt accessions (8): B4DV59, E9PPC5, E9PQE5, E9PR63, Q9P2K3, H0YDD7, H0YDR8, H0YF22

UniProt curated annotations — full annotation on UniProt →

Function. May act as a component of a corepressor complex that represses transcription.

Subcellular location. Nucleus.

Similarity. Belongs to the CoREST family.

Isoforms (4)

UniProt ID	Names	Canonical?
Q9P2K3-1	1	yes
Q9P2K3-2	2
Q9P2K3-3	3
Q9P2K3-4	4

RefSeq proteins (6): NP_001129695, NP_001129696, NP_001129697, NP_001336998, NP_001336999, NP_060724 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000949	ELM2_dom	Domain
IPR001005	SANT/Myb	Domain
IPR009057	Homeodomain-like_sf	Homologous_superfamily
IPR017884	SANT_dom	Domain
IPR049048	REST_helical	Domain
IPR051066	Trans_reg/Corepressor	Family

Pfam: PF00249, PF01448, PF20878

UniProt features (37 total): helix 7, compositionally biased region 6, modified residue 5, splice variant 5, domain 3, cross-link 3, turn 2, region of interest 2, chain 1, sequence variant 1, strand 1, coiled-coil region 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
4CZZ	X-RAY DIFFRACTION	3

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9P2K3-F1	69.28	0.37

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): 156, 171, 376, 445, 457, 20, 193, 285

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 186 (showing top): MODULE_205, ZHOU_INFLAMMATORY_RESPONSE_LIVE_DN, NAKAMURA_TUMOR_ZONE_PERIPHERAL_VS_CENTRAL_DN, CAIRO_HEPATOBLASTOMA_UP, BOYAULT_LIVER_CANCER_SUBCLASS_G12_UP, GOCC_TRANSCRIPTION_REPRESSOR_COMPLEX, GOCC_TRANSCRIPTION_REGULATOR_COMPLEX, GOCC_HISTONE_DEACETYLASE_COMPLEX, KIM_WT1_TARGETS_DN, GOMF_TRANSCRIPTION_COREPRESSOR_ACTIVITY, WANG_RESPONSE_TO_GSK3_INHIBITOR_SB216763_UP, GOBP_NEGATIVE_REGULATION_OF_NUCLEOBASE_CONTAINING_COMPOUND_METABOLIC_PROCESS, PLASARI_TGFB1_SIGNALING_VIA_NFIC_1HR_DN, FORTSCHEGGER_PHF8_TARGETS_UP, GOMF_TRANSCRIPTION_COREGULATOR_ACTIVITY

GO Biological Process (2): regulation of transcription by RNA polymerase II (GO:0006357), negative regulation of DNA-templated transcription (GO:0045892)

GO Molecular Function (2): transcription corepressor activity (GO:0003714), protein binding (GO:0005515)

GO Cellular Component (5): histone deacetylase complex (GO:0000118), nucleoplasm (GO:0005654), transcription regulator complex (GO:0005667), cytosol (GO:0005829), nucleus (GO:0005634)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
regulation of DNA-templated transcription	2
cellular anatomical structure	2
transcription by RNA polymerase II	1
DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
transcription coregulator activity	1
negative regulation of DNA-templated transcription	1
binding	1
nucleoplasm	1
nuclear protein-containing complex	1
catalytic complex	1
nuclear lumen	1
protein-containing complex	1
cytoplasm	1
intracellular membrane-bounded organelle	1

Protein interactions and networks

STRING

1050 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
RCOR3	KDM1A	O60341	741
RCOR3	HDAC2	Q92769	719
RCOR3	GSE1	Q14687	660
RCOR3	CTBP1	Q13363	650
RCOR3	PHF21B	Q96EK2	639
RCOR3	HMG20A	Q9NP66	634
RCOR3	HDAC1	Q13547	616
RCOR3	HMG20B	Q9P0W2	537
RCOR3	ZBTB33	Q86T24	534
RCOR3	HSPA1A	P08107	522
RCOR3	PHF21A	Q96BD5	502
RCOR3	RCOR2	Q8IZ40	487
RCOR3	ZNF771	Q7L3S4	470
RCOR3	REST	Q13127	464
RCOR3	RSRC2	Q7L4I2	460

IntAct

194 interactions, top by confidence:

A	B	Type	Score
HDAC1	KDM1A	psi-mi:“MI:0914”(association)	0.910
KDM1A	HDAC1	psi-mi:“MI:0914”(association)	0.910
HDAC2	KDM1A	psi-mi:“MI:0914”(association)	0.890
LLGL2	PRKCI	psi-mi:“MI:0914”(association)	0.890
GSE1	RCOR3	psi-mi:“MI:0915”(physical association)	0.860
RCOR3	GSE1	psi-mi:“MI:0915”(physical association)	0.860
HDAC1	CDK2AP1	psi-mi:“MI:0914”(association)	0.840
SNAI1	KDM1A	psi-mi:“MI:0914”(association)	0.830
HDAC1	TNRC18	psi-mi:“MI:0914”(association)	0.790
DYNLL1	BLTP3B	psi-mi:“MI:0914”(association)	0.730
HMG20A	KDM1A	psi-mi:“MI:0914”(association)	0.730
HDAC1	ZNF609	psi-mi:“MI:0914”(association)	0.730
RCOR3	KRT15	psi-mi:“MI:0915”(physical association)	0.700
KRT15	RCOR3	psi-mi:“MI:0915”(physical association)	0.700
CTBP1	CBX4	psi-mi:“MI:0914”(association)	0.700

BioGRID (257): RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid), RCOR3 (Two-hybrid)

ESM2 similar proteins: A4IFB1, B1H1X4, B2RY56, B3MJ69, B3N3F7, B4H732, B4II37, B4J497, B4KLY7, B4LIK8, B4MR46, B4NYV0, B4QCR6, O15042, P49756, P97496, Q02225, Q15233, Q17FR9, Q1LZD9, Q28WQ8, Q2T9I5, Q3UQU0, Q4KLH4, Q4R4J1, Q4V7D7, Q5FVM4, Q5R539, Q5R7X2, Q5RFL9, Q5T8P6, Q5TUF1, Q60436, Q66I22, Q6INH5, Q6NV83, Q6NZN0, Q6P616, Q6PDG5, Q8R326

Diamond homologs: A5PJX4, O75376, P25357, Q0GGX2, Q4KKX4, Q4R2Z8, Q55DP9, Q59E36, Q5FWT8, Q60974, Q6NRZ0, Q6P116, Q8C796, Q8CFE3, Q8IZ40, Q8QG78, Q90WN5, Q9H0D2, Q9H4R4, Q9P2K3, Q9UKL0, Q9WU42, Q9WUB5, Q9Y618, Q3U3N0, Q5REE1, Q5UAK0, Q5ZJ40, Q5ZKT9, Q6PGA0, Q6PJG2, Q7T105, Q8BXJ2, Q8N108, Q8N344, Q96PN7, O94776, Q18919, Q95Y41, Q9R190

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 150 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
Regulation of PTEN gene transcription	7	13.7×	2e-04
Deactivation of the beta-catenin transactivating complex	5	12.8×	3e-03
Negative Regulation of CDH1 Gene Transcription	9	11.9×	3e-05
HDACs deacetylate histones	7	9.2×	1e-03
Potential therapeutics for SARS	6	7.5×	7e-03
Factors involved in megakaryocyte development and platelet production	8	5.8×	5e-03

GO biological processes:

GO term	Partners	Fold	FDR
cell fate commitment	6	12.8×	1e-03
positive regulation of miRNA transcription	6	12.6×	1e-03
negative regulation of neuron differentiation	6	11.8×	1e-03
anatomical structure morphogenesis	8	8.1×	1e-03
transcription by RNA polymerase II	15	7.7×	4e-07
chromatin organization	8	5.8×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	43
Likely benign	3
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

2491 predictions. Top by Δscore:

Variant	Effect	Δscore
1:211271226:CCCCA:C	acceptor_loss	1.0000
1:211271227:CCCA:C	acceptor_loss	1.0000
1:211271228:CCAGG:C	acceptor_loss	1.0000
1:211271230:A:T	acceptor_loss	1.0000
1:211271306:AAATG:A	donor_loss	1.0000
1:211271307:AAT:A	donor_gain	1.0000
1:211271307:AATG:A	donor_loss	1.0000
1:211271308:AT:A	donor_gain	1.0000
1:211271308:ATG:A	donor_loss	1.0000
1:211271309:TGTA:T	donor_loss	1.0000
1:211271310:G:GC	donor_loss	1.0000
1:211271310:G:GG	donor_gain	1.0000
1:211271311:T:G	donor_loss	1.0000
1:211274203:A:AG	acceptor_gain	1.0000
1:211274204:TTGCA:T	acceptor_loss	1.0000
1:211274205:TGCAG:T	acceptor_loss	1.0000
1:211274206:GCA:G	acceptor_loss	1.0000
1:211274207:CAGTG:C	acceptor_loss	1.0000
1:211274208:A:AG	acceptor_gain	1.0000
1:211274208:A:C	acceptor_loss	1.0000
1:211274208:AGT:A	acceptor_gain	1.0000
1:211274208:AGTG:A	acceptor_gain	1.0000
1:211274209:G:A	acceptor_loss	1.0000
1:211274209:G:GA	acceptor_gain	1.0000
1:211274209:GT:G	acceptor_gain	1.0000
1:211274209:GTG:G	acceptor_gain	1.0000
1:211274209:GTGG:G	acceptor_gain	1.0000
1:211274261:AG:A	donor_loss	1.0000
1:211274262:GG:G	donor_loss	1.0000
1:211274263:GTAT:G	donor_loss	1.0000

AlphaMissense

3647 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
1:211260125:G:A	G4R	1.000
1:211260125:G:C	G4R	1.000
1:211260126:G:A	G4E	1.000
1:211260126:G:T	G4V	1.000
1:211271274:T:A	V31E	1.000
1:211271276:T:A	W32R	1.000
1:211271276:T:C	W32R	1.000
1:211271278:G:C	W32C	1.000
1:211271278:G:T	W32C	1.000
1:211274218:T:C	Y46H	1.000
1:211274218:T:G	Y46D	1.000
1:211274230:G:C	A50P	1.000
1:211274231:C:A	A50E	1.000
1:211274248:T:C	Y56H	1.000
1:211274248:T:G	Y56D	1.000
1:211274257:G:A	E59K	1.000
1:211274258:A:T	E59V	1.000
1:211274261:A:C	Q60P	1.000
1:211274262:G:C	Q60H	1.000
1:211274262:G:T	Q60H	1.000
1:211276257:G:C	A61P	1.000
1:211276258:C:A	A61E	1.000
1:211276261:T:C	L62P	1.000
1:211276263:G:C	G63R	1.000
1:211276263:G:T	G63C	1.000
1:211276264:G:A	G63D	1.000
1:211276264:G:T	G63V	1.000
1:211276267:T:A	M64K	1.000
1:211276267:T:C	M64T	1.000
1:211276267:T:G	M64R	1.000

dbSNP variants (sampled 300 via entrez): RS1000027268 (1:211297017 G>A,C), RS1000030453 (1:211296847 T>C), RS1000041038 (1:211289780 C>A,T), RS1000060373 (1:211268189 A>G), RS1000165722 (1:211271108 C>T), RS1000237133 (1:211304310 C>T), RS1000257829 (1:211305029 T>TA), RS1000290190 (1:211311988 G>A), RS1000297851 (1:211270947 C>T), RS1000407422 (1:211311607 A>G), RS1000521317 (1:211284369 T>C), RS1000526145 (1:211260029 ATTTT>A,ATTT,ATTTTT), RS1000588342 (1:211260455 C>A,T), RS1000588486 (1:211304743 T>C), RS1000593967 (1:211291783 C>T)

Disease associations

OMIM: gene MIM:620464 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

1 associations (top):

Study	Trait	p-value
GCST90002400_540	Plateletcrit	1.000000e-09

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0007985	platelet crit

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL4296112 (PROTEIN COMPLEX), CHEMBL4296114 (PROTEIN COMPLEX), CHEMBL6195596 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 50,431 (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
CHEMBL98	VORINOSTAT	4	50,361
CHEMBL3989843	TRANYLCYPROMINE	4	70

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

ChEMBL bioactivities

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

pChembl	Type	Value	Unit	Molecule
8.52	Ki	3.04	nM	VORINOSTAT
7.57	Ki	26.87	nM	CHEMBL4228572
7.37	Ki	42.52	nM	CHEMBL4228166
5.62	IC50	2400	nM	CHEMBL4228572
5.42	IC50	3850	nM	CHEMBL4228166

PubChem BioAssay actives

5 with measured affinity, of 10 total; 3 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
Vorinostat	1389960: Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay	ki	0.0030	uM
N-[4-[3-[3-[[4-[4-[(1S,2R)-2-aminocyclopropyl]anilino]-4-oxobutanoyl]amino]propylamino]propylcarbamoyl]phenyl]-N’-hydroxyoctanediamide;dihydrochloride	1389960: Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay	ki	0.0269	uM
N-[4-[3-[4-[3-[[4-[4-[(1S,2R)-2-aminocyclopropyl]anilino]-4-oxobutanoyl]amino]propylamino]butylamino]propylcarbamoyl]phenyl]-N’-hydroxyoctanediamide;trihydrochloride	1389960: Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay	ki	0.0425	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	increases methylation, decreases expression, increases expression, affects cotreatment	3
sodium arsenite	increases expression, decreases expression, increases abundance	3
GSK-J4	increases expression	1
FR900359	increases phosphorylation	1
bisphenol F	affects cotreatment, increases expression	1
TAK-243	decreases sumoylation	1
alpha-pinene	affects cotreatment, increases oxidation, increases abundance	1
geraniol	increases expression	1
trichostatin A	affects expression	1
2-butenal	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
manganese chloride	increases abundance, increases expression	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	affects cotreatment, decreases expression	1
coumarin	increases phosphorylation	1
methacrylaldehyde	increases abundance, affects cotreatment, increases oxidation	1
di-n-butylphosphoric acid	affects expression	1
abrine	increases expression	1
bisphenol S	increases expression, affects cotreatment	1
Fulvestrant	affects cotreatment, increases methylation	1
Leflunomide	increases expression	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1
Air Pollutants	affects cotreatment, increases abundance, increases oxidation	1
Ethanol	decreases expression, increases abundance, affects cotreatment	1
Arsenic	increases abundance, increases expression	1
Caffeine	decreases phosphorylation	1
Coumestrol	decreases expression, affects cotreatment	1
Dexamethasone	affects cotreatment, increases expression	1
Dimethyl Sulfoxide	increases expression	1
Gasoline	affects cotreatment, decreases expression, increases abundance	1
Hydrogen Peroxide	affects expression	1

ChEMBL screening assays

3 unique, capped per target: 3 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL4221523	Binding	Inhibition of HDAC1/CoREST3 in HEK293 whole cell extract using fluorescent acetylated histone peptide as substrate after 60 mins by fluorescence based assay	Novel polyamine-based Histone deacetylases-Lysine demethylase 1 dual binding inhibitors. — Bioorg Med Chem Lett

Clinical trials (associated diseases)

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