HDAC7

Summary

HDAC7 (histone deacetylase 7, HGNC:14067) is a protein-coding gene on chromosome 12q13.11, encoding Histone deacetylase 7 (Q8WUI4). Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4).

Histones play a critical role in transcriptional regulation, cell cycle progression, and developmental events. Histone acetylation/deacetylation alters chromosome structure and affects transcription factor access to DNA. The protein encoded by this gene has sequence homology to members of the histone deacetylase family. This gene is orthologous to mouse HDAC7 gene whose protein promotes repression mediated via the transcriptional corepressor SMRT. Alternatively spliced transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 51564 — RefSeq curated summary.

At a glance

• GWAS associations: 42
• Clinical variants (ClinVar): 192 total
• Druggable target: yes — 28 molecules with ChEMBL bioactivity
• Transcription factor: yes — 13 downstream targets (CollecTRI)
• MANE Select transcript: NM_015401

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14067
Approved symbol	HDAC7
Name	histone deacetylase 7
Location	12q13.11
Locus type	gene with protein product
Status	Approved
Aliases	DKFZP586J0917
Ensembl gene	ENSG00000061273
Ensembl biotype	protein_coding
OMIM	606542
Entrez	51564

Gene structure

Transcript identifiers

Ensembl transcripts: 38 — 25 protein_coding, 6 nonsense_mediated_decay, 5 retained_intron, 2 protein_coding_CDS_not_defined

ENST00000080059, ENST00000354334, ENST00000380610, ENST00000417107, ENST00000417902, ENST00000421231, ENST00000422254, ENST00000425451, ENST00000427332, ENST00000430670, ENST00000433685, ENST00000434070, ENST00000440293, ENST00000445237, ENST00000447463, ENST00000450805, ENST00000459625, ENST00000463732, ENST00000470668, ENST00000471235, ENST00000477203, ENST00000477937, ENST00000485796, ENST00000488927, ENST00000491464, ENST00000547259, ENST00000548080, ENST00000548938, ENST00000549883, ENST00000552960, ENST00000903431, ENST00000903432, ENST00000903433, ENST00000903434, ENST00000903435, ENST00000903436, ENST00000903437, ENST00000903438

RefSeq mRNA: 4 — MANE Select: NM_015401 NM_001098416, NM_001308090, NM_001368046, NM_015401

CCDS: CCDS41776, CCDS81685, CCDS8756

Canonical transcript exons

ENST00000080059 — 26 exons

Exon	Start	End
ENSE00000888040	47795906	47796016
ENSE00001853912	47782722	47783886
ENSE00001862271	47819767	47819903
ENSE00003459640	47798108	47798219
ENSE00003460861	47791871	47792004
ENSE00003474618	47795184	47795380
ENSE00003488616	47798562	47798652
ENSE00003491961	47789813	47789920
ENSE00003506538	47788045	47788164
ENSE00003512342	47798785	47798972
ENSE00003581790	47802224	47802274
ENSE00003599876	47789261	47789348
ENSE00003626481	47796207	47796298
ENSE00003641521	47785752	47785885
ENSE00003642796	47795587	47795767
ENSE00003658111	47785387	47785471
ENSE00003662696	47786585	47786703
ENSE00003664202	47789523	47789578
ENSE00003667866	47793369	47793588
ENSE00003674845	47794760	47794933
ENSE00003677330	47791259	47791308
ENSE00003688194	47784079	47784217
ENSE00003690258	47797017	47797142
ENSE00003691273	47787712	47787809
ENSE00003692328	47791586	47791706
ENSE00003785951	47797384	47797499

Expression profiles

Bgee: expression breadth ubiquitous, 282 present calls, max score 97.55.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 43.3751 / max 398.3701, expressed in 1813 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
130698	36.7470	1806
130699	5.7667	1648
206684	0.3999	169
130700	0.3339	163
130697	0.0928	23
130701	0.0347	13

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	97.55	gold quality
mucosa of stomach	UBERON:0001199	97.23	gold quality
metanephros cortex	UBERON:0010533	97.23	gold quality
left uterine tube	UBERON:0001303	97.13	gold quality
body of uterus	UBERON:0009853	97.03	gold quality
apex of heart	UBERON:0002098	97.02	gold quality
upper lobe of left lung	UBERON:0008952	96.97	gold quality
lower esophagus muscularis layer	UBERON:0035833	96.96	gold quality
lower esophagus	UBERON:0013473	96.94	gold quality
left adrenal gland cortex	UBERON:0035825	96.82	gold quality
endocervix	UBERON:0000458	96.77	gold quality
right ovary	UBERON:0002118	96.77	gold quality
right uterine tube	UBERON:0001302	96.68	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	96.66	gold quality
peripheral nervous system	UBERON:0000010	96.60	gold quality
nerve	UBERON:0001021	96.60	gold quality
tibial nerve	UBERON:0001323	96.60	gold quality
adrenal cortex	UBERON:0001235	96.56	gold quality
left adrenal gland	UBERON:0001234	96.54	gold quality
left ovary	UBERON:0002119	96.54	gold quality
right lung	UBERON:0002167	96.54	gold quality
right lobe of thyroid gland	UBERON:0001119	96.53	gold quality
right adrenal gland	UBERON:0001233	96.53	gold quality
right coronary artery	UBERON:0001625	96.37	gold quality
right adrenal gland cortex	UBERON:0035827	96.34	gold quality
ascending aorta	UBERON:0001496	96.33	gold quality
thoracic aorta	UBERON:0001515	96.31	gold quality
descending thoracic aorta	UBERON:0002345	96.26	gold quality
omental fat pad	UBERON:0010414	96.26	gold quality
peritoneum	UBERON:0002358	96.25	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-HCAD-6	yes	53.55
E-ANND-3	yes	11.75

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

13 targets.

Target	Regulation
ACTN4	Repression
AKAP12	Repression
CDKN1A	Activation
CYP7A1	Unknown
ESR1	Repression
HDC	Repression
HIF1A	Activation
MAML1	Unknown
MEF2A	Repression
MEF2C	Repression
MEF2D	Repression
MMP10	Repression
NR4A1	Unknown

Upstream regulators (CollecTRI, top): BCL6, MECP2, MEF2D, NFKB1, RELA, SP1, STAT1

miRNA regulators (miRDB)

61 targeting HDAC7, 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-8485	100.00	77.57	4731
HSA-MIR-5193	100.00	67.26	1744
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-9-3P	99.96	70.88	2068
HSA-MIR-23A-3P	99.95	74.24	3163
HSA-MIR-23B-3P	99.95	74.24	3163
HSA-MIR-23C	99.95	73.92	3192
HSA-MIR-96-5P	99.95	72.80	2140
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-12133	99.92	71.82	2006
HSA-MIR-6768-5P	99.92	67.36	1942
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-1271-5P	99.91	71.99	1972
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-6875-3P	99.82	70.26	2983
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-3150A-3P	99.76	64.44	1640
HSA-MIR-6763-5P	99.76	64.68	1767
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-92A-2-5P	99.75	67.01	2164
HSA-MIR-4422	99.72	72.07	2908
HSA-MIR-6766-5P	99.68	67.70	2325
HSA-MIR-6887-3P	99.66	67.83	1778
HSA-MIR-3175	99.65	66.30	2031
HSA-MIR-9851-3P	99.63	69.68	1110
HSA-MIR-7112-5P	99.59	65.76	104
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-4649-3P	99.56	66.90	1783
HSA-MIR-5689	99.50	71.26	1154

Literature-anchored findings (GeneRIF, showing 40)

• Characterization of the mouse HDAC7 ortholog. (PMID:10640276)
• Class II histone deacetylases are directly recruited by BCL6 transcriptional repressor (PMID:11929873)
• Interaction of HDAC7 with MEF2D is essential for repression of Nur77. (PMID:12753745)
• HDAC7 phosphorylation is mediated by calcium/calmodulin-dependent kinase I, which also promotes the association of HDAC7 with 14-3-3 and stabilizes HDAC7 (PMID:15166223)
• HDAC7 increased transcriptional activity of HIF-1alpha through the formation of a complex with HIF-1alpha, HDAC7, and p300 (PMID:15280364)
• HDAC7 is sequestered to the cytoplasm from mitochondrial and nuclear compartments upon initiation of apoptosis (PMID:15364908)
• Data indicate that protein kinase D1 regulates the expression of Nur77 during thymocyte activation at least in part by phosphorylating HDAC7. (PMID:15623513)
• a mutant of HDAC7 specifically deficient in phosphorylation by protein kinase D, inhibits T cell receptor-mediated apoptosis of T cell hybridomas (PMID:15738054)
• These results identify HDAC7 as a novel Androgen receptor corepressor whose subcellular and subnuclear compartmentalization can be regulated in an androgen-selective manner. (PMID:16860317)
• Class IIa histone deacetylases (HDACs) are subjected to signal-independent nuclear export that relies on their constitutive phosphorylation. EMK and C-TAK1, are identified as regulators of this process. (PMID:16980613)
• HDAC7 is a key modulator of endothelial cell migration and angiogenesis, at least in part, by regulating platelet-derived growth factor-B (PDGF-B) and its receptor PDGFR-beta gene expression. (PMID:17947801)
• Histone deacetylase 7 associates with Runx2 and represses its activity during osteoblast maturation in a deacetylation-independent manner (PMID:17997710)
• HDAC7 has a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity (PMID:18285338)
• PP2A constitutively dephosphorylates the class IIa member HDAC7 to control its biological functions as a regulator of T cell apoptosis and endothelial cell functions. (PMID:18339811)
• Caspase-8 cleaves histone deacetylase 7 and abolishes its transcription repressor function. (PMID:18458084)
• PML sequesters HDAC7 to relieve repression and up-regulate gene expression (PMID:18463162)
• The data showed alteration of HDACs gene expression in pancreatic cancer. Increased expression of HDAC7 discriminates PA from other pancreatic tumors. (PMID:18506539)
• These results demonstrate that phosphorylation of HDAC7 serves as a molecular switch to mediate VEGF signaling and endothelial function. (PMID:18509061)
• VEGF stimulates HDAC7 phosphorylation and cytoplasmic accumulation modulating MT-MMP1/MMP10 expression and angiogenesis. (PMID:18617643)
• These results demonstrate a novel function of HDAC7 and provide a regulatory mechanism of PML sumoylation. (PMID:18625722)
• recent developments in the crystal structure analysis of human HDAC4, HDAC7, and HDAC8 recent developments in the crystal structure analysis of human HDAC4, HDAC7, and HDAC8 [REVIEW] (PMID:19355988)
• Elevated HDAC7 expression in human osteoarthritis may contribute to cartilage degradation via promoting MMP-13 gene expression. (PMID:19784544)
• these data implicate a novel role for HDAC7 and FoxA1 in estrogen repression of RPRM. (PMID:19917725)
• histone deacetylase 7 has a role in function of misfolded CFTR in cystic fibrosis (PMID:19966789)
• HDAC7 interacts with beta-catenin keeping endothelial cells in a low proliferation stage. (PMID:20224040)
• The expression of HDAC7 protein plays an important role in the apoptosis and vascular tubulogenesis of hepatocellular carcinoma by the upregulation of p21 and HIF-1alpha and the downregulation of cyclin E and MMP10. (PMID:20693714)
• Findings highlight for the first time an unrecognized link between HDAC7 and c-Myc and offer a novel mechanistic insight into the contribution of HDAC7 to tumor progression. (PMID:21120446)
• Data demonstrate that Mitf and HDAC7 interact in RAW 264 cells and osteoclasts. The transcriptional activity of Mitf is repressed by HDAC7. (PMID:21324898)
• HDAC7 reduction in COPD causes a defect of HIF-1alpha induction response to hypoxia with impaired VEGF gene expression. This poor cellular adaptation might play a role in the pathogenesis of COPD. (PMID:22172637)
• demonstrated for the first time that AKAP12 tumor/angiogenesis suppressor gene is an epigenetic target of HDAC7 (PMID:22584896)
• VEGF and PKC promote degradation-independent protein ubiquitination of FLNB to control intracellular trafficking of HDAC7. (PMID:23401860)
• Our findings uncover a novel role for HDAC7 in maintaining the identity of a particular cell type by silencing lineage-inappropriate genes. (PMID:23696748)
• Histone deacetylase 7 promotes Toll-like receptor 4-dependent proinflammatory gene expression in macrophages. (PMID:23853092)
• Authors identified acetyltransferase p300 and deacetylase HDAC7 as enzymes modulating human T cell leukemia virus type 1 Tax protein acetylation. (PMID:23880157)
• Expression of JHDM2A was significantly increased but HDAC2, HDAC7, and SUV39H2 were significantly down-regulated in Systemic Sclerosis B cells relative to controls (PMID:23891737)
• endothelial progenitor cells involved in the angiogenesis might be controlled by VEGF-PKD1-HDAC7 axis, which regulates the EPCs angiogenesis by PKD1, but not the ERK and PI3K pathway (PMID:24189120)
• The transcriptional function of HCS was shown by in vitro pull down and in vivo co-immunoprecipitation assays to depend on its interaction with the histone deacetylases HDAC1, HDAC2 and HDAC7 (PMID:24239178)
• Study identifies the miR-34a-HDAC1/HDAC7-HSP70 K246 axis as a novel molecular signature predictive of therapy resistance. (PMID:25173798)
• identify a new target of ROCK signaling via myosin phosphatase subunit (MYPT1) and histone deacetylase (HDAC7) at the nuclear level (PMID:25511694)
• This study demonstrated a simple and straightforward method of quantifying proneural/mesenchymal markers in glioblastoma. Of note, HDAC7 expression might be a novel therapeutic target in glioblastoma treatment. (PMID:26272600)

Cross-species orthologs

7 orthologs

Organism	Symbol	Gene ID
danio_rerio	hdac7b	ENSDARG00000073850
danio_rerio	hdac7a	ENSDARG00000105179
mus_musculus	Hdac7	ENSMUSG00000022475
rattus_norvegicus	Hdac7	ENSRNOG00000055597
caenorhabditis_elegans		WBGENE00009657
caenorhabditis_elegans		WBGENE00009663
caenorhabditis_elegans		WBGENE00219378

Paralogs (10): HDAC9 (ENSG00000048052), HDAC4 (ENSG00000068024), HDAC6 (ENSG00000094631), HDAC10 (ENSG00000100429), HDAC5 (ENSG00000108840), HDAC1 (ENSG00000116478), HDAC8 (ENSG00000147099), HDAC11 (ENSG00000163517), HDAC3 (ENSG00000171720), HDAC2 (ENSG00000196591)

Protein

Protein identifiers

Histone deacetylase 7 — Q8WUI4 (reviewed: Q8WUI4)

Alternative names: Histone deacetylase 7A, Protein deacetylase HDAC7

All UniProt accessions (19): Q8WUI4, A0A087WYQ4, C9J102, C9JAH2, C9JBC2, C9JEB6, C9JF80, C9JGF5, C9JH46, C9JKN3, C9JNI4, C9JVZ1, C9JZ79, F8VWY3, H0YH91, H0YHJ5, H0YI15, H0YI41, J3KPH8

UniProt curated annotations — full annotation on UniProt →

Function. Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Involved in muscle maturation by repressing transcription of myocyte enhancer factors such as MEF2A, MEF2B and MEF2C. During muscle differentiation, it shuttles into the cytoplasm, allowing the expression of myocyte enhancer factors. May be involved in Epstein-Barr virus (EBV) latency, possibly by repressing the viral BZLF1 gene. Positively regulates the transcriptional repressor activity of FOXP3. Serves as a corepressor of RARA, causing its deacetylation and inhibition of RARE DNA element binding. In association with RARA, plays a role in the repression of microRNA-10a and thereby in the inflammatory response. Also acetylates non-histone proteins, such as ALKBH5.

Subunit / interactions. Interacts with HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, NCOR1, NCOR2, SIN3A, SIN3B, RBBP4, RBBP7, MTA1L1, SAP30 and MBD3. Interacts with KAT5 and EDNRA. Interacts with the 14-3-3 protein YWHAE, MEF2A, MEF2B and MEF2C. Interacts with ZMYND15. Interacts with KDM5B. Interacts with PML. Interacts with FOXP3. Interacts with RARA.

Subcellular location. Nucleus. Cytoplasm.

Post-translational modifications. May be phosphorylated by CaMK1. Phosphorylated by the PKC kinases PKN1 and PKN2, impairing nuclear import. Phosphorylation at Ser-155 by MARK2, MARK3 and PRKD1 promotes interaction with 14-3-3 proteins and export from the nucleus. Phosphorylation at Ser-155 is a prerequisite for phosphorylation at Ser-181.

Similarity. Belongs to the histone deacetylase family. HD type 2 subfamily.

Isoforms (10)

UniProt ID	Names	Canonical?
Q8WUI4-1	1	yes
Q8WUI4-2	2
Q8WUI4-3	3
Q8WUI4-4	4
Q8WUI4-5	5
Q8WUI4-6	6
Q8WUI4-7	7
Q8WUI4-8	8
Q8WUI4-9	9
Q8WUI4-10	10

RefSeq proteins (4): NP_001091886, NP_001295019, NP_001354975, NP_056216* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000286	HDACs	Family
IPR023696	Ureohydrolase_dom_sf	Homologous_superfamily
IPR023801	His_deacetylse_dom	Domain
IPR037138	His_deacetylse_dom_sf	Homologous_superfamily
IPR046949	HDAC4/5/7/9	Family

Pfam: PF00850

Enzyme classification (BRENDA):

• EC 3.5.1.98 — histone deacetylase (BRENDA: 33 organisms, 161 substrates, 590 inhibitors, 88 Km, 32 kcat entries)

Substrate kinetics (BRENDA)

32 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
FLUOR DE LYS HDAC8 SUBSTRATE	0.14–1.1	9
AC-KHK(ACETYL)K(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.273–2.403	6
FLUOR DE LYS HDAC SUBSTRATE	0.013–0.088	6
AC-FEK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0023–0.0359	5
AC-GGK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0043–0.0877	5
AC-GS(PO3)K(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0123–0.0666	5
AC-GSK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.004–0.0241	5
AC-IHK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0007–0.108	5
AC-KYK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0044–0.107	4
FLUOR DE LYS	—	4
AC-LYK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0069–0.03	3
AC-VLK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0119–0.0221	3
RHK(ACETYL)K(ACETYL)-FLUOROPHORE	0.16–1.1	3
AC-DQK(ACETYL)-7-AMIDO-4-METHYLCOUMARIN	0.0024–0.0165	2
BENZYLOXYCARBONYL-L-LYS(ACETYL)-7-AMIDO-4-METHYL	0.078–0.099	2

Catalyzed reactions (Rhea), 2 shown:

• N(6)-acetyl-L-lysyl-[protein] + H2O = L-lysyl-[protein] + acetate (RHEA:58108)
• N(6)-acetyl-L-lysyl-[histone] + H2O = L-lysyl-[histone] + acetate (RHEA:58196)

UniProt features (101 total): helix 21, modified residue 12, strand 12, sequence conflict 11, region of interest 10, splice variant 10, mutagenesis site 8, compositionally biased region 4, binding site 4, turn 4, chain 1, short sequence motif 1, active site 1, site 1, sequence variant 1

Structure

Experimental structures (PDB)

6 structures.

PDB	Method	Resolution (Å)
3C10	X-RAY DIFFRACTION	2
3C0Y	X-RAY DIFFRACTION	2.1
3C0Z	X-RAY DIFFRACTION	2.1
8Q9Q	X-RAY DIFFRACTION	2.11
3ZNR	X-RAY DIFFRACTION	2.4
3ZNS	X-RAY DIFFRACTION	2.45

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8WUI4-F1	62.90	0.36

Functional residue map

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

Catalytic / active sites (2): 670; 843 (contributes to catalysis)

Ligand- & substrate-binding residues (4): 533; 535; 541; 618

Post-translational modifications (12): 109, 155, 181, 283, 286, 358, 364, 405, 486, 487, 507, 595

Mutagenesis-validated functional residues (8):

Position	Phenotype
150	abolishes phosphorylation at s-155.
155	abolishes nuclear export; when associated with a-181; a-358 and a-486. abolishes phosphorylation by mark2 and mark3, int
181	abolishes nuclear export; when associated with a-155; a-358 and a-486.
358	abolishes nuclear export; when associated with a-192; a-1118 and a-486.
486	abolishes nuclear export; when associated with a-192; a-1118 and a-358.
843	enhanced deacetylase activity.
843	6000 fold increase in deacetylase activity.

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-2122947	NOTCH1 Intracellular Domain Regulates Transcription
R-HSA-2644606	Constitutive Signaling by NOTCH1 PEST Domain Mutants
R-HSA-2894862	Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
R-HSA-3108214	SUMOylation of DNA damage response and repair proteins
R-HSA-350054	Notch-HLH transcription pathway
R-HSA-8943724	Regulation of PTEN gene transcription
R-HSA-9976102	Differentiation of naive CD4+ T cells to T helper 2 cells (Th2 cells)

MSigDB gene sets: 291 (showing top): PID_HDAC_CLASSI_PATHWAY, REACTOME_SIGNALING_BY_NOTCH, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, GOBP_CELL_MIGRATION_INVOLVED_IN_SPROUTING_ANGIOGENESIS, GRAESSMANN_RESPONSE_TO_MC_AND_DOXORUBICIN_DN, GOBP_MACROMOLECULE_DEACYLATION, GOBP_OSTEOBLAST_DIFFERENTIATION, MEF2_02, GOBP_NEGATIVE_REGULATION_OF_INTRACELLULAR_SIGNAL_TRANSDUCTION, GOBP_POSITIVE_REGULATION_OF_ENDOTHELIAL_CELL_MIGRATION, GOBP_BLOOD_VESSEL_ENDOTHELIAL_CELL_MIGRATION, GOBP_PEPTIDYL_LYSINE_MODIFICATION, LIU_VAV3_PROSTATE_CARCINOGENESIS_DN, GOBP_NEGATIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_CELL_JUNCTION_ORGANIZATION

GO Biological Process (15): negative regulation of transcription by RNA polymerase II (GO:0000122), vasculogenesis (GO:0001570), protein deacetylation (GO:0006476), cell-cell junction assembly (GO:0007043), protein sumoylation (GO:0016925), negative regulation of interleukin-2 production (GO:0032703), epigenetic regulation of gene expression (GO:0040029), negative regulation of osteoblast differentiation (GO:0045668), regulation of mRNA processing (GO:0050684), positive regulation of cell migration involved in sprouting angiogenesis (GO:0090050), negative regulation of non-canonical NF-kappaB signal transduction (GO:1901223), chromatin organization (GO:0006325), negative regulation of macromolecule biosynthetic process (GO:0010558), negative regulation of DNA-templated transcription (GO:0045892), membraneless organelle assembly (GO:0140694)

GO Molecular Function (13): chromatin binding (GO:0003682), transcription corepressor activity (GO:0003714), histone deacetylase activity (GO:0004407), protein kinase C binding (GO:0005080), SUMO transferase activity (GO:0019789), protein kinase binding (GO:0019901), protein lysine deacetylase activity (GO:0033558), metal ion binding (GO:0046872), 14-3-3 protein binding (GO:0071889), DNA-binding transcription factor binding (GO:0140297), histone deacetylase activity, hydrolytic mechanism (GO:0141221), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (5): histone deacetylase complex (GO:0000118), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829)

Reactome top-level categories

Rollup of top-7 pathways:

Category	Pathways
Signaling by NOTCH1	1
Signaling by NOTCH1 PEST Domain Mutants in Cancer	1
Signaling by NOTCH1 HD+PEST Domain Mutants in Cancer	1
SUMO E3 ligases SUMOylate target proteins	1
Generic Transcription Pathway	1
PTEN Regulation	1
Differentiation of T cells	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
negative regulation of DNA-templated transcription	2
binding	2
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
cell differentiation	1
blood vessel morphogenesis	1
protein deacylation	1
cell junction assembly	1
cell-cell junction organization	1
peptidyl-lysine modification	1
protein modification by small protein conjugation	1
negative regulation of cytokine production	1
interleukin-2 production	1
regulation of interleukin-2 production	1
chromatin remodeling	1
regulation of gene expression	1
osteoblast differentiation	1
negative regulation of cell differentiation	1
regulation of osteoblast differentiation	1
mRNA processing	1
regulation of mRNA metabolic process	1
cell migration involved in sprouting angiogenesis	1
positive regulation of blood vessel endothelial cell migration	1
regulation of cell migration involved in sprouting angiogenesis	1
non-canonical NF-kappaB signal transduction	1
regulation of non-canonical NF-kappaB signal transduction	1
negative regulation of intracellular signal transduction	1
cellular component organization	1
macromolecule biosynthetic process	1
negative regulation of biosynthetic process	1
regulation of macromolecule biosynthetic process	1
negative regulation of macromolecule metabolic process	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
organelle assembly	1
transcription coregulator activity	1
protein lysine deacetylase activity	1
histone modifying activity	1

Protein interactions and networks

STRING

2548 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
HDAC7	KAT5	Q92993	969
HDAC7	FOXA1	P55317	954
HDAC7	FOXP3	Q9BZS1	936
HDAC7	NCOR1	O75376	869
HDAC7	HIF1A	Q16665	855
HDAC7	MEF2A	Q02078	847
HDAC7	EP300	Q09472	837
HDAC7	MEF2D	Q14814	804
HDAC7	MMP10	P09238	803
HDAC7	SIRT1	Q96EB6	780
HDAC7	NR4A1	P22736	688
HDAC7	BCORL1	Q5H9F3	685
HDAC7	DNMT1	P26358	674
HDAC7	CTBP1	Q13363	670
HDAC7	BCL6	P41182	638

IntAct

208 interactions, top by confidence:

A	B	Type	Score
HDAC7	YWHAG	psi-mi:“MI:0915”(physical association)	0.890
YWHAH	ABLIM1	psi-mi:“MI:0914”(association)	0.800
YWHAZ	HDAC7	psi-mi:“MI:0915”(physical association)	0.800
HDAC7	SFN	psi-mi:“MI:0915”(physical association)	0.690
HDAC7	PRKD2	psi-mi:“MI:0915”(physical association)	0.640
PRKD2	HDAC7	psi-mi:“MI:0915”(physical association)	0.640
HDAC7	PRKD2	psi-mi:“MI:0217”(phosphorylation reaction)	0.640
EGFR	HDAC7	psi-mi:“MI:0915”(physical association)	0.630
YWHAH	PLEKHG3	psi-mi:“MI:0914”(association)	0.610
YWHAG	SHTN1	psi-mi:“MI:0914”(association)	0.560
HDAC7	CALCOCO2	psi-mi:“MI:0915”(physical association)	0.550
HDAC7	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.550
YWHAQ	IGLC7	psi-mi:“MI:0914”(association)	0.530
BAG2	HGS	psi-mi:“MI:0914”(association)	0.530
ICP0	HDAC7	psi-mi:“MI:0915”(physical association)	0.520
Mef2c	HDAC7	psi-mi:“MI:0914”(association)	0.500
Mef2c	HDAC7	psi-mi:“MI:0915”(physical association)	0.500
YWHAB	PLEKHG3	psi-mi:“MI:0914”(association)	0.480
YWHAQ	PLEKHG3	psi-mi:“MI:0914”(association)	0.480
SDCBP	HDAC7	psi-mi:“MI:0407”(direct interaction)	0.440
HDAC7	PARD3	psi-mi:“MI:0407”(direct interaction)	0.440
HDAC7	HTRA1	psi-mi:“MI:0407”(direct interaction)	0.440
HDAC7	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (249): HDAC7 (Affinity Capture-Western), HDAC7 (Two-hybrid), HDAC7 (Two-hybrid), RIPPLY1 (Two-hybrid), HDAC7 (Affinity Capture-RNA), HDAC7 (Affinity Capture-RNA), HDAC7 (Affinity Capture-RNA), HDAC7 (Two-hybrid), FLYWCH2 (Affinity Capture-MS), ZYG11B (Affinity Capture-MS), HINT1 (Affinity Capture-MS), ZMYM6 (Affinity Capture-MS), TTF2 (Affinity Capture-MS), RAP1GDS1 (Affinity Capture-MS), MOCOS (Affinity Capture-MS)

ESM2 similar proteins: A2ARK0, A3KN19, A6ND36, E9Q0S6, E9Q2Z1, G5E5X0, O70405, O75385, O94983, O95402, P42335, Q04205, Q08EC4, Q32PJ7, Q3UJB9, Q3ZAV8, Q5D1E7, Q5D1E8, Q5PQS0, Q5SSZ5, Q5SWY7, Q5XIS1, Q5XK72, Q63HR2, Q68CZ2, Q6P2E9, Q6PDH0, Q7TSI1, Q80Y50, Q86UU1, Q8BG26, Q8C2B3, Q8CGB6, Q8IUC6, Q8K1S6, Q8K2P2, Q8K330, Q8TE77, Q8TF72, Q8WUI4

Diamond homologs: A0A8I6GM68, D2HBJ8, F1QCV2, O17323, O27262, O30107, P28606, P38748, P53973, P56523, P56524, P72702, P83038, Q09440, Q0V9G5, Q20296, Q2QWU2, Q3JUN4, Q54QE6, Q569C4, Q57955, Q5A960, Q5R902, Q5XGZ2, Q613L4, Q6NTR6, Q6NZM9, Q6P3E7, Q6P9L4, Q70CQ1, Q70I53, Q7Z569, Q7ZUM8, Q80ZH1, Q8C2B3, Q8C2S0, Q8GXJ1, Q8LRK8, Q8RX28, Q8WUI4

SIGNOR signaling

42 interactions.

A	Effect	B	Mechanism
PRKD1	down-regulates	HDAC7	phosphorylation
HDAC7	down-regulates	PLAG1	deacetylation
HDAC7	down-regulates	PLAGL2	deacetylation
MAP3K7	down-regulates	HDAC7	phosphorylation
MARK2	down-regulates	HDAC7	phosphorylation
PRKAA1	down-regulates	HDAC7	phosphorylation
AMPK	down-regulates	HDAC7	phosphorylation
PPP2CB	“up-regulates activity”	HDAC7	dephosphorylation
PPP2CA	“up-regulates activity”	HDAC7	dephosphorylation
BCORL1	“up-regulates activity”	HDAC7	binding
PRKD1	unknown	HDAC7	phosphorylation
belinostat	“down-regulates activity”	HDAC7	“chemical inhibition”
panobinostat	“down-regulates activity”	HDAC7	“chemical inhibition”
“N-[4-[(hydroxyamino)-oxomethyl]phenyl]carbamic acid [6-(diethylaminomethyl)-2-naphthalenyl]methyl ester”	“down-regulates activity”	HDAC7	“chemical inhibition”
vorinostat	“down-regulates activity”	HDAC7	“chemical inhibition”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 139 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
Activation of BAD and translocation to mitochondria	6	50.2×	5e-08
Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex	6	44.3×	1e-07
SARS-CoV-1 targets host intracellular signalling and regulatory pathways	6	44.3×	1e-07
Activation of BH3-only proteins	6	32.7×	7e-07
Ras activation upon Ca2+ influx through NMDA receptor	5	31.4×	1e-05
Unblocking of NMDA receptors, glutamate binding and activation	5	29.9×	1e-05
Negative regulation of NMDA receptor-mediated neuronal transmission	5	29.9×	1e-05
Assembly and cell surface presentation of NMDA receptors	10	27.9×	3e-10

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	50.3×	7e-14
protein localization to synapse	6	36.2×	2e-06
receptor clustering	7	34.4×	4e-07
regulation of postsynaptic membrane neurotransmitter receptor levels	7	27.3×	1e-06
protein targeting	7	20.2×	6e-06
Rho protein signal transduction	5	9.8×	6e-03
regulation of small GTPase mediated signal transduction	8	9.1×	2e-04
cell-cell adhesion	11	8.8×	6e-06

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	147
Likely benign	9
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

4167 predictions. Top by Δscore:

Variant	Effect	Δscore
12:47785385:A:AC	donor_gain	1.0000
12:47785386:C:CG	donor_gain	1.0000
12:47785387:TGTG:T	donor_gain	1.0000
12:47785467:TCCAC:T	acceptor_gain	1.0000
12:47785468:CCAC:C	acceptor_gain	1.0000
12:47785468:CCACC:C	acceptor_gain	1.0000
12:47785469:CAC:C	acceptor_gain	1.0000
12:47785469:CACC:C	acceptor_gain	1.0000
12:47785470:AC:A	acceptor_gain	1.0000
12:47785471:CC:C	acceptor_gain	1.0000
12:47785472:C:CC	acceptor_gain	1.0000
12:47785472:C:CG	acceptor_loss	1.0000
12:47785474:A:AC	acceptor_gain	1.0000
12:47785474:A:C	acceptor_gain	1.0000
12:47785750:AC:A	donor_gain	1.0000
12:47785751:CC:C	donor_gain	1.0000
12:47785882:AAAC:A	acceptor_gain	1.0000
12:47785886:C:CC	acceptor_gain	1.0000
12:47785886:CTAGA:C	acceptor_loss	1.0000
12:47785887:T:A	acceptor_loss	1.0000
12:47786578:C:CA	donor_gain	1.0000
12:47786583:A:AC	donor_gain	1.0000
12:47786584:C:CC	donor_gain	1.0000
12:47787707:CGTA:C	donor_loss	1.0000
12:47787708:GTA:G	donor_loss	1.0000
12:47787709:TA:T	donor_loss	1.0000
12:47787711:C:A	donor_loss	1.0000
12:47787806:CTAC:C	acceptor_gain	1.0000
12:47787807:TAC:T	acceptor_gain	1.0000
12:47787807:TACC:T	acceptor_loss	1.0000

AlphaMissense

6363 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:47789568:G:T	A662D	1.000
12:47786638:T:A	D801V	0.999
12:47786659:A:T	V794D	0.999
12:47788163:T:A	D707V	0.999
12:47788163:T:G	D707A	0.999
12:47789330:G:C	N683K	0.999
12:47789330:G:T	N683K	0.999
12:47789339:G:C	C680W	0.999
12:47789342:G:C	F679L	0.999
12:47789342:G:T	F679L	0.999
12:47789344:A:G	F679L	0.999
12:47789574:C:T	G660D	0.999
12:47789844:A:G	L648P	0.999
12:47789859:C:T	G643D	0.999
12:47789902:A:G	W629R	0.999
12:47789902:A:T	W629R	0.999
12:47791902:A:G	L555P	0.999
12:47791967:G:C	C533W	0.999
12:47791969:A:G	C533R	0.999
12:47792001:A:G	L522P	0.999
12:47793369:C:A	G521W	0.999
12:47797393:G:T	R151S	0.999
12:47798186:A:G	L89P	0.999
12:47785820:C:G	G841R	0.998
12:47785822:T:A	E840V	0.998
12:47785861:A:G	L827P	0.998
12:47786638:T:G	D801A	0.998
12:47786640:A:C	F800L	0.998
12:47786640:A:T	F800L	0.998
12:47786642:A:G	F800L	0.998

dbSNP variants (sampled 300 via entrez): RS1000034370 (12:47822044 C>T), RS1000045649 (12:47801540 G>A,C), RS1000051132 (12:47815061 A>C), RS1000142546 (12:47797595 G>A), RS1000171655 (12:47787606 T>C), RS1000187103 (12:47815468 A>C,G), RS1000298812 (12:47808867 A>G), RS1000351562 (12:47821788 C>G,T), RS1000358913 (12:47802686 C>T), RS1000422505 (12:47803251 G>A,C), RS1000425597 (12:47797950 T>C), RS1000452271 (12:47802912 T>C), RS1000533555 (12:47797346 T>G), RS1000604357 (12:47786961 T>G), RS1000795767 (12:47809086 A>C,T)

Disease associations

OMIM: gene MIM:606542 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

42 associations (top):

Study	Trait	p-value
GCST001762_46	Obesity-related traits	5.000000e-06
GCST001791_18	Urate levels	6.000000e-06
GCST004131_134	Inflammatory bowel disease	7.000000e-06
GCST004133_25	Ulcerative colitis	3.000000e-07
GCST004603_104	Platelet count	6.000000e-18
GCST004607_43	Plateletcrit	1.000000e-13
GCST004627_142	Lymphocyte count	2.000000e-10
GCST005038_136	Allergic disease (asthma, hay fever or eczema)	3.000000e-16
GCST005537_88	Chronic inflammatory diseases (ankylosing spondylitis, Crohn’s disease, psoriasis, primary sclerosing cholangitis, ulcerative colitis) (pleiotropy)	6.000000e-09
GCST006670_11	Primary sclerosing cholangitis	5.000000e-09
GCST007094_187	Diastolic blood pressure	5.000000e-08
GCST007095_21	Systolic blood pressure	9.000000e-06
GCST007099_67	Systolic blood pressure	2.000000e-10
GCST007611_20	Chronic obstructive pulmonary disease or high blood pressure (pleiotropy)	7.000000e-11
GCST007798_137	Asthma	9.000000e-08
GCST007799_3	Asthma (adult onset)	2.000000e-13
GCST007930_182	Medication use (agents acting on the renin-angiotensin system)	1.000000e-08
GCST007993_17	Asthma (adult onset)	2.000000e-10
GCST008103_172	Bipolar disorder	7.000000e-06
GCST009720_55	Asthma	5.000000e-09
GCST010042_61	Asthma	4.000000e-09
GCST010043_55	Asthma	7.000000e-11
GCST010106_4	Conjunctival UV autofluorescence (CUVAF)	6.000000e-07
GCST90002388_429	Lymphocyte count	2.000000e-17
GCST90002389_387	Lymphocyte percentage of white cells	2.000000e-16
GCST90002390_57	Mean corpuscular hemoglobin	5.000000e-16
GCST90002392_379	Mean corpuscular volume	3.000000e-13
GCST90002395_125	Mean platelet volume	3.000000e-13
GCST90002395_126	Mean platelet volume	3.000000e-09
GCST90002396_525	Mean reticulocyte volume	3.000000e-11

EFO canonical traits (17, from GWAS)

EFO ID	Trait name
EFO:0004531	urate measurement
EFO:0004309	platelet count
EFO:0007985	platelet crit
EFO:0004587	lymphocyte count
EFO:0006336	diastolic blood pressure
EFO:0006335	systolic blood pressure
EFO:1002011	adult onset asthma
EFO:0009931	Agents acting on the renin-angiotensin system use measurement
EFO:0004731	eye measurement
EFO:0010729	sun exposure measurement
EFO:0007993	lymphocyte percentage of leukocytes
EFO:0004527	mean corpuscular hemoglobin
EFO:0010701	mean reticulocyte volume
EFO:0007990	neutrophil percentage of leukocytes
EFO:0007984	platelet component distribution width
EFO:0007789	BMI-adjusted waist circumference
EFO:0007788	BMI-adjusted waist-hip ratio

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (4): CHEMBL2093865 (PROTEIN FAMILY), CHEMBL2716 (SINGLE PROTEIN), CHEMBL4630738 (PROTEIN-PROTEIN INTERACTION), CHEMBL6193803 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

28 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 437,477 (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
CHEMBL118	CELECOXIB	4	112,844
CHEMBL1469	PHENYLBUTANOIC ACID	4	37,081
CHEMBL1746	SODIUM PHENYLBUTYRATE	4	5,577
CHEMBL343448	ROMIDEPSIN	4	12,963
CHEMBL408513	BELINOSTAT	4	7,765
CHEMBL483254	PANOBINOSTAT	4	11,666
CHEMBL98	VORINOSTAT	4	50,361
CHEMBL1213492	GIVINOSTAT	4	2,827
CHEMBL140	CURCUMIN	3	93,882
CHEMBL145	CAFFEIC ACID	3	36,305
CHEMBL1851943	PRACINOSTAT	3	1,998
CHEMBL235191	TACEDINALINE	3	2,950
CHEMBL27759	ENTINOSTAT	3	6,584
CHEMBL3621988	TUCIDINOSTAT	3	2,182
CHEMBL2103863	ABEXINOSTAT	3	2,195
CHEMBL1801250	NANATINOSTAT	2	754
CHEMBL191482	AR-42	2	2,061
CHEMBL284616	CHLOROGENIC ACID	2	41,945
CHEMBL356066	DACINOSTAT	2	3,050
CHEMBL3622533	FIMEPINOSTAT	2	2,487
CHEMBL2105763	QUISINOSTAT	2
CHEMBL2364628	RICOLINOSTAT	2
CHEMBL3693786	CITARINOSTAT	2
CHEMBL353581	PYROXAMIDE	1
CHEMBL598797	CUDC-101	1
CHEMBL609583	R-306465	1
CHEMBL96	GAMMA-AMINOBUTYRIC ACID	1
CHEMBL99	TRICHOSTATIN	1

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 3.5.1.- Histone deacetylases (HDACs)

Most potent curated ligand interactions (12 total), top 12:

Ligand	Action	Affinity	Parameter
panobinostat	Inhibition	7.85	pEC50
TMP269	Inhibition	7.37	pIC50
belinostat	Inhibition	7.12	pKi
quisinostat	Inhibition	6.92	pIC50
trichostatin A	Inhibition	6.71	pKi
givinostat	Inhibition	6.62	pKi
CUDC-101	Inhibition	6.43	pIC50
KA1010	Inhibition	6.01	pIC50
romidepsin	Inhibition	5.9	pKi
scriptaid	Inhibition	5.65	pKi
SS-208	Inhibition	5.08	pIC50
dacinostat	Inhibition	5.02	pKi

Binding affinities (BindingDB)

41 measured of 52 human assays (53 total across all organisms); most potent 41 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
(E)-N-hydroxy-3-[4-[[2-(1-methylindol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide	IC50	0.2 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[4-[[1-adamantylmethyl(methyl)amino]methyl]phenyl]-N-hydroxyprop-2-enamide	IC50	0.3 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[4-[(1-adamantylmethylamino)methyl]-3-fluorophenyl]-N-hydroxyprop-2-enamide	IC50	0.78 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[4-[[1-adamantylmethyl(methyl)amino]methyl]-3-fluorophenyl]-N-hydroxyprop-2-enamide	IC50	0.78 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
N-hydroxy-6-(8-methoxy-6,11,11-trioxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide	IC50	0.8 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[4-[(1-adamantylmethylamino)methyl]phenyl]-N-hydroxyprop-2-enamide	IC50	0.95 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
Panobinostat	IC50	1 nM
N-hydroxy-6-(8-methoxy-6-oxobenzo[b][1,4]benzothiazepin-5-yl)hexanamide	IC50	1.2 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[4-[(cyclohexylmethylamino)methyl]phenyl]-N-hydroxyprop-2-enamide	IC50	1.8 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
BRD2492	IC50	2 nM
(E)-3-[2-butyl-1-[2-(dimethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide	IC50	4.7 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
CHEBI:46024	IC50	4.9 nM
(E)-N-hydroxy-3-[3-[methyl(2-phenylethyl)sulfamoyl]phenyl]prop-2-enamide	IC50	5 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
R-TSA	IC50	5.76 nM
HDAC inhibitor, Compound 2	IC50	7.93 nM
HDAC inhibitor, Compound 1	IC50	10.1 nM
(E)-N-hydroxy-3-[3-[methyl(phenyl)sulfamoyl]phenyl]prop-2-enamide	IC50	17.8 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
(E)-3-[3-[(1-adamantylamino)methyl]phenyl]-N-hydroxyprop-2-enamide	IC50	24 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)nonyl]acetamide	IC50	26 nM
3-(furan-3-yl)-N-[[4-(hydroxycarbamoyl)phenyl]methyl]-5-(4-hydroxyphenyl)-1H-pyrrole-2-carboxamide	IC50	49.9 nM	US-8685992: Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
6-[[1-adamantylmethyl(methyl)amino]methyl]-N-hydroxy-3,4-dihydronaphthalene-2-carboxamide	IC50	55.8 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
2-(5-methoxy-2-methyl-1H-indol-3-yl)-N-[(1S)-7-oxo-1-(5-phenyl-1H-imidazol-2-yl)octyl]acetamide	IC50	59 nM
N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]-3-(4-hydroxyphenyl)-5-thiophen-3-yl-1H-pyrrole-2-carboxamide	IC50	71 nM	US-8685992: Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
N-hydroxy-7-[pyridin-2-yl(quinolin-2-yl)amino]heptanamide	IC50	71 nM	US-8748458: Scriptaid isosteres and their use in therapy
3-(4-methoxyphenyl)-5-phenyl-N-[[4-(2-sulfanylethylcarbamoyl)phenyl]methyl]-1H-pyrrole-2-carboxamide	IC50	84.2 nM	US-8685992: Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
MGCD-0103	IC50	102 nM	US-9409858: Selective histone deactylase 6 inhibitors
(E)-N-Hydroxy-3-phenyl-acrylamide	IC50	133 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
N-hydroxy-4-[(3-oxo-[1,2]thiazolo[5,4-b]pyridin-2-yl)methyl]benzamide	IC50	175 nM	US-10011611: Histone deacetylase inhibitors and methods for use thereof
N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]-3-(furan-3-yl)-5-(4-hydroxyphenyl)-1H-pyrrole-2-carboxamide	IC50	184 nM	US-8685992: Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
S-TSA	IC50	206 nM
(E)-3-[4-[[1-adamantylmethyl(2-fluoroethyl)amino]methyl]phenyl]-N-hydroxyprop-2-enamide	IC50	221 nM	US-10188756: Imaging histone deacetylases with a radiotracer using positron emission tomography
MS-275	IC50	243 nM
3-(4-fluorophenyl)-N-[[4-(hydroxycarbamoyl)phenyl]methyl]-5-pyridin-3-yl-1H-pyrrole-2-carboxamide	IC50	332 nM	US-8685992: Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
Octanedioic acid adamantan-1-ylamide hydroxyamide	IC50	420 nM
(S)-Benzyl (6-acetamido-1-((4-methyl-2-oxo-2H-chromen-7-yl)amino)-1-oxohexan-2-yl)carbamate, 21	IC50	643 nM
N-acetyldinaline	IC50	900 nM
(S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide, 3	IC50	1180 nM
N’-(2-aminophenyl)-N-(4-methylphenyl)heptanediamide	IC50	2000 nM	US-9265734: Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors
5-chloranyl-7-[(4-ethylpiperazin-1-yl)-pyridin-3-yl-methyl]quinolin-8-ol	IC50	2390 nM
2-ethyl-1-[(3R)-1-[(5-methoxy-1H-1,3-benzodiazol-2-yl)carbonyl]pyrrolidin-3-yl]-1H-1,3-benzodiazole	IC50	4200 nM
N-(4-{(2R,4R,6S)-4-{[(4,5-diphenyl-1,3-oxazol-2-yl)sulfanyl]methyl}-6-[4-(hydroxymethyl)phenyl]-1,3-dioxan-2-yl}phenyl)-N -hydroxyoctanediamide	IC50	16400 nM	US-9249087: HDAC inhibitors and therapeutic methods using the same

ChEMBL bioactivities

3434 potent at pChembl≥5 of 3844 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.77	IC50	0.17	nM	CHEMBL5433552
9.70	IC50	0.2	nM	CHEMBL2371007
9.70	IC50	0.2	nM	CHEMBL5395502
9.70	IC50	0.2	nM	CHEMBL1793811
9.70	IC50	0.2	nM	CHEMBL1793991
9.70	IC50	0.2	nM	CHEMBL1793985
9.52	IC50	0.3	nM	CHEMBL2370998
9.52	IC50	0.3	nM	CHEMBL5199116
9.52	IC50	0.3	nM	CHEMBL5170036
9.52	IC50	0.3	nM	CHEMBL1793822
9.46	IC50	0.35	nM	VORINOSTAT
9.40	IC50	0.4	nM	CHEMBL2371000
9.40	IC50	0.4	nM	CHEMBL1793816
9.08	IC50	0.83	nM	PANOBINOSTAT
9.05	IC50	0.9	nM	CHEMBL605110
9.02	IC50	0.95	nM	CHEMBL595479
9.00	IC50	1	nM	CHEMBL3758184
9.00	IC50	1	nM	APICIDIN
9.00	IC50	1	nM	CHEMBL2371003
9.00	IC50	1	nM	ROMIDEPSIN
9.00	IC50	1	nM	CHEMBL4467135
9.00	IC50	1	nM	CHEMBL3692689
9.00	IC50	1	nM	CHEMBL595711
9.00	IC50	1	nM	CHEMBL595910
9.00	IC50	1	nM	CHEMBL1793947
9.00	IC50	1	nM	CHEMBL1793810
9.00	IC50	1	nM	CHEMBL1793823
8.99	IC50	1.03	nM	CHEMBL1214760
8.98	IC50	1.05	nM	CHEMBL594544
8.92	IC50	1.2	nM	CHEMBL604796
8.92	IC50	1.2	nM	CHEMBL608416
8.92	IC50	1.2	nM	CHEMBL594544
8.89	IC50	1.3	nM	CHEMBL1793992
8.85	IC50	1.4	nM	CHEMBL99661
8.85	IC50	1.42	nM	TRICHOSTATIN
8.82	IC50	1.5	nM	TRICHOSTATIN
8.82	IC50	1.5	nM	CHEMBL5280445
8.82	IC50	1.5	nM	CHEMBL594743
8.82	IC50	1.5	nM	CHEMBL593846
8.82	IC50	1.5	nM	CHEMBL594542
8.77	Ki	1.7	nM	QUISINOSTAT
8.77	IC50	1.7	nM	CHEMBL595908
8.74	IC50	1.8	nM	CHEMBL478727
8.74	IC50	1.8	nM	CHEMBL26159
8.74	IC50	1.8	nM	CHEMBL595910
8.72	IC50	1.9	nM	CHEMBL477093
8.70	IC50	2	nM	CHEMBL99392
8.70	IC50	2	nM	CHEMBL150237
8.70	IC50	2	nM	CHEMBL4228565
8.70	IC50	2	nM	CHEMBL4228304

PubChem BioAssay actives

2444 with measured affinity, of 6100 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
N-hydroxy-2-[4-(4-methylphenyl)sulfonylpiperazin-1-yl]-1,3-thiazole-5-carboxamide	1941741: Inhibition of HDAC (unknown origin)	ic50	0.0001	uM
7-[4-[[4-[3-(tert-butylsulfamoyl)anilino]-5-methylpyrimidin-2-yl]amino]-2-fluorophenoxy]-N-hydroxyheptanamide	2031064: Inhibition of HDAC in human HeLa cells nuclear extract incubated for 30 mins by multiplate reader analysis	ic50	0.0002	uM
7-[4-[[4-[3-(tert-butylsulfamoyl)anilino]-5-methylpyrimidin-2-yl]amino]phenoxy]-N-hydroxyheptanamide	2031064: Inhibition of HDAC in human HeLa cells nuclear extract incubated for 30 mins by multiplate reader analysis	ic50	0.0002	uM
(9S,12R)-3-[(2S)-butan-2-yl]-9-(6-hydroxy-5-oxoheptyl)-6-[(1-methoxyindol-3-yl)methyl]-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	1847765: Inhibition of HDAC (unknown origin)	ic50	0.0003	uM
(9S,12R)-3-[(2S)-butan-2-yl]-6-(1H-indol-3-ylmethyl)-9-(5-oxoheptyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	1847765: Inhibition of HDAC (unknown origin)	ic50	0.0003	uM
(3S,6S,9S,12R)-3-[(2S)-butan-2-yl]-9-(7-hydroxy-6-oxooctyl)-6-[(1-methoxyindol-3-yl)methyl]-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	90356: Inhibitory concentration against human Histone deacetylase in Hela cells	ic50	0.0003	uM
N-hydroxy-2-[4-[(E)-1-hydroxy-4-(4-phenylphenyl)but-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0009	uM
N-hydroxy-2-[4-[(E)-1-hydroxy-4-(4-methoxyphenyl)but-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0009	uM
N-hydroxy-2-[4-[(E)-1-hydroxy-4-phenylbut-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0010	uM
2-[4-[(E)-4-(4-fluorophenyl)-1-hydroxybut-3-en-2-yl]piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0010	uM
(3S,6R,9S,12R)-3-[(2S)-butan-2-yl]-6-[(1-methoxyindol-2-yl)methyl]-9-(6-oxooctyl)-1,4,10-triazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	1622995: Inhibition of HDAC (unknown origin)	ic50	0.0010	uM
N-hydroxy-6-[(2S,5S,8S,11S)-8-(1H-indol-3-ylmethyl)-2-methyl-11-(2-methylpropyl)-3,6,9,13-tetraoxo-1,4,7,10-tetrazacyclotridec-5-yl]hexanamide	447991: Inhibition of HDAC in human HeLa cell nuclear extract after 30 mins by fluorimetric assay	ic50	0.0010	uM
N-hydroxy-2-[4-[(E)-1-hydroxy-4-(4-methylphenyl)but-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0010	uM
6-[(5S,8S,11R)-11-[(2S)-butan-2-yl]-8-(1H-indol-2-ylmethyl)-3,6,9,13-tetraoxo-1,4,7,10-tetrazacyclotridec-5-yl]-N-hydroxyhexanamide	487230: Inhibition of HDAC in human HeLa cells	ic50	0.0010	uM
7-[4-[4-[[[(2S,3R,4S,6R)-2-[[(2R,4R,5R,6R,8R,11R,12S,19R,20R)-11-ethyl-4-methoxy-2,4,6,8,12,19-hexamethyl-7,9,14-trioxo-10,13-dioxa-15,18-diazatricyclo[10.6.2.015,20]icos-1(18)-en-5-yl]oxy]-3-hydroxy-6-methyloxan-4-yl]-methylamino]methyl]phenyl]triazol-1-yl]-N-hydroxyheptanamide	499799: Inhibition of HDAC in human HeLa cell nuclear extracts	ic50	0.0010	uM
(E)-N-hydroxy-3-[4-oxo-1’-(2-phenylethyl)spiro[3H-chromene-2,3’-piperidine]-6-yl]prop-2-enamide	1273866: Inhibition of HDAC in human HeLa cells nuclear extract using Fluor de lys as substrate after 15 mins by fluorometric analysis	ic50	0.0010	uM
2-[4-[(E)-4-(3-fluorophenyl)-1-hydroxybut-3-en-2-yl]piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0012	uM
2-[4-[(E)-4-(4-chlorophenyl)-1-hydroxybut-3-en-2-yl]piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0012	uM
N’-hydroxy-N-[(2R)-4-(methylamino)-3-oxo-1-phenylbutan-2-yl]octanediamide	90195: Concentration required to inhibit Histone Deacetylase (HDAC) from K562 erythroleukemia cells	ic50	0.0014	uM
(2E,4E,6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide	1273502: Inhibition of HDAC in human HeLa cell nuclear extract using BML-KI104 Fluor de Lys as substrate by fluorescence-based assay	ic50	0.0014	uM
N-hydroxy-2-[4-(naphthalen-2-ylmethyl)piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0015	uM
N-hydroxy-2-[4-[(E)-1-methoxy-4-phenylbut-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0015	uM
N-hydroxy-2-[4-[[[(E)-1-hydroxy-4-phenylbut-3-en-2-yl]amino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0015	uM
N-hydroxy-2-[4-[[(1-methylindol-3-yl)methylamino]methyl]piperidin-1-yl]pyrimidine-5-carboxamide	1399820: Inhibition of human recombinant HDAC7 using fluorogenic HDAC substrate class 2a after 45 mins by fluorimetrc method	ki	0.0017	uM
N-hydroxy-2-[4-[(E)-4-phenylbut-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0017	uM
N-hydroxy-6-[4-(6-methoxynaphthalen-2-yl)triazol-1-yl]hexanamide	382342: Inhibition of human HDAC in HeLa cells by flour de lys assay	ic50	0.0018	uM
N-hydroxy-6-[4-(3-phenylphenyl)triazol-1-yl]hexanamide	382342: Inhibition of human HDAC in HeLa cells by flour de lys assay	ic50	0.0019	uM
2-[2-[2-[[(2E)-3-(3-bromo-4-hydroxyphenyl)-2-hydroxyiminopropanoyl]amino]ethyldisulfanyl]ethylamino]-2-oxoacetic acid	90530: Inhibitory concentration against isolated Histone deacetylase	ic50	0.0020	uM
(3S,6S,9S,12R)-3-[(2S)-butan-2-yl]-6-(1H-indol-3-ylmethyl)-9-(6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.4.0]hexadecane-2,5,8,11-tetrone	81887: Inhibitory activity against histone deacetylase (HDAC) enzyme derived from partially purified extracts of human HeLa cells using [3H]11 as radioligand	ic50	0.0020	uM
6-[4-[[5-chloro-4-(4-chloroanilino)pyrimidin-2-yl]amino]pyrazol-1-yl]-N-hydroxyhexanamide	1550094: Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	ic50	0.0020	uM
7-[4-[[5-chloro-4-(4-chloroanilino)pyrimidin-2-yl]amino]pyrazol-1-yl]-N-hydroxyheptanamide	1550094: Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	ic50	0.0020	uM
4-[(E)-3-[[(2S)-1-(4-bromoanilino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-oxoprop-1-enyl]-N-hydroxybenzamide	1390020: Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay	ic50	0.0020	uM
4-[(E)-3-[[(2S)-1-(4-fluoroanilino)-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-oxoprop-1-enyl]-N-hydroxybenzamide	1390020: Inhibition of HDAC in human HeLa cell nuclear extract using Boc-Lys (acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition measured after 30 mins by fluorescence assay	ic50	0.0020	uM
2-(6-ethoxy-3-pyridinyl)-N-[7-(hydroxyamino)-7-oxoheptyl]-9-(2-methoxy-3-pyridinyl)-8-oxo-7H-purine-6-carboxamide	2079009: Inhibition of HDAC in human HeLa cells nuclear extract	ic50	0.0020	uM
2-[4-[(E)-4-(2-fluorophenyl)-1-hydroxybut-3-en-2-yl]piperazin-1-yl]-N-hydroxypyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0020	uM
N-hydroxy-7-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]heptanamide	316872: Inhibition of HDAC from human K562 cells	ic50	0.0021	uM
N-hydroxy-6-[4-(4-methoxyphenyl)triazol-1-yl]hexanamide	382342: Inhibition of human HDAC in HeLa cells by flour de lys assay	ic50	0.0021	uM
tert-butyl (8R,9R,12S)-12-[[6-(hydroxyamino)-6-oxohexyl]carbamoyl]-9-(2-methylpropyl)-2-oxa-11-azabicyclo[12.2.2]octadeca-1(16),14,17-triene-8-carboxylate	90195: Concentration required to inhibit Histone Deacetylase (HDAC) from K562 erythroleukemia cells	ic50	0.0021	uM
N-hydroxy-6-(4-quinolin-2-yltriazol-1-yl)hexanamide	382342: Inhibition of human HDAC in HeLa cells by flour de lys assay	ic50	0.0021	uM
N-hydroxy-2-[4-[(E)-1-hydroxy-4-[4-(trifluoromethyl)phenyl]but-3-en-2-yl]piperazin-1-yl]pyrimidine-5-carboxamide	454842: Inhibition of HDAC in human HeLa cells extractt	ic50	0.0021	uM
6-[4-(4-bromoanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyhexanamide	1720096: Inhibition of HDAC (unknown origin)	ic50	0.0022	uM
7-[4-(4-bromoanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide	1275247: Inhibition of HDAC in human HeLa cell nuclear extracts preincubated for 15 mins followed by addition of Fluor de Lys as substrate for 1 hr by fluorometric assay	ic50	0.0022	uM
N-hydroxy-6-[4-(4-pyridin-4-ylphenyl)triazol-1-yl]hexanamide	382342: Inhibition of human HDAC in HeLa cells by flour de lys assay	ic50	0.0023	uM
N-hydroxy-7-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]heptanamide	316872: Inhibition of HDAC from human K562 cells	ic50	0.0025	uM
7-[5-(4-bromophenyl)-1,3-oxazol-2-yl]-N-hydroxyheptanamide	316872: Inhibition of HDAC from human K562 cells	ic50	0.0027	uM
(E)-N-hydroxy-3-[4-[2-(2-methyl-1H-indol-3-yl)ethylsulfamoyl]phenyl]prop-2-enamide	1187258: Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay	ic50	0.0028	uM
6-[4-(2,4-dichloroanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyhexanamide	1256443: Inhibition of human HDAC in HeLa cell nuclear extract by fluorometric assay using Fluor de Lys substrate	ic50	0.0028	uM
7-[4-(2,4-dichloroanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide	1915571: Inhibition of HDAC (unknown origin)	ic50	0.0028	uM
N-hydroxy-7-[4-(2-methylphenyl)triazol-1-yl]heptanamide	456795: Inhibition of HDAC in human HeLa cell nuclear extracts after 15 mins by fluorescence assay	ic50	0.0028	uM
7-[4-[[5-chloro-4-(4-fluoroanilino)pyrimidin-2-yl]amino]pyrazol-1-yl]-N-hydroxyheptanamide	1550094: Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	ic50	0.0030	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Vorinostat	affects cotreatment, decreases expression	3
Air Pollutants	affects cotreatment, increases abundance, increases oxidation, affects expression, increases expression	3
Valproic Acid	affects expression, decreases expression	3
Benzo(a)pyrene	affects methylation, increases expression	2
Estradiol	affects expression, decreases expression, increases reaction	2
Ozone	affects cotreatment, increases oxidation, increases abundance, affects expression	2
Particulate Matter	increases abundance, increases expression	2
GSK-J4	increases expression	1
FR900359	affects phosphorylation	1
dicrotophos	increases expression	1
triphenyl phosphate	affects expression	1
alpha-pinene	increases abundance, affects cotreatment, increases oxidation	1
propionaldehyde	decreases expression	1
bisphenol A	increases expression	1
arsenite	decreases methylation	1
sodium arsenite	affects expression, decreases expression, increases reaction	1
butyraldehyde	decreases expression	1
perfluorooctanoic acid	decreases expression	1
coumarin	increases phosphorylation	1
methacrylaldehyde	affects cotreatment, increases oxidation, increases abundance	1
testosterone-3-carboxymethyloxime-bovine serum albumin conjugate	affects expression	1
perfluorooctane sulfonic acid	decreases expression	1
perfluoro-n-nonanoic acid	decreases expression	1
monomethylarsonous acid	increases expression, affects cotreatment, decreases expression	1
perfluorohexanesulfonic acid	decreases expression	1
bisphenol S	affects cotreatment, decreases expression	1
(+)-JQ1 compound	decreases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Sunitinib	increases expression	1
Acrolein	affects cotreatment, increases oxidation, increases abundance	1

ChEMBL screening assays

1710 unique, capped per target: 1695 binding, 10 admet, 4 functional, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1003756	Binding	Inhibition of HDAC in human NB4 cells assessed as induction of histone H3 acetylation after 6 hrs by Western blot analysis	Design, synthesis and preliminary biological evaluation of new hydroxamate histone deacetylase inhibitors as potential antileukemic agents. — Bioorg Med Chem Lett
CHEMBL4346553	ADMET	Inhibition of HDAC in HUVEC using Boc-Lys(Ac)-AMC as substrate preincubated for 12 hrs followed by substrate addition and measured after 4 hrs by fluorimetry	Discovery of Novel Fungal Lanosterol 14α-Demethylase (CYP51)/Histone Deacetylase Dual Inhibitors to Treat Azole-Resistant Candidiasis. — J Med Chem
CHEMBL5049470	Functional	In vivo inhibition of HDAC in HEL cells xenografted in BALB/C mouse assessed as upregulation of caspase-9 levels at 5 to 10 mg/kg by immunohistochemical staining method	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy. — J Med Chem

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B8HB	Abcam HCT 116 HDAC7 KO	Cancer cell line	Male
CVCL_B8WP	Abcam MCF-7 HDAC7 KO	Cancer cell line	Female
CVCL_SR16	HAP1 HDAC7 (-) 1	Cancer cell line	Male
CVCL_SR17	HAP1 HDAC7 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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