PARG

Summary

PARG (poly(ADP-ribose) glycohydrolase, HGNC:8605) is a protein-coding gene on chromosome 10q11.23, encoding Poly(ADP-ribose) glycohydrolase (Q86W56). Poly(ADP-ribose) glycohydrolase that degrades poly(ADP-ribose) by hydrolyzing the ribose-ribose bonds present in poly(ADP-ribose). It is a selective cancer dependency (DepMap: 29.7% of cell lines).

Poly(ADP-ribose) glycohydrolase (PARG) is the major enzyme responsible for the catabolism of poly(ADP-ribose), a reversible covalent-modifier of chromosomal proteins. The protein is found in many tissues and may be subject to proteolysis generating smaller, active products. Several transcript variants encoding different isoforms have been found for this gene.

Source: NCBI Gene 8505 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 67 total
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer dependency (DepMap): dependent in 29.7% of screened cell lines
• MANE Select transcript: NM_003631

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:8605
Approved symbol	PARG
Name	poly(ADP-ribose) glycohydrolase
Location	10q11.23
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000227345
Ensembl biotype	protein_coding
OMIM	603501
Entrez	8505

Gene structure

Transcript identifiers

Ensembl transcripts: 14 — 9 protein_coding, 2 protein_coding_CDS_not_defined, 2 nonsense_mediated_decay, 1 retained_intron

ENST00000402038, ENST00000492350, ENST00000497481, ENST00000610922, ENST00000611974, ENST00000614063, ENST00000616448, ENST00000865657, ENST00000934076, ENST00000941174, ENST00000941175, ENST00000941176, ENST00000941177, ENST00000941178

RefSeq mRNA: 5 — MANE Select: NM_003631 NM_001303486, NM_001303487, NM_001303489, NM_001324381, NM_003631

CCDS: CCDS73130

Canonical transcript exons

ENST00000616448 — 18 exons

Exon	Start	End
ENSE00001462471	49843554	49843632
ENSE00001555046	49841950	49842058
ENSE00001560903	49818279	49819494
ENSE00001710602	49922547	49922669
ENSE00001722038	49820165	49820293
ENSE00001761710	49832803	49832908
ENSE00002438024	49861588	49861663
ENSE00002442787	49857306	49857453
ENSE00002451543	49869476	49869555
ENSE00002451899	49885203	49885295
ENSE00002464919	49915917	49915991
ENSE00002501568	49922336	49922419
ENSE00002510511	49879673	49879830
ENSE00003490059	49865321	49865381
ENSE00003718680	49933177	49934163
ENSE00003721498	49932100	49932283
ENSE00003737831	49941509	49942027
ENSE00003745578	49935076	49935142

Expression profiles

Bgee: expression breadth ubiquitous, 252 present calls, max score 91.91.

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
calcaneal tendon	UBERON:0003701	91.91	gold quality
adrenal tissue	UBERON:0018303	90.49	gold quality
germinal epithelium of ovary	UBERON:0001304	89.00	silver quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	88.10	gold quality
nephron tubule	UBERON:0001231	86.28	silver quality
ventricular zone	UBERON:0003053	85.99	gold quality
epithelium of nasopharynx	UBERON:0001951	85.11	gold quality
ganglionic eminence	UBERON:0004023	85.01	gold quality
embryo	UBERON:0000922	84.80	gold quality
cortical plate	UBERON:0005343	84.57	gold quality
corpus callosum	UBERON:0002336	84.31	gold quality
gingival epithelium	UBERON:0001949	84.13	silver quality
muscle of leg	UBERON:0001383	83.99	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	83.91	silver quality
secondary oocyte	CL:0000655	83.79	gold quality
gastrocnemius	UBERON:0001388	83.66	gold quality
esophagus squamous epithelium	UBERON:0006920	83.31	silver quality
sural nerve	UBERON:0015488	83.21	gold quality
biceps brachii	UBERON:0001507	83.13	silver quality
hair follicle	UBERON:0002073	82.95	silver quality
stromal cell of endometrium	CL:0002255	82.78	gold quality
kidney epithelium	UBERON:0004819	82.75	silver quality
tonsil	UBERON:0002372	82.69	gold quality
rectum	UBERON:0001052	82.65	gold quality
islet of Langerhans	UBERON:0000006	82.59	gold quality
muscle organ	UBERON:0001630	82.57	gold quality
metanephric glomerulus	UBERON:0004736	82.41	silver quality
monocyte	CL:0000576	82.38	gold quality
leukocyte	CL:0000738	82.27	gold quality
mononuclear cell	CL:0000842	82.23	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.64

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): ETV5, PARP1, SP1, SPI1

miRNA regulators (miRDB)

110 targeting PARG, 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-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-9-5P	100.00	72.28	2361
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-29A-3P	100.00	73.11	1835
HSA-MIR-29B-3P	100.00	73.18	1833
HSA-MIR-29C-3P	100.00	73.15	1833
HSA-MIR-200B-3P	100.00	73.31	2693
HSA-MIR-200C-3P	100.00	73.35	2685
HSA-MIR-429	100.00	73.44	2698
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-513B-5P	99.99	69.96	2150
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4534	99.99	66.58	1907
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-548AQ-3P	99.93	72.66	4867

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 29.7% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 39)

• Subcellular localization of human poly(ADP-ribose) glycohydrolase in mammalian cells. (PMID:12878198)
• PARG is expressed in alternatiuve splice variants yielding isoforms that localize to different cell compartments. (PMID:15212953)
• PARG in modulating chromatin structure, participares in transcription, DNA repair and apoptosis [review]. (PMID:15868399)
• PARG is resident in FMRP (Fragile-X mental retardation protein)-associated messenger ribonucleoparticles complexes. (PMID:16117724)
• results suggest that PARG may play an autonomous role in the cellular response to oxidative DNA damage (PMID:16526943)
• hPARG55, that can be expressed through alternative translation initiation from hPARG60 transcripts is strictly targeted to the mitochondria. (PMID:17509564)
• PARG is identified as a novel and critical component of single-strand break repair that accelerates this process in concert with PARP-1. (PMID:17548475)
• PPAR gamma ligands inhibit growth and induce apoptosis of liver cancer cell (PMID:18407589)
• suggest that PU.1-binding motifs are essential for PARG promoter activity and that PU.1 modulates PARG gene expression during differentiation of HL-60 cells. (PMID:19076642)
• The identification of a PARG isoform as a component of the mitochondrial matrix raises several interesting possibilities concerning mechanisms of nuclear-mitochondrial cross talk involved in regulation of cell death pathways. (PMID:19389396)
• PARG could be a novel potential therapeutic target for radiotherapy. (PMID:19454480)
• These data indicate that PARG is a survival factor at mild oxidative damage but contributes to the apoptosis-necrosis switch in severely damaged cells. (PMID:19571039)
• PARP-1 and PARG, nuclear enzymes with opposing enzymatic activities, localize to target promoters and act in a similar, rather than antagonistic, manner to regulate gene expression (PMID:19812418)
• inhibition of PARG leads to an accumulation of PAR polymers, the collapse of replication forks and the induction of homologous recombination in wild-type cells. (PMID:22333589)
• PARG knockdown, concomitant with inhibition of PARP, suppressed the metastatic potency of colon carcinoma cells by activation of PI3K/Akt signaling pathway. (PMID:22508044)
• Silencing of Apoptosis-Inducing factor and poly(ADP-ribose) glycohydrolase reveals novel roles in breast cancer cell death after chemotherapy. (PMID:22839996)
• PARG silencing could inhibit the ability of HUVEC migration and proliferation by downregulating the activity of NF-kappaB in LoVo cells that in turn decreases angiogenic factors such as VEGF, b-FGF, ICAM-1, MMP-9, as well as phosphorylation of p38 and ERK. (PMID:22918473)
• Results define PARG as a coactivator regulating chromatin remodeling during retinoic acid receptor-dependent gene expression. (PMID:23102699)
• Therefore, strategies that target PAR metabolism for the improved treatment of cancer may be required to target PARP-1 and PARG individually in order to optimize cancer cell death. (PMID:23254695)
• The amount of poly(ADP-ribose) in a cell is regulated under the control of PARP1/PARG gene expression balance. (PMID:23467693)
• PARG knockdown enhances sensitivity to MMS in MIAPaCa2 and RKO tumor cell lines. (PMID:23744356)
• poly(ADP-ribose) glycohydrolase is crucial for Trypanosoma cruzi infection cycle. (PMID:23776710)
• Radiation-induced G2/M arrest was largely suppressed by PARG siRNA in PC-14 and A427 cells, which exhibited significantly enhanced radiosensitivity in response to PARG knockdown. (PMID:24211580)
• Nuclear Smad function is negatively regulated by PARP-1 that is assisted by PARP-2 and positively regulated by PARG during the course of TGFB signaling. (PMID:25133494)
• Poly(ADP-ribosyl) glycohydrolase (PARG) is involved in cell proliferation and DNA synthesis, with depletion leading to replication-coupled H2AX phosphorylation. In addition, PARG depletion or inhibition slows down individual replication forks similarly to mild chemotherapeutic treatment. (PMID:25535335)
• Studies indicate that poly (ADP-ribose) glycohydrolase (PARG) and terminal ADP-ribose glycohydrolase 1 (TARG1) are key enzymes in poly(ADP-ribose) polymerases (PARPs)-mediated ADP-ribosylation. (PMID:26091342)
• Data show that poly-(ADP-ribose) polymerase 1 (PARP1) opposes the function of poly-(ADP-ribose) glycohydrolase (PARG) during regulation of bone morphogenetic protein target gene expression. (PMID:27129221)
• PARG inhibition leads to stalled replication forks and increased homologous recombination (HRR). The lack of HRR proteins at PARG inhibitor-induced replication stalling that induces cell death. (PMID:28254358)
• PARG is acetylated at multiple sites.PARG interacts with PCNA via a non-canonical PIP-box. (PMID:28934471)
• Oncogenic activity of poly (ADP-ribose) glycohydrolase (PMID:30459355)
• PARG, an enzyme family that hydrolyzes poly(ADP-ribose), is sufficient to dissociate damaged DNA-rich compartments in vitro and initiates the nucleocytoplasmic shuttling of FUS in cells. (PMID:31067465)
• PARG role in the pancreatic ductal adenocarcinoma. (PMID:31273064)
• PARG has a robust endo-glycohydrolase activity that releases protein-free poly(ADP-ribose) chains. (PMID:32439163)
• Regulation of ALT-associated homology-directed repair by polyADP-ribosylation. (PMID:33046907)
• PARG overexpression partially but significantly inhibited ASK3 dephosphorylation under hyperosmotic stress, while the glycohydrolase-inactive PARG mutant did not. (PMID:33649309)
• Unrestrained poly-ADP-ribosylation provides insights into chromatin regulation and human disease. (PMID:34019811)
• Upregulation of PARG in prostate cancer cells suppresses their malignant behavior and downregulates tumor-promoting genes. (PMID:36076593)
• PARG Promotes Esophagus Cancer Cell Metastasis by Activation of the Wnt/beta-Catenin Pathway. (PMID:37429965)
• O-GlcNAc has crosstalk with ADP-ribosylation via PARG. (PMID:37858678)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	parga	ENSDARG00000061114
mus_musculus	Parg	ENSMUSG00000021911
rattus_norvegicus	Parg	ENSRNOG00000019978
drosophila_melanogaster	Parg	FBGN0023216
caenorhabditis_elegans		WBGENE00004051
caenorhabditis_elegans		WBGENE00004052

Protein

Protein identifiers

Poly(ADP-ribose) glycohydrolase — Q86W56 (reviewed: Q86W56)

All UniProt accessions (3): Q86W56, A0A087WX07, A0A087WXI6

UniProt curated annotations — full annotation on UniProt →

Function. Poly(ADP-ribose) glycohydrolase that degrades poly(ADP-ribose) by hydrolyzing the ribose-ribose bonds present in poly(ADP-ribose). Mainly acts as an exo-glycohydrolase but can act as an endo-glycohydrolase at low efficiency, releasing poly(ADP-ribose) of different length as well as ADP-ribose monomers. It is however unable to cleave the ester bond between the terminal ADP-ribose and ADP-ribosylated residues, leaving proteins that are mono-ADP-ribosylated. Poly(ADP-ribose) synthesized after DNA damage is only present transiently and is rapidly degraded by PARG. Required to prevent detrimental accumulation of poly(ADP-ribose) upon prolonged replicative stress, while it is not required for recovery from transient replicative stress. Responsible for the prevalence of mono-ADP-ribosylated proteins in cells, thanks to its ability to degrade poly(ADP-ribose) without cleaving the terminal protein-ribose bond. Required for retinoid acid-dependent gene transactivation, probably by removing poly(ADP-ribose) from histone demethylase KDM4D, allowing chromatin derepression at RAR-dependent gene promoters. Involved in the synthesis of ATP in the nucleus, together with PARP1, NMNAT1 and NUDT5. Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming.

Subunit / interactions. Interacts with PCNA. Interacts with NUDT5.

Subcellular location. Nucleus Cytoplasm Cytoplasm Cytoplasm. Mitochondrion Mitochondrion matrix.

Tissue specificity. Ubiquitously expressed.

Domain organisation. The PIP-box mediates interaction with PCNA and localization to replication foci.

Miscellaneous. Catalytically inactive. Catalytically inactive.

Similarity. Belongs to the poly(ADP-ribose) glycohydrolase family.

Isoforms (5)

UniProt ID	Names	Canonical?
Q86W56-1	1, hPARG111	yes
Q86W56-2	2, hPARG102
Q86W56-3	3, hPARG99
Q86W56-4	4, hPARG60
Q86W56-5	5, hPARG55

RefSeq proteins (5): NP_001290415, NP_001290416, NP_001290418, NP_001311310, NP_003622* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR007724	Poly_GlycHdrlase	Family
IPR046372	PARG_cat_C	Domain
IPR048362	PARG_helical	Domain

Pfam: PF05028, PF20811

Enzyme classification (BRENDA):

• EC 3.2.1.143 — poly(ADP-ribose) glycohydrolase (BRENDA: 15 organisms, 83 substrates, 316 inhibitors, 21 Km, 4 kcat entries)

Substrate kinetics (BRENDA)

4 substrates with measured Km, best-characterized 4. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
(ADP-RIBOSE)N	0.0006–0.0066	10
POLY(ADP-RIBOSE)	0.0003–0.0111	7
(ADP-D-RIBOSE)15	0.0054–0.0058	2
ALPHA-NAD+	0.0006	1

Catalyzed reactions (Rhea), 1 shown:

• (1’’->2’)-ADP-alpha-D-ribose + H2O = (1’’->2’)-ADP-alpha-D-ribose + ADP-D-ribose (RHEA:52216)

UniProt features (131 total): helix 26, mutagenesis site 24, strand 17, modified residue 17, sequence conflict 14, turn 6, splice variant 6, compositionally biased region 5, binding site 5, region of interest 4, active site 3, short sequence motif 2, chain 1, site 1

Structure

Experimental structures (PDB)

25 structures.

PDB	Method	Resolution (Å)
7KG8	X-RAY DIFFRACTION	1.43
6OAL	X-RAY DIFFRACTION	1.6
7KG1	X-RAY DIFFRACTION	1.65
7KG0	X-RAY DIFFRACTION	1.66
6O9X	X-RAY DIFFRACTION	1.7
6OAK	X-RAY DIFFRACTION	1.7
4A0D	X-RAY DIFFRACTION	1.75
6OA1	X-RAY DIFFRACTION	1.8
4B1G	X-RAY DIFFRACTION	1.83
6HH6	X-RAY DIFFRACTION	1.85
7KG7	X-RAY DIFFRACTION	1.85
6HMM	X-RAY DIFFRACTION	1.9
6OA3	X-RAY DIFFRACTION	1.9
7KFP	X-RAY DIFFRACTION	1.9
5A7R	X-RAY DIFFRACTION	1.95
7KG6	X-RAY DIFFRACTION	1.96
4B1H	X-RAY DIFFRACTION	2
6O9Y	X-RAY DIFFRACTION	2
6OA0	X-RAY DIFFRACTION	2
6HMK	X-RAY DIFFRACTION	2.06
4B1J	X-RAY DIFFRACTION	2.08
4B1I	X-RAY DIFFRACTION	2.14
5LHB	X-RAY DIFFRACTION	2.23
6HML	X-RAY DIFFRACTION	2.25
6HMN	X-RAY DIFFRACTION	2.87

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q86W56-F1	68.92	0.52

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 (4): 737 (charge relay system); 755 (charge relay system); 756 (proton donor); 902 (sterically intereferes with binding of internal adp-d-ribose moieties of poly(adp-ribose) to preferntially bind terminal moieties and drive exo-glycohydrolitic action)

Ligand- & substrate-binding residues (5): 726–727; 740; 754; 795; 869–874

Post-translational modifications (17): 1, 22, 68, 133, 137, 139, 197, 199, 261, 264, 286, 291, 298, 302, 316, 340, 448

Mutagenesis-validated functional residues (24):

Position	Phenotype
1–619	reduces protein stability but does not abrogate poly(adp-ribose) glycohydrolase activity.
12–13	abolishes nuclear targeting.
36	no effect on poly(adp-ribose) glycohydrolase activity.
37	no effect on poly(adp-ribose) glycohydrolase activity.
653	no effect on poly(adp-ribose) glycohydrolase activity.
671	no effect on poly(adp-ribose) glycohydrolase activity.
671	slightly reduces poly(adp-ribose) glycohydrolase activity.
726	severly reduces poly(adp-ribose) glycohydrolase activity.
727	severly reduces poly(adp-ribose) glycohydrolase activity.
740	severly reduces poly(adp-ribose) glycohydrolase activity.
745	abolishes poly(adp-ribose) glycohydrolase activity.
746	no effect on poly(adp-ribose) glycohydrolase activity.
749	no effect on poly(adp-ribose) glycohydrolase activity.
753	no effect on poly(adp-ribose) glycohydrolase activity.
755	abolishes poly(adp-ribose) glycohydrolase activity.
756	abolishes poly(adp-ribose) glycohydrolase activity.
756	reduces hydrolase activity.
795	reduces poly(adp-ribose) glycohydrolase activity.
869	reduces poly(adp-ribose) glycohydrolase activity.
874	reduced poly(adp-ribose) glycohydrolase activity.
875	abolishes poly(adp-ribose) glycohydrolase activity.
902	slightly increases poly(adp-ribose) glycohydrolase efficiency and facilitates endo-glycohydrolitic action.
904	severly reduces poly(adp-ribose) glycohydrolase activity.

Function

Pathways and Gene Ontology

Reactome pathways

1 pathways

ID	Pathway
R-HSA-110362	POLB-Dependent Long Patch Base Excision Repair

MSigDB gene sets: 140 (showing top): TGGTGCT_MIR29A_MIR29B_MIR29C, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_REGULATION_OF_DNA_REPAIR, GOBP_CARBOHYDRATE_DERIVATIVE_METABOLIC_PROCESS, PUJANA_CHEK2_PCC_NETWORK, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_NUCLEOSIDE_TRIPHOSPHATE_METABOLIC_PROCESS, GOBP_REGULATION_OF_RESPONSE_TO_STRESS, GOBP_CARBOHYDRATE_METABOLIC_PROCESS, DACOSTA_UV_RESPONSE_VIA_ERCC3_COMMON_DN, GOBP_DNA_DAMAGE_RESPONSE, ATTCTTT_MIR186, SCHLOSSER_SERUM_RESPONSE_DN, BENPORATH_NOS_TARGETS

GO Biological Process (6): carbohydrate metabolic process (GO:0005975), regulation of DNA repair (GO:0006282), base-excision repair, gap-filling (GO:0006287), nucleotide-sugar metabolic process (GO:0009225), ATP generation from poly-ADP-D-ribose (GO:1990966), DNA damage response (GO:0006974)

GO Molecular Function (3): poly(ADP-ribose) glycohydrolase activity (GO:0004649), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (7): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), mitochondrial matrix (GO:0005759), cytosol (GO:0005829), nuclear body (GO:0016604), mitochondrion (GO:0005739)

Reactome top-level categories

Rollup of top-1 pathways:

Category	Pathways
Resolution of AP sites via the multiple-nucleotide patch replacement pathway	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	3
intracellular membrane-bounded organelle	2
cytoplasm	2
primary metabolic process	1
DNA repair	1
regulation of DNA metabolic process	1
regulation of cellular response to stress	1
DNA metabolic process	1
base-excision repair	1
nucleoside phosphate metabolic process	1
carbohydrate derivative metabolic process	1
macromolecule metabolic process	1
ATP metabolic process	1
cellular response to stress	1
hydrolase activity, hydrolyzing O-glycosyl compounds	1
binding	1
catalytic activity	1
nuclear lumen	1
intracellular anatomical structure	1
mitochondrion	1
intracellular organelle lumen	1
nucleoplasm	1
intracellular membraneless organelle	1

Protein interactions and networks

STRING

1424 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARG	PARP1	P09874	940
PARG	PARP2	Q9UGN5	897
PARG	ART5	Q96L15	881
PARG	ADPRS	Q9NX46	874
PARG	ARHGAP29	Q52LW3	862
PARG	MACROD1	Q9BQ69	821
PARG	AIFM1	O95831	804
PARG	ART3	Q13508	796
PARG	XRCC1	P18887	786
PARG	MACROD2	A1Z1Q3	777
PARG	OARD1	Q9Y530	777
PARG	PDE1A	P54750	761
PARG	PARP3	Q9Y6F1	756
PARG	NUDT5	Q9UKK9	756
PARG	ART1	P52961	744

IntAct

10 interactions, top by confidence:

A	B	Type	Score
ATF6	ATF6	psi-mi:“MI:0914”(association)	0.790
PARG	PARP1	psi-mi:“MI:0414”(enzymatic reaction)	0.440
LIN28A	MEX3A	psi-mi:“MI:0914”(association)	0.350
LIN28A	AGPS	psi-mi:“MI:0914”(association)	0.350
SPSB4	CCDC85C	psi-mi:“MI:0914”(association)	0.350
CENPM	DNM1L	psi-mi:“MI:0914”(association)	0.350
EZR	EEF2K	psi-mi:“MI:2364”(proximity)	0.270
H2BC10	SMCHD1	psi-mi:“MI:2364”(proximity)	0.270
PCNA	PARG	psi-mi:“MI:2364”(proximity)	0.270

BioGRID (37): PARG (Affinity Capture-MS), PARG (Proximity Label-MS), BRCA1 (Biochemical Activity), BARD1 (Affinity Capture-Western), PARG (Affinity Capture-MS), PARG (Affinity Capture-MS), PARG (Proximity Label-MS), PARG (Biochemical Activity), PARG (Proximity Label-MS), PARG (Proximity Label-MS), PARG (Affinity Capture-MS), PARG (Affinity Capture-MS), PARG (Affinity Capture-MS), PARG (Negative Genetic), PARG (Co-fractionation)

ESM2 similar proteins: A0A3Q2TTB3, A0JMR6, A4IIA7, F4JNY0, F6RRD7, I3XHK1, O60934, O88622, P14629, P28715, P79457, Q08DZ8, Q12789, Q17RS7, Q1LWH4, Q28I29, Q32PL8, Q3B7T1, Q4R7Q1, Q5FWP4, Q5M954, Q5QJC2, Q5RA37, Q5RCV3, Q5ZIN2, Q66J91, Q6GQV7, Q6NVF4, Q6P1E7, Q6P1H6, Q6P256, Q6P7W5, Q76CY8, Q7TP65, Q86W56, Q8BMI4, Q8C0W1, Q8C5W4, Q8GT06, Q8IXW5

Diamond homologs: O02776, O46043, O88622, Q867X0, Q86W56, Q8VYA1, Q9N5L4, Q9QYM2, Q9SKB3, P0C6C0, Q6NSW3

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	54
Likely benign	3
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

3504 predictions. Top by Δscore:

Variant	Effect	Δscore
10:49820289:TAAGG:T	acceptor_gain	1.0000
10:49820294:C:CC	acceptor_gain	1.0000
10:49841944:A:AC	donor_gain	1.0000
10:49841945:C:CC	donor_gain	1.0000
10:49841945:CTGG:C	donor_gain	1.0000
10:49842054:CGTCC:C	acceptor_gain	1.0000
10:49842056:TCC:T	acceptor_gain	1.0000
10:49842057:CCC:C	acceptor_gain	1.0000
10:49842058:CCT:C	acceptor_loss	1.0000
10:49842059:C:CC	acceptor_gain	1.0000
10:49842060:T:C	acceptor_loss	1.0000
10:49842066:A:T	acceptor_gain	1.0000
10:49843550:TCA:T	donor_loss	1.0000
10:49843551:CA:C	donor_loss	1.0000
10:49843552:A:AC	donor_gain	1.0000
10:49843553:C:CC	donor_gain	1.0000
10:49843553:C:CG	donor_loss	1.0000
10:49843553:CCTTT:C	donor_gain	1.0000
10:49843631:ACCTG:A	acceptor_loss	1.0000
10:49843633:C:CA	acceptor_loss	1.0000
10:49843633:C:CC	acceptor_gain	1.0000
10:49843634:TGAAA:T	acceptor_loss	1.0000
10:49857301:CTAA:C	donor_loss	1.0000
10:49857302:TAACC:T	donor_loss	1.0000
10:49857303:AACCT:A	donor_loss	1.0000
10:49857304:A:AT	donor_loss	1.0000
10:49857305:CC:C	donor_loss	1.0000
10:49857449:TCCAC:T	acceptor_gain	1.0000
10:49857450:CCAC:C	acceptor_gain	1.0000
10:49857450:CCACC:C	acceptor_gain	1.0000

AlphaMissense

6485 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
10:49832825:A:C	F875L	1.000
10:49832825:A:T	F875L	1.000
10:49832827:A:G	F875L	1.000
10:49832840:C:A	W870C	1.000
10:49832840:C:G	W870C	1.000
10:49832842:A:G	W870R	1.000
10:49832842:A:T	W870R	1.000
10:49841950:C:A	K847N	1.000
10:49841950:C:G	K847N	1.000
10:49857394:T:A	E755D	1.000
10:49857394:T:G	E755D	1.000
10:49857395:T:A	E755V	1.000
10:49857428:C:T	G744E	1.000
10:49857431:A:T	V743D	1.000
10:49857445:A:C	F738L	1.000
10:49857445:A:T	F738L	1.000
10:49857447:A:G	F738L	1.000
10:49865328:A:G	W708R	1.000
10:49865328:A:T	W708R	1.000
10:49879681:G:C	N660K	1.000
10:49879681:G:T	N660K	1.000
10:49915952:A:G	W568R	1.000
10:49915952:A:T	W568R	1.000
10:49922392:A:G	W536R	1.000
10:49922392:A:T	W536R	1.000
10:49922593:A:T	V511D	1.000
10:49922607:C:A	W506C	1.000
10:49922607:C:G	W506C	1.000
10:49922609:A:G	W506R	1.000
10:49922609:A:T	W506R	1.000

dbSNP variants (sampled 300 via entrez): RS1000086998 (10:49835923 C>A), RS1000292112 (10:49820732 A>AG), RS1000714436 (10:49841660 A>G), RS1000844558 (10:49822464 T>C,G), RS1000896909 (10:49822879 C>T), RS1001036296 (10:49837131 C>G), RS1001321040 (10:49843284 T>C), RS1002031722 (10:49831580 C>T), RS1002045111 (10:49838470 A>G), RS1002097422 (10:49838775 T>C), RS1002721374 (10:49844656 A>C,T), RS1002848026 (10:49826021 G>A,T), RS1003076499 (10:49833411 C>T), RS1003152805 (10:49839402 C>T), RS1003195809 (10:49819034 G>T)

Disease associations

OMIM: gene MIM:603501 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST002890_7	Prostate cancer	1.000000e-15
GCST008058_222	Estimated glomerular filtration rate	4.000000e-12
GCST008059_161	Estimated glomerular filtration rate	7.000000e-11
GCST012490_343	Femur bone mineral density x serum urate levels interaction	3.000000e-09

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004531	urate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1795143 (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: 476 (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
CHEMBL1208422	ROSE BENGAL FREE ACID	4	476

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

Binding affinities (BindingDB)

641 measured of 932 human assays (933 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	6 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	8 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-1-(1,3-thiazol-5-ylmethyl)-6H-quinazolin-1-ium-6-sulfonamide	IC50	8 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-[(2,4-dimethyl-1,3-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	11 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,4-dimethyl-1,3-oxazol-5-yl)methyl]-7-fluoro-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	11 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1-[(3-methylimidazol-4-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	19 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-[(2-methyl-1,3-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	20 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	23 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
7-fluoro-N-(1-methylcyclopropyl)-1-[(3-methyl-1,2-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	24 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1-[(3-methyl-1,2-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	24 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-1-(1,2-thiazol-4-ylmethyl)-6H-quinazolin-1-ium-6-sulfonamide	IC50	24 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-(cyclopropylmethyl)-7-fluoro-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	25 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-1-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	25 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
PDD00017273 (4)	IC50	26 nM
N-(1-cyanocyclopropyl)-3-[(2-methyl-1,3-oxazol-5-yl)methyl]-1-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	27 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
7-fluoro-N-(1-methylcyclopropyl)-1,3-bis[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	28 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	29 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(1-methylpyrrol-3-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	29 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-[1-(fluoromethyl)cyclopropyl]-3-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	29 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
US10239843, Example 590	IC50	30 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-1-[(3-methyl-1,2-thiazol-5-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	30 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-(cyclopropylmethyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	31 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1-[(2-methyl-1,3-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	34 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-1-[(3-methyl-1,2-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	35 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-1,3-bis[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	36 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-1-(1,3-oxazol-5-ylmethyl)-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	38 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-1-(1,2-oxazol-5-ylmethyl)-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	38 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-(cyclobutylmethyl)-N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	39 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
PDD00017238 (5)	IC50	40 nM
1-(cyclopropylmethyl)-N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	40 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-[(1-methylpyrazol-4-yl)methyl]-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	42 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(3-ethylimidazol-4-yl)methyl]-N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	42 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1-(3-methylbutyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	42 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-[(3-methyl-1,2-oxazol-5-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	43 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-1-(oxan-4-ylmethyl)-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	43 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1,3-bis[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	44 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
7-fluoro-N-(1-methylcyclopropyl)-1-[(3-methyloxetan-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	44 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-1-[(3-methyloxetan-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	47 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-cyanocyclopropyl)-1-(cyclopropylmethyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	47 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,5-dimethylpyrazol-3-yl)methyl]-7-fluoro-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	47 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-1,3-bis[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	48 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1,3-bis[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	48 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(4-fluorophenyl)methyl]-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4a,5,6,7,8,8a-hexahydroquinazoline-6-sulfonamide	IC50	49 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-1-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	49 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-[1-(fluoromethyl)cyclopropyl]-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	50 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1-(3-methylbut-2-enyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-4aH-quinazolin-1-ium-6-sulfonamide	IC50	51 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-1-prop-2-ynyl-6H-quinazolin-1-ium-6-sulfonamide	IC50	52 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-[1-(fluoromethyl)cyclopropyl]-1,3-bis[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	54 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	55 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG
N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-1-[[1-methyl-3-(trifluoromethyl)pyrazol-5-yl]methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	IC50	55 nM	US-10239843: 2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG

ChEMBL bioactivities

1204 potent at pChembl≥5 of 1244 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.84	Kd	1.45	nM	CHEMBL4290650
8.40	IC50	4	nM	CHEMBL4290666
8.32	EC50	4.8	nM	CHEMBL4290666
8.22	EC50	6	nM	CHEMBL4282478
8.22	IC50	6	nM	CHEMBL4282478
8.22	IC50	6	nM	CHEMBL5841488
8.15	IC50	7	nM	CHEMBL5846792
8.10	IC50	8	nM	CHEMBL5779623
8.10	IC50	8	nM	CHEMBL5759235
8.05	IC50	9	nM	CHEMBL5808260
8.04	EC50	9.2	nM	CHEMBL4290666
8.00	IC50	10	nM	CHEMBL5770565
7.96	IC50	11	nM	CHEMBL5879209
7.96	IC50	11	nM	CHEMBL5815651
7.92	IC50	12	nM	CHEMBL5951064
7.80	IC50	16	nM	CHEMBL6002898
7.77	IC50	17	nM	CHEMBL5987435
7.75	IC50	18	nM	CHEMBL4293745
7.72	EC50	19	nM	CHEMBL4290954
7.72	IC50	19	nM	CHEMBL4290954
7.72	IC50	19	nM	CHEMBL5918538
7.70	EC50	20	nM	CHEMBL4282478
7.70	IC50	20	nM	CHEMBL4459798
7.70	IC50	20	nM	CHEMBL4518815
7.70	IC50	20	nM	CHEMBL5981658
7.64	EC50	23	nM	CHEMBL4293745
7.64	IC50	23	nM	CHEMBL5865827
7.62	IC50	24	nM	CHEMBL5970309
7.62	IC50	24	nM	CHEMBL5887931
7.62	IC50	24	nM	CHEMBL6062334
7.60	IC50	25	nM	CHEMBL5990387
7.60	IC50	25	nM	CHEMBL5882944
7.58	EC50	26	nM	CHEMBL4286938
7.57	IC50	27	nM	CHEMBL5857418
7.55	EC50	28	nM	CHEMBL4290954
7.55	IC50	28	nM	CHEMBL5883286
7.54	EC50	29	nM	CHEMBL4278621
7.54	IC50	29	nM	CHEMBL4278621
7.54	IC50	29	nM	CHEMBL5984551
7.54	IC50	29	nM	CHEMBL5777112
7.54	EC50	29	nM	CHEMBL5887537
7.52	IC50	30	nM	CHEMBL4459166
7.52	IC50	30	nM	CHEMBL5821150
7.52	IC50	30	nM	CHEMBL5895594
7.51	IC50	31	nM	CHEMBL5845944
7.48	IC50	33	nM	CHEMBL5939055
7.47	IC50	34	nM	CHEMBL5940274
7.46	IC50	35	nM	CHEMBL6050716
7.44	IC50	36	nM	CHEMBL5759400
7.43	EC50	37	nM	CHEMBL4286938

PubChem BioAssay actives

146 with measured affinity, of 236 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-tert-butyl-9,10-dioxoanthracene-2-sulfonamide	1850548: Binding affinity to human PARG assessed as dissociation constant by SPR analysis	kd	0.0014	uM
1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0048	uM
1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0060	uM
1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0190	uM
N-[1-(fluoromethyl)cyclopropyl]-1-[(1-methylpyrazol-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536152: Inhibition of recombinant full-length human C-terminal His6-tagged PARG (1 to 976 residues) expressed in Escherichia coli BL21 (DE3) cells using 6HIS-TEV-PARylated-PARP1 (2 to 1014 residues) as substrate measured after 10 mins by HTRF assay	ic50	0.0200	uM
N-(1-methylcyclopropyl)-1-[(1-methylpyrazol-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536152: Inhibition of recombinant full-length human C-terminal His6-tagged PARG (1 to 976 residues) expressed in Escherichia coli BL21 (DE3) cells using 6HIS-TEV-PARylated-PARP1 (2 to 1014 residues) as substrate measured after 10 mins by HTRF assay	ic50	0.0200	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0230	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0260	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-6H-quinazolin-1-ium-6-sulfonamide	1802220: PARG Biochemical Assay from Article 10.1021/acschembio.6b00609: “First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.”	ic50	0.0260	uM
1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0290	uM
1-[(1-methylpyrazol-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-N-[1-(trideuteriomethyl)cyclopropyl]quinazoline-6-sulfonamide	1536152: Inhibition of recombinant full-length human C-terminal His6-tagged PARG (1 to 976 residues) expressed in Escherichia coli BL21 (DE3) cells using 6HIS-TEV-PARylated-PARP1 (2 to 1014 residues) as substrate measured after 10 mins by HTRF assay	ic50	0.0300	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0380	uM
1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-N-(1-methylcyclopropyl)-2-oxo-3-(1,2,4-thiadiazol-5-yl)benzimidazole-5-sulfonamide	1802220: PARG Biochemical Assay from Article 10.1021/acschembio.6b00609: “First-in-Class Chemical Probes against Poly(ADP-ribose) Glycohydrolase (PARG) Inhibit DNA Repair with Differential Pharmacology to Olaparib.”	ic50	0.0400	uM
N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxo-1-prop-2-ynylquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0450	uM
1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.0490	uM
N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxo-1-prop-2-ynylquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0520	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0640	uM
N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-1-(oxetan-3-ylmethyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.0690	uM
N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxo-1-prop-2-ynylquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.0760	uM
1-ethyl-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.0780	uM
1-ethyl-N-[1-(fluoromethyl)cyclopropyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536153: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 30 to 120 mins by Alexafluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ic50	0.0800	uM
1-ethyl-N-(1-methylcyclopropyl)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.1200	uM
1-ethyl-N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.1200	uM
[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(2R,3R,4S)-3,4-dihydroxypyrrolidin-2-yl]methyl hydrogen phosphate	610958: Inhibition of PARG using [alpha-32P]ADP-ribose polymers after 5 mins by TRAP assay	ic50	0.1200	uM
1-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.1800	uM
3-methyl-N-(1-methylcyclopropyl)-2,4-dioxo-1-prop-2-ynylquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.2500	uM
3-(cyanomethyl)-N-(1-methylcyclopropyl)-2,4-dioxo-1-prop-2-ynylquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.2500	uM
3-(cyanomethyl)-1-(cyclopropylmethyl)-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.2700	uM
3-(cyanomethyl)-1-[(2,5-dimethylpyrazol-3-yl)methyl]-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.2800	uM
N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-1-(oxetan-3-ylmethyl)-2,4-dioxoquinazoline-6-sulfonamide	1418899: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 1 hr by Alexofluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ec50	0.2800	uM
N-[1-(fluoromethyl)cyclopropyl]-1-methyl-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536153: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 30 to 120 mins by Alexafluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ic50	0.2900	uM
N-[1-(difluoromethyl)cyclopropyl]-1-[(1-methylpyrazol-3-yl)methyl]-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536152: Inhibition of recombinant full-length human C-terminal His6-tagged PARG (1 to 976 residues) expressed in Escherichia coli BL21 (DE3) cells using 6HIS-TEV-PARylated-PARP1 (2 to 1014 residues) as substrate measured after 10 mins by HTRF assay	ic50	0.3200	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(1-methylpyrazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1536153: Inhibition of PARG in human HeLa cells assessed as induction of MMS-induced PAR chains preincubated for 1 hr followed by MMS addition and measured after 30 to 120 mins by Alexafluor 488-conjugated secondary antibody and Hoechst 33342 staining based assay	ic50	0.3300	uM
3-[[1-(cyanomethyl)pyrazol-4-yl]methyl]-1-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.3700	uM
1-[(2,5-dimethylpyrazol-3-yl)methyl]-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.3800	uM
1-methyl-N-(1-methylcyclopropyl)-2,4-dioxo-3-(1H-pyrazol-4-ylmethyl)quinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.3800	uM
1-(cyclopropylmethyl)-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4400	uM
3-[(1-ethylpyrazol-4-yl)methyl]-1-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4500	uM
1-[(4-methoxyphenyl)methyl]-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4500	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(5-methyl-1,3,4-thiadiazol-2-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4700	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(3-methyl-1,2-oxazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4700	uM
3-[(2-amino-1,3-thiazol-5-yl)methyl]-1-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4800	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(2-methyl-1,3-thiazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.4800	uM
1-[(4-fluorophenyl)methyl]-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.5300	uM
1-(cyclohexylmethyl)-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.5600	uM
3-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]-1-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.6200	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(5-methyl-1,2-oxazol-4-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.7700	uM
1-[(3-methoxyphenyl)methyl]-3-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.8600	uM
1-methyl-N-(1-methylcyclopropyl)-3-[(4-methylthiadiazol-5-yl)methyl]-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.8800	uM
3-[(2,4-dimethyl-1,3-thiazol-5-yl)methyl]-1-methyl-N-(1-methylcyclopropyl)-2,4-dioxoquinazoline-6-sulfonamide	1418898: Inhibition of human full length PARG using Bt-NAD ribosylated PARP1 substrate after 10 mins by TR-FRET assay	ec50	0.9100	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects reaction, increases expression, increases response to substance	3
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
methylmercuric chloride	decreases response to substance	1
triphenyl phosphate	affects expression	1
bisphenol A	affects cotreatment, decreases methylation	1
glycidyl methacrylate	increases expression	1
ascorbate-2-phosphate	affects cotreatment, decreases reaction, increases expression, increases reaction	1
kojic acid	increases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
coumarin	decreases phosphorylation	1
beta-glycerophosphoric acid	affects cotreatment, decreases reaction, increases expression, increases reaction	1
myricetin	decreases activity	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
di-n-butylphosphoric acid	affects expression	1
CGP 52608	affects binding, increases reaction	1
Fulvestrant	affects cotreatment, decreases methylation	1
Rosmarinic Acid	decreases activity	1
Air Pollutants, Occupational	decreases expression	1
Arbutin	increases expression	1
Caffeine	affects phosphorylation	1
Cholecalciferol	affects cotreatment, decreases reaction, increases expression, increases reaction	1
Dexamethasone	increases reaction, affects cotreatment, decreases reaction, increases expression	1
Doxorubicin	decreases expression	1
Ellagic Acid	decreases activity	1
Endosulfan	decreases expression	1
Enzyme Inhibitors	decreases activity, increases O-linked glycosylation	1
Hydrogen Peroxide	increases expression	1
Ivermectin	decreases expression	1
Ketoconazole	increases expression	1

ChEMBL screening assays

17 unique, capped per target: 17 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1814966	Binding	Inhibition of PARG using [alpha-32P]ADP-ribose polymers after 5 mins by TRAP assay	Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG). — J Med Chem

Cellosaurus cell lines

17 cell lines: 15 cancer cell line, 1 transformed cell line, 1 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D1Y4	Abcam A-549 PARG KO	Cancer cell line	Male
CVCL_D2CC	Abcam HCT 116 PARG KO	Cancer cell line	Male
CVCL_E8DG	BPS Bioscience HeLa PARG KO	Cancer cell line	Female
CVCL_KT88	HeLa SilenciX PARG	Cancer cell line	Female
CVCL_QZ51	HEK293T shPARG	Transformed cell line	Female
CVCL_QZ52	HCT 116 shPARG	Cancer cell line	Male
CVCL_RA87	HCC1937 shPARG	Cancer cell line	Female
CVCL_RA88	MCF-10A shPARG	Spontaneously immortalized cell line	Female
CVCL_RA89	MCF-7 shPARG	Cancer cell line	Female
CVCL_RA90	MDA-MB-231 shPARG	Cancer cell line	Female

Clinical trials (associated diseases)

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