PARP8

Summary

PARP8 (poly(ADP-ribose) polymerase family member 8, HGNC:26124) is a protein-coding gene on chromosome 5q11.1, encoding Protein mono-ADP-ribosyltransferase PARP8 (Q8N3A8). Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins.

Enables NAD+-protein mono-ADP-ribosyltransferase activity. Involved in protein auto-ADP-ribosylation. Predicted to be active in endoplasmic reticulum tubular network and nuclear envelope.

Source: NCBI Gene 79668 — RefSeq curated summary.

At a glance

• GWAS associations: 12
• Clinical variants (ClinVar): 113 total
• Druggable target: yes — 3 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_024615

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:26124
Approved symbol	PARP8
Name	poly(ADP-ribose) polymerase family member 8
Location	5q11.1
Locus type	gene with protein product
Status	Approved
Aliases	FLJ21308, pART16, ARTD16
Ensembl gene	ENSG00000151883
Ensembl biotype	protein_coding
Entrez	79668

Gene structure

Transcript identifiers

Ensembl transcripts: 22 — 10 protein_coding, 6 nonsense_mediated_decay, 5 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000281631, ENST00000502524, ENST00000503046, ENST00000503193, ENST00000503561, ENST00000503665, ENST00000503707, ENST00000503790, ENST00000503888, ENST00000505180, ENST00000505554, ENST00000505697, ENST00000507812, ENST00000510040, ENST00000510303, ENST00000511363, ENST00000513414, ENST00000513738, ENST00000514067, ENST00000515166, ENST00000515175, ENST00000898727

RefSeq mRNA: 5 — MANE Select: NM_024615 NM_001178055, NM_001178056, NM_001331028, NM_001427055, NM_024615

CCDS: CCDS3954, CCDS54849, CCDS82996

Canonical transcript exons

ENST00000281631 — 26 exons

Exon	Start	End
ENSE00001848826	50841966	50846519
ENSE00002062768	50666637	50667186
ENSE00003464714	50826755	50826803
ENSE00003471220	50832781	50832854
ENSE00003479261	50760292	50760362
ENSE00003482062	50815432	50815524
ENSE00003500473	50794853	50795417
ENSE00003508032	50829892	50829961
ENSE00003521644	50828312	50828384
ENSE00003536800	50778560	50778650
ENSE00003537028	50796982	50797032
ENSE00003549962	50794207	50794332
ENSE00003554318	50761821	50761898
ENSE00003585559	50763148	50763242
ENSE00003613761	50833979	50834048
ENSE00003614172	50827944	50828056
ENSE00003624524	50759643	50759732
ENSE00003627797	50797138	50797233
ENSE00003645724	50750151	50750188
ENSE00003652908	50778069	50778129
ENSE00003660055	50788523	50788589
ENSE00003660919	50834931	50835015
ENSE00003674375	50821213	50821338
ENSE00003681724	50822335	50822400
ENSE00003683796	50824908	50824975
ENSE00003687831	50668071	50668125

Expression profiles

Bgee: expression breadth ubiquitous, 256 present calls, max score 96.32.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 6.5897 / max 169.1343, expressed in 1325 samples.

FANTOM5 promoters (11 alternative TSS)

Promoter ID	TPM avg	Samples expressed
56364	2.1489	740
56366	1.4292	654
56363	0.9156	262
56365	0.8052	478
56368	0.4606	240
56362	0.2230	78
56367	0.1992	83
56374	0.1525	48
56369	0.1184	37
56370	0.1131	36

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
granulocyte	CL:0000094	96.32	gold quality
monocyte	CL:0000576	96.20	gold quality
leukocyte	CL:0000738	96.18	gold quality
mononuclear cell	CL:0000842	96.18	gold quality
blood	UBERON:0000178	96.07	gold quality
spleen	UBERON:0002106	93.63	gold quality
left lobe of thyroid gland	UBERON:0001120	93.54	gold quality
bone marrow cell	CL:0002092	93.24	gold quality
right lobe of thyroid gland	UBERON:0001119	93.23	gold quality
thyroid gland	UBERON:0002046	93.13	gold quality
gall bladder	UBERON:0002110	92.89	gold quality
bone marrow	UBERON:0002371	92.80	gold quality
right uterine tube	UBERON:0001302	91.83	gold quality
colonic epithelium	UBERON:0000397	91.81	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	91.81	gold quality
lymph node	UBERON:0000029	91.46	gold quality
islet of Langerhans	UBERON:0000006	89.86	gold quality
small intestine Peyer’s patch	UBERON:0003454	89.86	gold quality
right lung	UBERON:0002167	89.41	gold quality
bone element	UBERON:0001474	89.30	gold quality
adenohypophysis	UBERON:0002196	89.08	gold quality
vermiform appendix	UBERON:0001154	89.07	gold quality
body of stomach	UBERON:0001161	88.69	gold quality
upper lobe of left lung	UBERON:0008952	88.33	gold quality
stomach	UBERON:0000945	88.21	gold quality
Brodmann (1909) area 23	UBERON:0013554	88.01	gold quality
right coronary artery	UBERON:0001625	88.00	gold quality
small intestine	UBERON:0002108	87.79	gold quality
mucosa of stomach	UBERON:0001199	87.78	gold quality
upper lobe of lung	UBERON:0008948	87.45	gold quality

Single-cell (SCXA)

Detected in 11 experiment(s), a significant marker in 9.

Experiment	Marker?	Max mean expression
E-ANND-2	yes	2846.41
E-GEOD-180759	yes	2779.43
E-HCAD-25	yes	1198.80
E-CURD-122	yes	41.56
E-CURD-46	yes	39.16
E-MTAB-6678	yes	24.60
E-ANND-3	yes	20.71
E-CURD-88	yes	15.36
E-CURD-112	yes	4.85
E-CURD-97	no	1103.23
E-CURD-89	no	723.28

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

200 targeting PARP8, 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-5692A	100.00	74.40	6850
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4500	99.99	72.72	2367
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-19A-3P	99.98	75.33	2762
HSA-MIR-19B-3P	99.98	75.44	2754
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-3617-3P	99.98	67.86	918
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-LET-7A-5P	99.98	72.29	1790
HSA-LET-7B-5P	99.98	72.31	1790
HSA-LET-7C-5P	99.98	72.29	1790

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	parp8	ENSDARG00000059789
mus_musculus	Parp8	ENSMUSG00000021725
rattus_norvegicus	Parp8	ENSRNOG00000010824

Paralogs (2): PARP6 (ENSG00000137817), PARP16 (ENSG00000138617)

Protein

Protein identifiers

Protein mono-ADP-ribosyltransferase PARP8 — Q8N3A8 (reviewed: Q8N3A8)

Alternative names: ADP-ribosyltransferase diphtheria toxin-like 16, Poly [ADP-ribose] polymerase 8

All UniProt accessions (13): Q8N3A8, D6R914, D6R9T2, D6RAL6, D6RB30, D6RC81, D6RCA6, D6RCN2, D6RF37, D6RF59, D6RFH0, D6RGZ9, E9PFI7

UniProt curated annotations — full annotation on UniProt →

Function. Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins.

Post-translational modifications. Auto-mono-ADP-ribosylated.

Similarity. Belongs to the ARTD/PARP family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q8N3A8-1	1	yes
Q8N3A8-2	2

RefSeq proteins (5): NP_001171526, NP_001171527, NP_001317957, NP_001413984, NP_078891* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR012317	Poly(ADP-ribose)pol_cat_dom	Domain
IPR051838	ARTD_PARP	Family

Pfam: PF00644

Catalyzed reactions (Rhea), 1 shown:

• L-cysteinyl-[protein] + NAD(+) = S-(ADP-D-ribosyl)-L-cysteinyl-[protein] + nicotinamide + H(+) (RHEA:56612)

UniProt features (14 total): modified residue 4, region of interest 3, compositionally biased region 2, chain 1, domain 1, splice variant 1, sequence variant 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q8N3A8-F1	66.07	0.26

Functional residue map

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

Post-translational modifications (4): 395, 332, 367, 376

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-196807	Nicotinate metabolism
R-HSA-9683610	Maturation of nucleoprotein
R-HSA-9694631	Maturation of nucleoprotein

MSigDB gene sets: 389 (showing top): CREL_01, BENPORATH_ES_WITH_H3K27ME3, GNF2_CASP8, GOBP_RESPONSE_TO_ENDOPLASMIC_RETICULUM_STRESS, MODULE_511, TATTATA_MIR374, CAGCTG_AP4_Q5, FOXD3_01, GOBP_CELLULAR_RESPONSE_TO_TOPOLOGICALLY_INCORRECT_PROTEIN, NFKB_Q6, GOMF_KINASE_ACTIVATOR_ACTIVITY, NFKB_C, IRF7_01, SOX9_B1, FOSTER_TOLERANT_MACROPHAGE_UP

GO Biological Process (2): endoplasmic reticulum unfolded protein response (GO:0030968), protein auto-ADP-ribosylation (GO:0070213)

GO Molecular Function (8): NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), nucleotidyltransferase activity (GO:0016779), kinase binding (GO:0019900), protein serine/threonine kinase activator activity (GO:0043539), NAD+-protein-cysteine ADP-ribosyltransferase activity (GO:0140803), NAD+-protein mono-ADP-ribosyltransferase activity (GO:1990404), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757)

GO Cellular Component (3): nuclear envelope (GO:0005635), membrane (GO:0016020), endoplasmic reticulum tubular network (GO:0071782)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Metabolism of water-soluble vitamins and cofactors	1
Translation of Structural Proteins	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
pentosyltransferase activity	2
cellular response to unfolded protein	1
response to endoplasmic reticulum stress	1
intracellular signal transduction	1
post-translational protein modification	1
transferase activity, transferring phosphorus-containing groups	1
enzyme binding	1
protein serine/threonine kinase activity	1
protein kinase activator activity	1
NAD+-protein mono-ADP-ribosyltransferase activity	1
catalytic activity, acting on a protein	1
catalytic activity	1
transferase activity	1
nucleus	1
endomembrane system	1
organelle envelope	1
cellular anatomical structure	1
endoplasmic reticulum subcompartment	1

Protein interactions and networks

STRING

2500 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARP8	PARP11	Q9NR21	705
PARP8	PARP10	Q53GL7	699
PARP8	PARP15	Q460N3	675
PARP8	PARP4	Q9UKK3	635
PARP8	PARP3	Q9Y6F1	630
PARP8	PARP12	Q9H0J9	613
PARP8	PARP14	Q460N5	594
PARP8	PARP9	Q8IXQ6	591
PARP8	PARP2	Q9UGN5	555
PARP8	ZC3HAV1	Q7Z2W4	529
PARP8	TIPARP	Q7Z3E1	523
PARP8	TNKS2	Q9H2K2	506
PARP8	TNKS	O95271	487
PARP8	PDE4DIP	Q5VU43	439
PARP8	ART5	Q96L15	417

IntAct

16 interactions, top by confidence:

A	B	Type	Score
YWHAG	BLTP3B	psi-mi:“MI:0914”(association)	0.640
YWHAH	PLEKHG3	psi-mi:“MI:0914”(association)	0.610
YWHAB	BLTP3B	psi-mi:“MI:0914”(association)	0.610
YWHAE	PIK3C2A	psi-mi:“MI:0914”(association)	0.570
YWHAH	BLTP3B	psi-mi:“MI:0914”(association)	0.570
YWHAZ	PIK3C2A	psi-mi:“MI:0914”(association)	0.570
PARP8	HTR6	psi-mi:“MI:0915”(physical association)	0.370
HIF1AN	CNOT1	psi-mi:“MI:0914”(association)	0.350
YWHAG	C1orf226	psi-mi:“MI:0914”(association)	0.350
PARP8	PRMT3	psi-mi:“MI:0914”(association)	0.350
M		psi-mi:“MI:0914”(association)	0.350
YWHAQ	MCRIP1	psi-mi:“MI:0914”(association)	0.350
YWHAG	FOXO6	psi-mi:“MI:0914”(association)	0.350
PARP8	GSK3A	psi-mi:“MI:0914”(association)	0.350
CREB3L2	PLEKHG3	psi-mi:“MI:0914”(association)	0.350

BioGRID (23): PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-RNA), PARP8 (Two-hybrid), PARP8 (Affinity Capture-RNA), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PUS1 (Affinity Capture-MS), GSK3A (Affinity Capture-MS), YWHAH (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS), PARP8 (Affinity Capture-MS)

ESM2 similar proteins: A0A0R4IXF6, A0JMR6, A5WW08, F4HRV8, O17482, O60934, O88974, O94988, P12757, P14629, P49021, P79457, Q08AW4, Q08D35, Q12789, Q28C33, Q2TB10, Q3B7T1, Q3UD82, Q3UWM4, Q498F0, Q5F363, Q5F3F2, Q5FWP4, Q5HYC2, Q5JSH3, Q5R431, Q5R7T9, Q5R9R1, Q5RGA4, Q5VVJ2, Q60665, Q63505, Q69Z66, Q6GQV7, Q6INA9, Q6NVE8, Q6P256, Q6ZMT4, Q8C5W4

Diamond homologs: Q2NL67, Q3UD82, Q5RDU4, Q6P6P7, Q8N3A8

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 19 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	268.7×	2e-12
Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex	6	237.1×	2e-12
SARS-CoV-1 targets host intracellular signalling and regulatory pathways	6	237.1×	2e-12
Activation of BH3-only proteins	6	175.2×	1e-11
RHO GTPases activate PKNs	6	112.0×	2e-10
Intrinsic Pathway for Apoptosis	6	103.3×	3e-10
SARS-CoV-1-host interactions	6	62.0×	6e-09
Apoptosis	6	59.3×	7e-09

GO biological processes:

GO term	Partners	Fold	FDR
protein targeting	5	107.8×	1e-07
intracellular protein localization	6	36.9×	7e-07

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	73
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

4553 predictions. Top by Δscore:

Variant	Effect	Δscore
5:50666178:G:T	donor_gain	1.0000
5:50723489:G:GT	donor_gain	1.0000
5:50759639:GCAG:G	acceptor_loss	1.0000
5:50759641:A:AG	acceptor_gain	1.0000
5:50759641:A:C	acceptor_loss	1.0000
5:50759642:G:GT	acceptor_gain	1.0000
5:50759642:GA:G	acceptor_gain	1.0000
5:50759642:GAT:G	acceptor_gain	1.0000
5:50759642:GATA:G	acceptor_gain	1.0000
5:50759642:GATAA:G	acceptor_gain	1.0000
5:50759708:G:GG	donor_gain	1.0000
5:50759730:CAGGT:C	donor_loss	1.0000
5:50759731:AG:A	donor_loss	1.0000
5:50759732:GGTAA:G	donor_loss	1.0000
5:50759734:T:G	donor_loss	1.0000
5:50761810:A:AG	acceptor_gain	1.0000
5:50761811:T:G	acceptor_gain	1.0000
5:50761813:A:AG	acceptor_gain	1.0000
5:50761814:T:G	acceptor_gain	1.0000
5:50761818:A:AG	acceptor_gain	1.0000
5:50761818:AAG:A	acceptor_gain	1.0000
5:50761819:A:AG	acceptor_gain	1.0000
5:50761819:AG:A	acceptor_gain	1.0000
5:50761820:G:A	acceptor_gain	1.0000
5:50761820:G:GT	acceptor_gain	1.0000
5:50761820:GGA:G	acceptor_gain	1.0000
5:50761894:GGCAG:G	donor_gain	1.0000
5:50761895:GCAG:G	donor_gain	1.0000
5:50761895:GCAGG:G	donor_gain	1.0000
5:50761899:G:GC	donor_loss	1.0000

AlphaMissense

5601 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
5:50763185:T:C	L154P	1.000
5:50763206:T:A	V161D	1.000
5:50778104:T:C	L185P	1.000
5:50778578:T:A	W200R	1.000
5:50778578:T:C	W200R	1.000
5:50778609:T:A	V210D	1.000
5:50778612:G:C	R211P	1.000
5:50778615:T:C	L212P	1.000
5:50788526:C:A	P225H	1.000
5:50788538:T:A	V229D	1.000
5:50788583:T:C	L244P	1.000
5:50797183:T:C	C509R	1.000
5:50797184:G:A	C509Y	1.000
5:50797184:G:T	C509F	1.000
5:50797185:T:G	C509W	1.000
5:50797192:T:C	C512R	1.000
5:50797193:G:A	C512Y	1.000
5:50797194:T:G	C512W	1.000
5:50797229:T:A	L524H	1.000
5:50815441:T:A	C529S	1.000
5:50815441:T:C	C529R	1.000
5:50815442:G:A	C529Y	1.000
5:50815442:G:C	C529S	1.000
5:50815442:G:T	C529F	1.000
5:50815443:T:G	C529W	1.000
5:50815454:T:C	L533P	1.000
5:50815456:T:A	C534S	1.000
5:50815456:T:C	C534R	1.000
5:50815457:G:A	C534Y	1.000
5:50815457:G:C	C534S	1.000

dbSNP variants (sampled 300 via entrez): RS1000052886 (5:50688972 G>A), RS1000083098 (5:50743579 G>A), RS1000083524 (5:50688675 A>G,T), RS1000094818 (5:50784044 A>C), RS1000130279 (5:50772188 T>A,C), RS1000139052 (5:50705435 TAAG>T), RS1000139567 (5:50812298 G>T), RS1000152461 (5:50665117 T>C), RS1000179245 (5:50665358 G>A,T), RS1000209399 (5:50788452 A>C,G,T), RS1000229933 (5:50828158 A>C,G), RS1000255294 (5:50834983 T>C), RS1000259214 (5:50754622 T>G), RS1000287475 (5:50807220 ACT>A), RS1000304690 (5:50711569 T>C)

Disease associations

OMIM: gene `` | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

12 associations (top):

Study	Trait	p-value
GCST001561_2	Myopia (pathological)	4.000000e-06
GCST002092_3	Callous-unemotional behaviour	5.000000e-06
GCST002701_30	Verbal declarative memory	1.000000e-06
GCST002701_31	Verbal declarative memory	3.000000e-08
GCST003074_10	Cerebral amyloid deposition in APOEe4 non-carriers (PET imaging)	8.000000e-08
GCST003991_17	Childhood ear infection	3.000000e-07
GCST007325_69	General risk tolerance (MTAG)	5.000000e-10
GCST007847_111	Type 2 diabetes	8.000000e-09
GCST007847_57	Type 2 diabetes	2.000000e-07
GCST010118_42	Type 2 diabetes	4.000000e-08
GCST010724_10	HOMA-B (corrected for HOMA-IR)	6.000000e-09
GCST010724_9	HOMA-B (corrected for HOMA-IR)	6.000000e-09

EFO canonical traits (8, from GWAS)

EFO ID	Trait name
EFO:0004207	pathological myopia
EFO:0005322	callous-unemotional behaviour
EFO:0004874	memory performance
EFO:0006805	word list delayed recall measurement
EFO:0007707	cerebral amyloid deposition measurement
EFO:0007904	susceptibility to childhood ear infection measurement
EFO:0008579	risk-taking behaviour
EFO:0004469	HOMA-B

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL3091262 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 20,686 (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
CHEMBL3137320	TALAZOPARIB	4	5,534
CHEMBL521686	OLAPARIB	4	13,038
CHEMBL4112930	PAMIPARIB	3	2,114

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

ChEMBL bioactivities

7 potent at pChembl≥5 of 7 total, top 7 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.89	IC50	13	nM	CHEMBL5403305
6.62	IC50	240	nM	OLAPARIB
5.96	Kd	1100	nM	TALAZOPARIB
5.89	IC50	1300	nM	CHEMBL5199558
5.75	IC50	1789	nM	OLAPARIB
5.53	IC50	2934	nM	CHEMBL5558410
5.08	IC50	8400	nM	PAMIPARIB

PubChem BioAssay actives

7 with measured affinity, of 91 total; 6 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
sodium 1-[[4-fluoro-3-(3-oxo-4-pentan-3-ylpiperazine-1-carbonyl)phenyl]methyl]quinazolin-3-ide-2,4-dione	2019988: Inhibition of PARP8 (unknown origin)	ic50	0.0130	uM
Olaparib	2019988: Inhibition of PARP8 (unknown origin)	ic50	0.2400	uM
Talazoparib	1895784: Binding affinity to PARP8 (unknown origin) assessed as apparent dissociation constant	kd	1.1000	uM
3-[4-(2-hydroxypropan-2-yl)phenyl]-6-methyl-2H-pyrrolo[1,2-a]pyrazin-1-one	1925210: Inhibition of human PARP8 by chemiluminescence assay	ic50	1.3000	uM
4-(5-chloro-2-methoxyphenyl)-N-[5-[[1-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]piperidin-4-yl]methoxy]-1,3,4-thiadiazol-2-yl]-6-methylpyridine-3-carboxamide	2080541: Inhibition of PARP8 (unknown origin)	ic50	2.9340	uM
(2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one	1683875: Inhibition of PARP-8 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay	ic50	8.4000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, decreases expression, decreases methylation	6
sodium arsenite	decreases expression, affects cotreatment, increases abundance	3
trichostatin A	affects cotreatment, decreases expression	2
entinostat	decreases expression, affects cotreatment	2
Silicon Dioxide	decreases expression	2
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
propionaldehyde	increases expression	1
bisphenol A	affects cotreatment, increases methylation	1
butyraldehyde	increases expression	1
manganese chloride	affects cotreatment, decreases expression, increases abundance	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
pentanal	increases expression	1
phenethyl isothiocyanate	increases expression	1
di-n-butylphosphoric acid	affects expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	decreases expression, affects cotreatment	1
abrine	increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
MRK 003	decreases expression	1
bisphenol S	decreases methylation	1
Fulvestrant	affects cotreatment, increases methylation	1
Acetaminophen	increases expression	1
Air Pollutants	increases abundance, increases expression	1
Aldehydes	increases expression	1
Arsenic	affects cotreatment, decreases expression, increases abundance	1
Benzo(a)pyrene	decreases methylation	1
Calcitriol	decreases 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
CHEMBL3096300	Binding	Binding affinity to ATRD8 (unknown origin) assessed as change in melting temperature by thermal stabilization assay	Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3. — J Med Chem

Clinical trials (associated diseases)

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