PARP14

Summary

PARP14 (poly(ADP-ribose) polymerase family member 14, HGNC:29232) is a protein-coding gene on chromosome 3q21.1, encoding Protein mono-ADP-ribosyltransferase PARP14 (Q460N5). ADP-ribosyltransferase that mediates mono-ADP-ribosylation of glutamate residues on target proteins.

This gene encodes a member of the poly(ADP-ribose) polymerase (PARP) protein family. The encoded anti-apoptotic protein may regulate aerobic glycolysis and promote survival of cancer cells. Increased expression of this gene has been reported in a variety of tumor types.

Source: NCBI Gene 54625 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 230 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_017554

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:29232
Approved symbol	PARP14
Name	poly(ADP-ribose) polymerase family member 14
Location	3q21.1
Locus type	gene with protein product
Status	Approved
Aliases	KIAA1268, pART8, ARTD8, BAL2
Ensembl gene	ENSG00000173193
Ensembl biotype	protein_coding
OMIM	610028
Entrez	54625

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 3 protein_coding, 2 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000460683, ENST00000474629, ENST00000474669, ENST00000475640, ENST00000483611, ENST00000494811, ENST00000649945, ENST00000935443

RefSeq mRNA: 1 — MANE Select: NM_017554 NM_017554

CCDS: CCDS46894

Canonical transcript exons

ENST00000474629 — 17 exons

Exon	Start	End
ENSE00001853157	122680839	122681070
ENSE00002326770	122699390	122701635
ENSE00002330585	122687080	122687113
ENSE00002347400	122685185	122685318
ENSE00002378712	122692301	122692543
ENSE00002385793	122695426	122695662
ENSE00003466230	122728308	122730840
ENSE00003507932	122708190	122708268
ENSE00003519859	122718359	122718958
ENSE00003568593	122703742	122703978
ENSE00003569535	122704527	122704748
ENSE00003614291	122713872	122713934
ENSE00003617544	122727812	122727986
ENSE00003635731	122720255	122720388
ENSE00003641756	122713424	122713573
ENSE00003654293	122714262	122714429
ENSE00003688174	122718071	122718277

Expression profiles

Bgee: expression breadth ubiquitous, 243 present calls, max score 96.04.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 13.0058 / max 456.8134, expressed in 1626 samples.

FANTOM5 promoters (10 alternative TSS)

Promoter ID	TPM avg	Samples expressed
38253	5.5660	1403
38254	4.6847	1080
202900	0.7703	295
38252	0.7212	447
38257	0.6543	204
38256	0.1991	69
38251	0.1937	97
38255	0.1053	42
38250	0.0712	34
38249	0.0398	19

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	96.04	gold quality
kidney epithelium	UBERON:0004819	96.01	silver quality
nasal cavity epithelium	UBERON:0005384	95.10	gold quality
calcaneal tendon	UBERON:0003701	94.92	gold quality
leukocyte	CL:0000738	94.11	gold quality
monocyte	CL:0000576	94.10	gold quality
spleen	UBERON:0002106	94.00	gold quality
granulocyte	CL:0000094	93.94	gold quality
decidua	UBERON:0002450	93.85	gold quality
vermiform appendix	UBERON:0001154	93.77	gold quality
caecum	UBERON:0001153	93.34	gold quality
lymph node	UBERON:0000029	93.33	gold quality
upper lobe of left lung	UBERON:0008952	92.81	gold quality
upper lobe of lung	UBERON:0008948	92.38	gold quality
bone marrow cell	CL:0002092	92.32	gold quality
epithelium of nasopharynx	UBERON:0001951	92.19	gold quality
right lung	UBERON:0002167	92.09	gold quality
trigeminal ganglion	UBERON:0001675	92.03	gold quality
ileal mucosa	UBERON:0000331	91.99	gold quality
upper arm skin	UBERON:0004263	91.65	silver quality
lung	UBERON:0002048	91.60	gold quality
pylorus	UBERON:0001166	91.49	gold quality
cardia of stomach	UBERON:0001162	91.32	gold quality
epithelial cell of pancreas	CL:0000083	91.29	gold quality
left ventricle myocardium	UBERON:0006566	91.25	silver quality
tonsil	UBERON:0002372	91.10	gold quality
colonic epithelium	UBERON:0000397	90.89	gold quality
cardiac muscle of right atrium	UBERON:0003379	90.70	silver quality
blood	UBERON:0000178	90.52	gold quality
tendon	UBERON:0000043	90.04	gold quality

Single-cell (SCXA)

Detected in 8 experiment(s), a significant marker in 4.

Experiment	Marker?	Max mean expression
E-CURD-53	yes	2294.90
E-MTAB-7052	yes	955.74
E-MTAB-8559	yes	627.43
E-MTAB-7051	no	3656.91
E-GEOD-100618	no	2080.96
E-GEOD-86618	no	854.20
E-HCAD-13	no	109.48
E-ANND-3	no	0.00

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

1 targets.

Target	Regulation
PARP9	Repression

Upstream regulators (CollecTRI, top): PARP9, STAT1

miRNA regulators (miRDB)

96 targeting PARP14, 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-1252-5P	100.00	69.80	2774
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-4455	100.00	65.48	1587
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-3185	99.99	68.12	1959
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-3148	99.97	75.06	6478
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-651-3P	99.94	73.48	5177
HSA-MIR-3143	99.93	71.96	3104
HSA-MIR-1297	99.91	73.41	3162
HSA-MIR-124-3P	99.89	73.74	3043
HSA-MIR-506-3P	99.89	73.55	3057
HSA-MIR-5582-3P	99.86	72.48	4221
HSA-MIR-659-3P	99.85	70.69	1620
HSA-MIR-4760-5P	99.80	69.88	1619
HSA-MIR-489-3P	99.80	66.46	839
HSA-MIR-4668-5P	99.79	70.58	3782
HSA-MIR-26A-5P	99.78	73.52	2303
HSA-MIR-26B-5P	99.78	73.51	2305
HSA-MIR-4465	99.71	72.56	2096
HSA-MIR-4729	99.69	72.18	4233

Literature-anchored findings (GeneRIF, showing 22)

• BAL macro domains repress transcription when tethered to a promoter; BAL2 and BAL3, but not BAL1, exhibit PARP activity (PMID:16061477)
• PARP enzymatic activity is associated with CoaSt6, and this function of CoaSt6 can append ADP-ribose to itself and p100 (PMID:17478423)
• loss of PARP14 protein is a feature of gastric and colorectal cancers with high microsatellite instability and these alterations might contribute to development of cancers with high microsatellite instability by deregulating PARP-mediated signaling (PMID:21333322)
• Poly(ADP-ribose) polymerase family member 14 (PARP14) is a novel effector of the JNK2-dependent pro-survival signal in multiple myeloma. (PMID:23045269)
• PARP14 has a significant role in the development of allergic inflammation, and targeting PARP14, or even PARP activity in general, might be an effective therapy for allergic diseases including eosinophilic esophagitis. (PMID:24238647)
• The present study further suggests that the combined targeted inhibition of STAT1, ARTD8, ARTD9 and/or DTX3L could increase the efficacy of chemotherapy or radiation treatment in prostate and other high-risk tumor types with an increased STAT1 signaling. (PMID:24886089)
• PARP14 interacts with the DNA replication machinery component PCNA and promotes replication of DNA lesions and common fragile sites. (PMID:25753673)
• The PARP14-JNK1-PKM2 regulatory axis is an important determinant for the Warburg effect in tumour cells and provides a mechanistic link between apoptosis and metabolism. (PMID:26258887)
• PARP9 and PARP14 regulate macrophage activation in macrophage cell lines treated with either IFNgamma or IL-4; PARP14 silencing induces pro-inflammatory genes and STAT1 phosphorylation in M(IFNgamma) cells, whereas it suppresses anti-inflammatory gene expression and STAT6 phosphorylation in M(IL-4) cells (PMID:27796300)
• murine Artd8 macrodomain constructs can serve as a tool to evaluate intracellular ARTD10 auto-modification levels using the described methods, while the human ARTD8 macrodomains are less suited because of ADPr-independent binding to ARTD10. Protocols for co-immunoprecipitation and co-localization experiments are described in detail. (PMID:30097860)
• This study summarizes specific molecular pathways, including those involving poly(ADP-ribose) polymerase family member 14 (PARP14) and poly(ADP-ribose) polymerase family member 9 (PARP9) at the intersection of interferon gamma (IFN-gamma) and ADP-ribosylation signaling pathways. (PMID:30848916)
• PARP14 could promote Pancreatic cancer cell proliferation, antiapoptosis, and gemcitabine resistance via NF-kappaB signaling pathway, highlighting its potential role as a therapeutic target for Pancreatic cancer. (PMID:30968979)
• Genome-wide CRISPR synthetic lethality screen identifies a role for the ADP-ribosyltransferase PARP14 in DNA replication dynamics controlled by ATR. (PMID:32542389)
• The potential association between PARP14 and SARS-CoV-2 infection (COVID-19). (PMID:33467912)
• PARP14 regulates cyclin D1 expression to promote cell-cycle progression. (PMID:34158578)
• PARP14 regulates EP4 receptor expression in human colon cancer HCA-7 cells. (PMID:35914351)
• PARP14 promotes the growth and glycolysis of acute myeloid leukemia cells by regulating HIF-1alpha expression. (PMID:35944879)
• NMR study of human macroPARPs domains: (1)H, (15)N and (13)C resonance assignment of hPARP14 macro domain 2 in the free and the ADPr bound state. (PMID:36107366)
• PARP14 correlates with GBM proliferation and poor prognosis by elevating expression of SAMD/SAMD9L. (PMID:37612499)
• Exploration of glycosyltransferases mutation status in cervical cancer reveals PARP14 as a potential prognostic marker. (PMID:37650946)
• Targeting PARP14 with lomitapide suppresses drug resistance through the activation of DRP1-induced mitophagy in multiple myeloma. (PMID:38467180)
• PARP14 Contributes to the Development of the Tumor-Associated Macrophage Phenotype. (PMID:38612413)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	parp14rs1	ENSDARG00000040445
mus_musculus	Parp14	ENSMUSG00000034422
rattus_norvegicus	Parp14	ENSRNOG00000023334

Paralogs (8): PARP12 (ENSG00000059378), ZC3HAV1 (ENSG00000105939), PARP11 (ENSG00000111224), PARP9 (ENSG00000138496), ZC3HAV1L (ENSG00000146858), TIPARP (ENSG00000163659), PARP15 (ENSG00000173200), PARP10 (ENSG00000178685)

Protein

Protein identifiers

Protein mono-ADP-ribosyltransferase PARP14 — Q460N5 (reviewed: Q460N5)

Alternative names: ADP-ribosyltransferase diphtheria toxin-like 8, B aggressive lymphoma protein 2, Poly [ADP-ribose] polymerase 14

All UniProt accessions (4): Q460N5, A0A3B3ITD5, H7C4Y3, H7C5R8

UniProt curated annotations — full annotation on UniProt →

Function. ADP-ribosyltransferase that mediates mono-ADP-ribosylation of glutamate residues on target proteins. In contrast to PARP1 and PARP2, it is not able to mediate poly-ADP-ribosylation. Has been shown to catalyze the mono-ADP-ribosylation of STAT1 at ‘Glu-657’ and ‘Glu-705’, thus decreasing STAT1 phosphorylation which negatively regulates pro-inflammatory cytokine production in macrophages in response to IFNG stimulation. However, the role of ADP-ribosylation in the prevention of STAT1 phosphorylation has been called into question and it has been suggested that the inhibition of phosphorylation may be the result of sumoylation of STAT1 ‘Lys-703’. Mono-ADP-ribosylates STAT6; enhancing STAT6-dependent transcription. In macrophages, positively regulates MRC1 expression in response to IL4 stimulation by promoting STAT6 phosphorylation. Mono-ADP-ribosylates PARP9.

Subunit / interactions. Interacts with STAT6. Interacts with PARP10. Interacts with PARP9 in IFNG-stimulated macrophages; the interaction prevents PARP14-mediated STAT1 and STAT6 ADP-riboslylation.

Subcellular location. Nucleus. Cytoplasm.

Tissue specificity. Expressed in macrophages.

Post-translational modifications. Auto-ADP-ribosylated.

Induction. Up-regulated by IFNG in macrophages. Down-regulated by IL4 in macrophages.

Similarity. Belongs to the ARTD/PARP family.

Isoforms (5)

UniProt ID	Names	Canonical?
Q460N5-6	6	yes
Q460N5-1	1, BAL2B
Q460N5-3	3, BAL2A
Q460N5-4	4
Q460N5-5	5

RefSeq proteins (1): NP_060024* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002589	Macro_dom	Domain
IPR004170	WWE_dom	Domain
IPR012317	Poly(ADP-ribose)pol_cat_dom	Domain
IPR012677	Nucleotide-bd_a/b_plait_sf	Homologous_superfamily
IPR034517	PAR14_RRM2	Domain
IPR037197	WWE_dom_sf	Homologous_superfamily
IPR043472	Macro_dom-like	Homologous_superfamily
IPR052056	Mono-ARTD/PARP	Family
IPR054596	PARP14_WWE	Domain
IPR057043	PARP14_KH_2	Domain
IPR057044	PARP14_KH_1	Domain
IPR057045	PARP14_KH_3	Domain
IPR057046	PARP14_KH_4	Domain
IPR057047	PARP14_KH_5	Domain
IPR057048	PARP14_KH_6	Domain
IPR057049	PARP14_KH_8	Domain
IPR057050	RRM_PARP14_2	Domain
IPR057051	PARP14_RPM_1	Domain

Pfam: PF00644, PF01661, PF22005, PF23084, PF23085, PF23222, PF23245, PF23248, PF23249, PF23251, PF23252, PF23253, PF23254

Enzyme classification (BRENDA):

• EC 2.4.2.30 — NAD+ ADP-ribosyltransferase (BRENDA: 32 organisms, 193 substrates, 306 inhibitors, 42 Km, 24 kcat entries)

Substrate kinetics (BRENDA)

5 substrates with measured Km, best-characterized 5. Km ranges are aggregated across organisms/conditions.

Substrate	Km (mM)	Measurements
NAD+	0.002–0.251	25
(ADP-D-RIBOSYL)N-ACTIN	0.011–0.037	7
(ADP-D-RIBOSYL)N-SOYBEAN-TRYPSIN-INHIBITOR	0.03–0.429	6
(ADP-D-RIBOSYL)N-RHOA PROTEIN	0.017	1
N6-ETHENO-NAD+	0.0225	1

Catalyzed reactions (Rhea), 1 shown:

• L-glutamyl-[protein] + NAD(+) = 5-O-(ADP-D-ribosyl)-L-glutamyl-[protein] + nicotinamide (RHEA:58224)

UniProt features (103 total): strand 37, helix 27, binding site 14, splice variant 6, domain 5, sequence conflict 5, modified residue 3, turn 3, chain 1, mutagenesis site 1, region of interest 1

Structure

Experimental structures (PDB)

47 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
5QHT	X-RAY DIFFRACTION	1.05
5QHU	X-RAY DIFFRACTION	1.05
5QHV	X-RAY DIFFRACTION	1.05
5QI0	X-RAY DIFFRACTION	1.05
5QI1	X-RAY DIFFRACTION	1.05
5QI3	X-RAY DIFFRACTION	1.05
5QI5	X-RAY DIFFRACTION	1.05
5QI7	X-RAY DIFFRACTION	1.05
5QI9	X-RAY DIFFRACTION	1.05
5QI2	X-RAY DIFFRACTION	1.08
5QI8	X-RAY DIFFRACTION	1.09
5QI6	X-RAY DIFFRACTION	1.1
5QHX	X-RAY DIFFRACTION	1.11
5QHW	X-RAY DIFFRACTION	1.12
5QIA	X-RAY DIFFRACTION	1.14
4ABL	X-RAY DIFFRACTION	1.15
5QHZ	X-RAY DIFFRACTION	1.15
5QHY	X-RAY DIFFRACTION	1.17
5QI4	X-RAY DIFFRACTION	1.2
3SMJ	X-RAY DIFFRACTION	1.5
7D2C	X-RAY DIFFRACTION	1.56
4ABK	X-RAY DIFFRACTION	1.6
5O2D	X-RAY DIFFRACTION	1.6
6WE4	X-RAY DIFFRACTION	1.6
4F1L	X-RAY DIFFRACTION	1.9
6WE3	X-RAY DIFFRACTION	1.95
4D86	X-RAY DIFFRACTION	2
7R3L	X-RAY DIFFRACTION	2
5LXP	X-RAY DIFFRACTION	2.07
6FYM	X-RAY DIFFRACTION	2.15

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q460N5-F1	82.00	0.32

Functional residue map

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

Ligand- & substrate-binding residues (14): 961; 1023–1024; 1034; 1046–1049; 1133–1137; 1175–1178; 1235–1236; 1247; 1258; 1332–1336; 1371; 824 …

Post-translational modifications (3): 33, 1403, 1411

Mutagenesis-validated functional residues (1):

Position	Phenotype
1055	abolishes interaction with parp10.

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: 369 (showing top): GOBP_NEGATIVE_REGULATION_OF_PEPTIDYL_TYROSINE_PHOSPHORYLATION, GOBP_REGULATION_OF_PHOSPHORYLATION, GOBP_RESPONSE_TO_INTERLEUKIN_4, GOBP_RESPONSE_TO_PEPTIDE, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GRAESSMANN_RESPONSE_TO_MC_AND_SERUM_DEPRIVATION_UP, GOBP_NEGATIVE_REGULATION_OF_INNATE_IMMUNE_RESPONSE, GOBP_ORGANOPHOSPHATE_METABOLIC_PROCESS, GOBP_CELL_SURFACE_RECEPTOR_SIGNALING_PATHWAY_VIA_JAK_STAT, GOBP_NADPLUS_METABOLIC_PROCESS, GOBP_POSITIVE_REGULATION_OF_PEPTIDYL_TYROSINE_PHOSPHORYLATION, GOBP_NUCLEOBASE_CONTAINING_SMALL_MOLECULE_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_RESPONSE_TO_BIOTIC_STIMULUS, GOBP_REGULATION_OF_IMMUNE_RESPONSE, GOBP_DEFENSE_RESPONSE_TO_OTHER_ORGANISM

GO Biological Process (12): negative regulation of gene expression (GO:0010629), NAD+ catabolic process (GO:0019677), positive regulation of tyrosine phosphorylation of STAT protein (GO:0042531), negative regulation of tyrosine phosphorylation of STAT protein (GO:0042532), innate immune response (GO:0045087), negative regulation of type II interferon-mediated signaling pathway (GO:0060336), protein poly-ADP-ribosylation (GO:0070212), positive regulation of interleukin-4-mediated signaling pathway (GO:1902216), positive regulation of cytokine-mediated signaling pathway (GO:0001961), immune system process (GO:0002376), negative regulation of DNA-templated transcription (GO:0045892), regulation of type II interferon-mediated signaling pathway (GO:0060334)

GO Molecular Function (10): transcription corepressor activity (GO:0003714), NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), nucleotidyltransferase activity (GO:0016779), enzyme binding (GO:0019899), NAD+ binding (GO:0070403), NAD+-protein-glutamate ADP-ribosyltransferase activity (GO:0140807), NAD+-protein mono-ADP-ribosyltransferase activity (GO:1990404), protein binding (GO:0005515), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757)

GO Cellular Component (5): nucleus (GO:0005634), cytoplasm (GO:0005737), cytosol (GO:0005829), plasma membrane (GO:0005886), membrane (GO:0016020)

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
cellular anatomical structure	3
tyrosine phosphorylation of STAT protein	2
regulation of tyrosine phosphorylation of STAT protein	2
type II interferon-mediated signaling pathway	2
regulation of cytokine-mediated signaling pathway	2
pentosyltransferase activity	2
gene expression	1
regulation of gene expression	1
negative regulation of macromolecule biosynthetic process	1
purine nucleotide catabolic process	1
pyridine nucleotide catabolic process	1
NAD+ metabolic process	1
positive regulation of peptidyl-tyrosine phosphorylation	1
negative regulation of receptor signaling pathway via JAK-STAT	1
negative regulation of peptidyl-tyrosine phosphorylation	1
immune response	1
defense response to symbiont	1
negative regulation of cytokine-mediated signaling pathway	1
negative regulation of response to type II interferon	1
regulation of type II interferon-mediated signaling pathway	1
post-translational protein modification	1
positive regulation of cytokine-mediated signaling pathway	1
interleukin-4-mediated signaling pathway	1
regulation of interleukin-4-mediated signaling pathway	1
positive regulation of signal transduction	1
cytokine-mediated signaling pathway	1
positive regulation of response to cytokine stimulus	1
biological_process	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
negative regulation of RNA biosynthetic process	1
regulation of response to type II interferon	1
transcription coregulator activity	1
negative regulation of DNA-templated transcription	1
transferase activity, transferring phosphorus-containing groups	1
protein binding	1
anion binding	1
NAD binding	1
NAD+-protein mono-ADP-ribosyltransferase activity	1
catalytic activity, acting on a protein	1

Protein interactions and networks

STRING

972 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARP14	DTX3L	Q8TDB6	898
PARP14	PARP1	P09874	787
PARP14	PARP16	Q8N5Y8	720
PARP14	PARP3	Q9Y6F1	686
PARP14	PARP6	Q2NL67	673
PARP14	PARP2	Q9UGN5	656
PARP14	PARP4	Q9UKK3	649
PARP14	PARP10	Q53GL7	616
PARP14	PARG	Q86W56	612
PARP14	PARP8	Q8N3A8	594
PARP14	MAPK8	P45983	593
PARP14	PARP9	Q8IXQ6	589
PARP14	STAT6	P42226	582
PARP14	IFI44	Q8TCB0	582
PARP14	ISG15	P05161	576

IntAct

28 interactions, top by confidence:

A	B	Type	Score
FAM174A	BLTP3B	psi-mi:“MI:0914”(association)	0.530
DCAF8	DCAF8L1	psi-mi:“MI:0914”(association)	0.530
ZNRD2	MYO9A	psi-mi:“MI:0914”(association)	0.530
LPAR1	TMEM223	psi-mi:“MI:0914”(association)	0.530
TGOLN2	DENND11	psi-mi:“MI:0914”(association)	0.530
ZNRD2	CCDC85C	psi-mi:“MI:0914”(association)	0.530
PARP14	STAT6	psi-mi:“MI:0915”(physical association)	0.400
PARP14	MAF1b1	psi-mi:“MI:0915”(physical association)	0.370
MKI67	ARHGAP10	psi-mi:“MI:0914”(association)	0.350
CUL2	ANXA2P2	psi-mi:“MI:0914”(association)	0.350
PA	ESYT2	psi-mi:“MI:0914”(association)	0.350
EEF1AKMT3	SMCHD1	psi-mi:“MI:0914”(association)	0.350
PNPLA1	METTL15	psi-mi:“MI:0914”(association)	0.350
KDM4B	AP3B1	psi-mi:“MI:0914”(association)	0.350
TYROBP	KCNN4	psi-mi:“MI:0914”(association)	0.350
RNF166	SNX3	psi-mi:“MI:0914”(association)	0.350
FYCO1	HAUS5	psi-mi:“MI:0914”(association)	0.350
AURKB	VWA8	psi-mi:“MI:0914”(association)	0.350
CAMK2D	PPM1D	psi-mi:“MI:0914”(association)	0.350
CD80	RIMOC1	psi-mi:“MI:0914”(association)	0.350
CIAO2A	MAP2K7	psi-mi:“MI:0914”(association)	0.350
FAM20B	PLEKHG3	psi-mi:“MI:0914”(association)	0.350
GSDME	DDX39A	psi-mi:“MI:0914”(association)	0.350
HPN	DDX39A	psi-mi:“MI:0914”(association)	0.350
PPT1	CLGN	psi-mi:“MI:0914”(association)	0.350
TYROBP	SCAMP2	psi-mi:“MI:0914”(association)	0.350
SLC47A1	PLOD2	psi-mi:“MI:0914”(association)	0.350

BioGRID (48): PARP14 (Affinity Capture-MS), PARP10 (Reconstituted Complex), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Proximity Label-MS), PARP14 (Affinity Capture-RNA), PARP14 (Affinity Capture-MS), PARP14 (Proximity Label-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS), PARP14 (Affinity Capture-MS)

ESM2 similar proteins: A0A140LI67, A0JM98, A1L1H3, A6NAF9, A9CPT4, B5MCY1, D2H0H6, D2H3M0, D4A7V9, E1C3S7, E2QTD3, E2RDV1, E7FDW8, F1R237, M0R4F8, O60522, P0C5Y8, P61407, Q0P5I2, Q1L981, Q2EMV9, Q460N5, Q4KMD7, Q4QQS0, Q4R3G4, Q58EK5, Q5BIW4, Q5M7P8, Q5R810, Q5VZ19, Q68DX3, Q6NU04, Q6NZP1, Q6PCM1, Q6TXD4, Q6XZF7, Q80YY7, Q8CAS9, Q8K1H1, Q8NAT2

Diamond homologs: A0A166ACJ5, A0A559KX76, A1Z1Q3, A4W960, A7MG20, A7T167, A8AI35, B4T2X8, B5F961, B5RBF3, B5XXK9, B7LT90, C9Y0V8, D2TT52, D3RKJ0, D5CE05, E1PL40, E1SDF1, O28751, O59182, P0A8D6, P0A8D7, P0A8D8, P0DC28, P0DC29, P0DN70, P27282, P36327, P36328, P67341, P67342, P67343, P67344, P9WK28, P9WK29, Q0T5Z6, Q292F9, Q2EMV9, Q2KHU5, Q2KIX2

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	168
Likely benign	24
Benign	6

Top pathogenic / likely-pathogenic (0)

SpliceAI

3163 predictions. Top by Δscore:

Variant	Effect	Δscore
3:122681067:G:GT	donor_gain	1.0000
3:122685173:T:A	acceptor_gain	1.0000
3:122687126:T:G	donor_gain	1.0000
3:122688246:G:GT	donor_gain	1.0000
3:122692293:A:AG	acceptor_gain	1.0000
3:122692294:A:G	acceptor_gain	1.0000
3:122695416:T:TA	acceptor_gain	1.0000
3:122695417:G:A	acceptor_gain	1.0000
3:122695424:A:AC	acceptor_loss	1.0000
3:122695424:A:AG	acceptor_gain	1.0000
3:122695425:G:GG	acceptor_gain	1.0000
3:122695425:GAT:G	acceptor_gain	1.0000
3:122695425:GATA:G	acceptor_gain	1.0000
3:122699388:A:G	acceptor_gain	1.0000
3:122703740:A:G	acceptor_gain	1.0000
3:122708309:C:G	donor_gain	1.0000
3:122713419:TTCA:T	acceptor_loss	1.0000
3:122713420:TCAG:T	acceptor_loss	1.0000
3:122713421:CAG:C	acceptor_loss	1.0000
3:122713422:A:AG	acceptor_gain	1.0000
3:122713423:G:GG	acceptor_gain	1.0000
3:122713534:ATT:A	donor_gain	1.0000
3:122713570:GCAG:G	donor_gain	1.0000
3:122713571:CAGG:C	donor_loss	1.0000
3:122713572:AG:A	donor_loss	1.0000
3:122713573:GGTAC:G	donor_loss	1.0000
3:122713574:G:GA	donor_loss	1.0000
3:122713575:T:G	donor_loss	1.0000
3:122718068:CAG:C	acceptor_loss	1.0000
3:122718069:A:AG	acceptor_gain	1.0000

AlphaMissense

11929 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:122718760:T:A	W1537R	0.994
3:122718760:T:C	W1537R	0.994
3:122728320:G:A	G1710E	0.992
3:122713542:T:A	N1246K	0.991
3:122713542:T:G	N1246K	0.991
3:122728325:G:A	G1712R	0.991
3:122728325:G:C	G1712R	0.991
3:122727960:T:C	F1697S	0.990
3:122714412:T:C	L1328P	0.989
3:122718118:G:C	A1350P	0.989
3:122728334:T:C	F1715L	0.989
3:122728336:T:A	F1715L	0.989
3:122728336:T:G	F1715L	0.989
3:122680963:T:C	L27S	0.988
3:122728320:G:T	G1710V	0.988
3:122699701:T:A	W383R	0.987
3:122699701:T:C	W383R	0.987
3:122701336:T:C	F928L	0.987
3:122701338:T:A	F928L	0.987
3:122701338:T:G	F928L	0.987
3:122727911:T:C	F1681L	0.987
3:122727913:C:A	F1681L	0.987
3:122727913:C:G	F1681L	0.987
3:122727914:C:G	H1682D	0.987
3:122680926:T:A	W15R	0.986
3:122680926:T:C	W15R	0.986
3:122728547:T:C	F1786L	0.986
3:122728549:T:A	F1786L	0.986
3:122728549:T:G	F1786L	0.986
3:122704623:T:C	F1139L	0.985

dbSNP variants (sampled 300 via entrez): RS1000007837 (3:122703196 C>T), RS1000069467 (3:122693558 G>A,C), RS1000314909 (3:122713167 C>T), RS1000491395 (3:122719968 C>A,T), RS1000517181 (3:122714815 C>G), RS1000563751 (3:122701809 A>G), RS1000624620 (3:122712787 A>T), RS1000845449 (3:122701030 G>A), RS1000936115 (3:122693331 A>C,G), RS1000942843 (3:122681558 C>A,T), RS1001003458 (3:122707354 C>T), RS1001056158 (3:122715148 G>A), RS1001098167 (3:122707711 T>C), RS1001127446 (3:122728138 A>G), RS1001259658 (3:122681796 C>T)

Disease associations

OMIM: gene MIM:610028 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2176777 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 32,147 (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
CHEMBL1094636	NIRAPARIB	4	6,433
CHEMBL1173055	RUCAPARIB	4	7,009
CHEMBL521686	OLAPARIB	4	13,038
CHEMBL506871	VELIPARIB	3	5,421
CHEMBL5095043	ATAMPARIB	1	246

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs10433340	PARP14		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Mono-ADP-ribosylating PARPs

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
RBN012759	Inhibition	8.52	pIC50

Binding affinities (BindingDB)

42 measured of 200 human assays (200 total across all organisms); most potent 42 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
8-methyl-2-(pyrrolidin-3-ylsulfanylmethyl)-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methyl-2-[(1-methylpyrrolidin-3-yl)sulfanylmethyl]-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[(4-hydroxycyclohexyl)sulfanylmethyl]-8-methyl-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[(4-methoxycyclohexyl)sulfanylmethyl]-8-methyl-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methylidene-2-[(1-methylpiperidin-3-yl)sulfanylmethyl]quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-fluoro-2-[(4-hydroxycyclohexyl)sulfanylmethyl]-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[(3-hydroxycyclobutyl)sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methylidene-2-(piperidin-3-ylsulfanylmethyl)quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[(4-aminocyclohexyl)sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[(3-aminocyclobutyl)sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[(1S,4S)-4-aminocycloheptyl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methyl-2-[(4-methylcyclohexyl)sulfanylmethyl]-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[4-(aminomethyl)cyclohexyl]sulfanylmethyl]-8-methyl-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[4-[(dimethylamino)methyl]cyclohexyl]sulfanylmethyl]-8-methyl-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[(1R,3S)-3-(hydroxymethyl)cyclohexyl]sulfanylmethyl]-8-methyl-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-anilino-2-[(4-hydroxycyclohexyl)sulfanylmethyl]-2,3,4a,5,6,7,8,8a-octahydro-1H-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-anilino-2-[[4-(hydroxymethyl)cyclohexyl]sulfanylmethyl]-2,3,4a,5,6,7,8,8a-octahydro-1H-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[4-(hydroxymethyl)cyclohexyl]sulfanylmethyl]-7-(pyridin-3-ylamino)-2,3,4a,5,6,7,8,8a-octahydro-1H-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-[(1-benzylpiperidin-3-yl)amino]-2-(oxan-4-ylsulfanylmethyl)-2,3,4a,5,6,7,8,8a-octahydro-1H-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-(oxan-4-ylsulfanylmethyl)-7-pyrrolidin-3-ylimino-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-(1-acetylpyrrolidin-3-yl)imino-2-(oxan-4-ylsulfanylmethyl)-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[1-[(2S)-2,3-dihydroxypropyl]piperidin-4-yl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[1-[(2R)-2,3-dihydroxypropyl]piperidin-4-yl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methylidene-2-[[1-[[(2S)-pyrrolidin-2-yl]methyl]piperidin-4-yl]sulfanylmethyl]quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
N-[[4-[(8-methylidene-4-oxoquinazolin-2-yl)methylsulfanyl]cyclohexyl]methyl]acetamide	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[(1R,3S)-3-(2-aminoethyl)cyclopentyl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[3-(aminomethyl)cyclopentyl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
8-methylidene-2-(oxepan-4-ylsulfanylmethyl)quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
4-[(8-methyl-4-oxo-4aH-quinazolin-2-yl)methylsulfanyl]cyclohexane-1-carboxamide	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
4-[(7-cyclopentylimino-5-fluoro-4-oxo-3,4a-dihydroquinazolin-2-yl)methylsulfanyl]cyclohexane-1-carboxylic acid	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[(3S,6S)-6-(hydroxymethyl)oxan-3-yl]sulfanylmethyl]-8-methylidenequinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-cyclopentylimino-5-fluoro-2-[[(2S,4S)-2-(trifluoromethyl)piperidin-4-yl]sulfanylmethyl]-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-cyclopentylimino-5-fluoro-2-[[(2R,4S)-2-(trifluoromethyl)piperidin-4-yl]sulfanylmethyl]-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
5-fluoro-7-(4-morpholin-4-ylcyclohexyl)imino-2-(oxan-4-ylsulfanylmethyl)-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[(3R,6R)-6-(aminomethyl)oxan-3-yl]sulfanylmethyl]-7-cyclopentylimino-5-fluoro-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
7-(cyclopropylmethoxy)-5-fluoro-2-[[(3R,4R)-3-fluoropiperidin-4-yl]sulfanylmethyl]-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
4-[[7-(cyclobutylmethoxy)-5-fluoro-4-oxo-4aH-quinazolin-2-yl]methylsulfanyl]cyclohexane-1-carboxamide	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
2-[[4-(aminomethyl)-4-fluorocyclohexyl]sulfanylmethyl]-7-(cyclobutylmethoxy)-5-fluoro-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
5-fluoro-7-[[(3R,4R)-3-fluoropiperidin-4-yl]methoxy]-2-(oxan-4-ylsulfanylmethyl)-4aH-quinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors
5,6-difluoro-7-[[(3S,4R)-3-fluoro-1-methylpiperidin-4-yl]methylimino]-2-(oxan-4-ylsulfanylmethyl)-3,4a-dihydroquinazolin-4-one	IC50	5500 nM	US-10562891: Quinazolinones as PARP14 inhibitors

ChEMBL bioactivities

409 potent at pChembl≥5 of 436 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.44	IC50	0.36	nM	CHEMBL6167618
9.38	IC50	0.42	nM	CHEMBL6143555
9.33	IC50	0.47	nM	CHEMBL6167737
9.12	IC50	0.75	nM	CHEMBL6171127
9.12	IC50	0.75	nM	CHEMBL6174540
9.02	IC50	0.95	nM	CHEMBL6174890
8.98	IC50	1.04	nM	CHEMBL6175947
8.77	IC50	1.69	nM	CHEMBL5880861
8.66	IC50	2.21	nM	CHEMBL6174111
8.64	IC50	2.3	nM	CHEMBL6171562
8.62	IC50	2.4	nM	CHEMBL6174864
8.52	IC50	3	nM	CHEMBL5179405
8.52	IC50	3	nM	CHEMBL6174131
8.40	IC50	4	nM	CHEMBL5880861
8.30	IC50	4.99	nM	CHEMBL6174829
8.26	IC50	5.52	nM	CHEMBL6170737
8.04	IC50	9.18	nM	CHEMBL6174889
8.00	IC50	10	nM	CHEMBL5180081
7.72	IC50	19	nM	CHEMBL5171039
7.69	IC50	20.59	nM	CHEMBL6175005
7.54	IC50	28.5	nM	CHEMBL6172711
7.34	IC50	45.15	nM	CHEMBL6166509
7.26	IC50	54.27	nM	CHEMBL6151548
7.12	IC50	76	nM	CHEMBL5178541
6.88	IC50	132.4	nM	CHEMBL6159732
6.80	IC50	160	nM	CHEMBL4068366
6.60	IC50	251.2	nM	CHEMBL6170252
6.57	IC50	270	nM	CHEMBL4074448
6.56	IC50	275.4	nM	CHEMBL4074448
6.52	IC50	300	nM	CHEMBL5180051
6.52	IC50	300	nM	CHEMBL5404785
6.52	IC50	302	nM	CHEMBL5404785
6.51	IC50	310	nM	CHEMBL5196898
6.43	IC50	370	nM	CHEMBL4104938
6.43	IC50	371.5	nM	CHEMBL4104938
6.39	IC50	410	nM	CHEMBL4079213
6.39	IC50	407.4	nM	CHEMBL4084742
6.39	IC50	407.4	nM	CHEMBL4079213
6.35	IC50	450	nM	CHEMBL4104503
6.35	IC50	446.7	nM	CHEMBL4104503
6.31	IC50	490	nM	CHEMBL5205408
6.31	IC50	490	nM	CHEMBL6170265
6.26	Kd	550	nM	CHEMBL4226482
6.24	IC50	580	nM	CHEMBL5199759
6.21	IC50	616.6	nM	CHEMBL4068366
6.21	IC50	610	nM	CHEMBL5191979
6.20	IC50	630	nM	CHEMBL4293771
6.19	IC50	650	nM	CHEMBL4080281
6.19	IC50	650	nM	CHEMBL5431108
6.19	IC50	645.6	nM	CHEMBL5431108

PubChem BioAssay actives

171 with measured affinity, of 393 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
7-(cyclopropylmethoxy)-5-fluoro-2-[(4-hydroxycyclohexyl)sulfanylmethyl]-3H-quinazolin-4-one	1868266: Displacement of a biotinylated small molecule probe from human PARP14 catalytic domain incubated for 30 mins by TR-FRET assay	ic50	0.0030	uM
2-[4-[[7-(cyclopentylamino)-5-fluoro-4-oxo-3H-quinazolin-2-yl]methylsulfanyl]piperidin-1-yl]-N-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexyl]acetamide	1869176: Inhibition of PARP14 (unknown origin)	ic50	0.0100	uM
7-(cyclopentylamino)-5-fluoro-2-(piperidin-4-ylsulfanylmethyl)-3H-quinazolin-4-one	1869176: Inhibition of PARP14 (unknown origin)	ic50	0.0190	uM
2-[(1-methylpiperidin-4-yl)methylamino]-5,6,7,8-tetrahydro-3H-[1]benzothiolo[2,3-d]pyrimidin-4-one	1869176: Inhibition of PARP14 (unknown origin)	ic50	0.0760	uM
3-[[(Z)-4-[4-(4-chlorophenyl)piperazin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.1600	uM
3-[[(Z)-4-[4-(4-fluorophenyl)piperidin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.2700	uM
2-[(4-hydroxycyclohexyl)sulfanylmethyl]-8-methyl-3H-quinazolin-4-one	1869177: Inhibition of PARP14 (unknown origin) by TR-FRET assay	ic50	0.3000	uM
5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965931: Inhibition of N-terminal MBP tagged/C-terminal PARP14 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.3000	uM
2-(pyridin-4-ylmethylamino)-5,6,7,8-tetrahydro-3H-[1]benzothiolo[2,3-d]pyrimidin-4-one	1869175: Displacement of [3H]NAD+ from GST-tagged PARP14 (unknown origin) incubated for 210 mins by radiometric assay	ic50	0.3100	uM
tert-butyl 4-[(Z)-4-(3-carbamoylanilino)-4-oxobut-2-enoyl]piperazine-1-carboxylate	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.3700	uM
ethyl 2-[1-[(Z)-4-(3-carbamoylanilino)-4-oxobut-2-enoyl]piperidin-4-yl]acetate	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.4074	uM
3-[[(Z)-4-[4-(2-fluorophenyl)piperazin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.4074	uM
3-[[(Z)-4-(4-benzylpiperidin-1-yl)-4-oxobut-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.4467	uM
3-[2-[4-[2-[[4-(3-carbamoylanilino)-4-oxobutanoyl]amino]ethyl]triazol-1-yl]ethylsulfamoyl]benzoic acid	1869159: Inhibition of PARP14 (unknown origin) expressed in bacterial expression system using histone substrate incubated for 60 mins by chemiluminescence assay	ic50	0.4900	uM
N-[2-(9H-carbazol-1-yl)phenyl]-1-(3-cyanophenyl)methanesulfonamide	1391151: Binding affinity to PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system by ITC assay	kd	0.5500	uM
6-[3-(4-benzhydryloxypiperidin-1-yl)propoxy]-[1,2,4]triazolo[4,3-b]pyridazine	1869175: Displacement of [3H]NAD+ from GST-tagged PARP14 (unknown origin) incubated for 210 mins by radiometric assay	ic50	0.5800	uM
N-[4-(4-benzhydryloxypiperidin-1-yl)butyl]-[1,2,4]triazolo[4,3-b]pyridazin-6-amine	1869176: Inhibition of PARP14 (unknown origin)	ic50	0.6100	uM
4-[(3-bromophenyl)methoxy]benzamide	1833807: Inhibition of PARP14 (unknown origin) using NAD+ as substrate incubated for 18 hrs by fluorescence based assay	ic50	0.6300	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965931: Inhibition of N-terminal MBP tagged/C-terminal PARP14 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.6456	uM
3-[[(Z)-4-oxo-4-[4-(2-phenylethyl)piperidin-1-yl]but-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.6500	uM
3-[[(Z)-4-oxo-4-(3-phenylpiperidin-1-yl)but-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.6900	uM
4-[3-[4-(3,4-difluorophenyl)piperazine-1-carbonyl]phenoxy]benzamide	1496064: Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.6918	uM
3-[[(Z)-4-[4-(4-fluorophenyl)piperazin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.7000	uM
N-[2-(9H-carbazol-1-yl)phenyl]acetamide	1869198: Inhibition of PARP14 MD2 (unknown origin)	ic50	0.7100	uM
N’-(3-carbamoylphenyl)-N-[[1-(1-phenylethyl)triazol-4-yl]methyl]pentanediamide	1869159: Inhibition of PARP14 (unknown origin) expressed in bacterial expression system using histone substrate incubated for 60 mins by chemiluminescence assay	ic50	0.7600	uM
N’-(3-carbamoylphenyl)-N-[(5S)-5-[(2-methyl-5-nitrophenyl)sulfonylamino]-6-oxo-6-(propan-2-ylamino)hexyl]butanediamide	1869159: Inhibition of PARP14 (unknown origin) expressed in bacterial expression system using histone substrate incubated for 60 mins by chemiluminescence assay	ic50	0.7700	uM
4-[3-[4-(4-fluorophenyl)piperazine-1-carbonyl]phenoxy]benzamide	1496064: Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.7762	uM
3-[[(Z)-4-oxo-4-(4-phenylpiperazin-1-yl)but-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.8912	uM
N-[2-(9H-carbazol-1-yl)phenyl]methanesulfonamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	0.9000	uM
N-[2-(9H-carbazol-1-yl)phenyl]butanamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	0.9000	uM
4-[(8-methyl-4-oxo-7-prop-1-ynyl-3H-quinazolin-2-yl)methylsulfanyl]benzoic acid	1869176: Inhibition of PARP14 (unknown origin)	ic50	0.9170	uM
N-[2-(9H-carbazol-1-yl)phenyl]propanamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.0000	uM
N-[2-(9H-carbazol-1-yl)phenyl]-2-(6-methyl-3-pyridinyl)acetamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.0000	uM
8-methyl-2-(pyridin-4-ylsulfanylmethyl)-3H-quinazolin-4-one	1869177: Inhibition of PARP14 (unknown origin) by TR-FRET assay	ic50	1.0000	uM
3-[[(Z)-4-oxo-4-(3-phenoxypiperidin-1-yl)but-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	1.0233	uM
4-[3-(4-phenylpiperazine-1-carbonyl)phenoxy]benzamide	1496064: Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	1.0471	uM
3-[[(Z)-4-oxo-4-(2-phenylpiperidin-1-yl)but-2-enoyl]amino]benzamide	1467135: Inhibition of recombinant human His6-tagged PARP14 catalytic/WWE domain (1459 to 1801 residues) expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	1.0715	uM
4-[3-[4-(2-fluorophenyl)piperazine-1-carbonyl]phenoxy]benzamide	1496064: Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	1.0715	uM
N-[2-(6,7,8,9-tetrahydro-5H-carbazol-1-yl)phenyl]acetamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.1000	uM
N-[2-(9H-carbazol-1-yl)-5-methylphenyl]methanesulfonamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.1000	uM
N-[2-(9H-carbazol-1-yl)phenyl]-2-pyridin-3-ylacetamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.1000	uM
N-[2-(9H-carbazol-1-yl)phenyl]-2,2,2-trifluoroacetamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.1000	uM
N-[2-(9H-carbazol-1-yl)phenyl]-1-(5-cyano-2-fluorophenyl)methanesulfonamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.2000	uM
N-[2-(9H-carbazol-1-yl)phenyl]cyclopropanecarboxamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.2000	uM
N-[2-(9H-carbazol-1-yl)phenyl]ethanesulfonamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.2000	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965917: Inhibition of N-terminal MBP tagged/C-terminal PARP14 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	1.2000	uM
4-[3-[4-(4-fluorophenyl)-4-hydroxypiperidine-1-carbonyl]phenoxy]benzamide	1496064: Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	1.2882	uM
8-methyl-2-(pyrimidin-2-ylsulfanylmethyl)-3H-quinazolin-4-one	1869176: Inhibition of PARP14 (unknown origin)	ic50	1.3000	uM
4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]-N-[4-[(4-methoxyphenyl)carbamoyl]phenyl]piperazine-1-carboxamide	1868365: Inhibition of PARP-14 (unknown origin)	ic50	1.3690	uM
N-[2-(7,8-dichloro-9H-carbazol-1-yl)phenyl]acetamide	1391152: Displacement of ARTK(Bio)QTARK(Aoa-RADP)S from His6-tagged PARP14 MD2 (A994 to N1191 residues) (unknown origin) expressed in bacterial expression system after 30 mins by AlphaScreen assay	ic50	1.4000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation, increases expression	4
bisphenol A	decreases methylation, increases expression, affects cotreatment, increases methylation, decreases expression	3
Valproic Acid	affects cotreatment, increases expression, affects expression, decreases expression	3
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression, increases expression	2
(+)-JQ1 compound	decreases expression	2
Acetaminophen	decreases expression	2
Air Pollutants	increases abundance, increases expression, decreases expression	2
Estradiol	decreases expression, increases expression, affects cotreatment	2
Nickel	increases expression	2
Plant Extracts	affects cotreatment, increases expression	2
Tetrachlorodibenzodioxin	increases expression	2
Tretinoin	increases expression	2
SBI-797812	increases activity	1
2,4,6-tribromophenol	decreases expression	1
alpha phellandrene	increases expression	1
decabromobiphenyl ether	increases expression	1
trichostatin A	increases expression	1
sodium arsenite	increases expression	1
tetrabromobisphenol A	decreases expression	1
benzo(e)pyrene	increases methylation	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression	1
perfluorooctane sulfonic acid	decreases expression	1
N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride	affects binding	1
ICG 001	increases expression	1
abrine	decreases expression	1
pentabrominated diphenyl ether 100	decreases expression	1
hexabrominated diphenyl ether 153	decreases expression	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Temozolomide	increases expression	1

ChEMBL screening assays

71 unique, capped per target: 70 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2187439	Binding	Binding affinity at human recombinant ARTD8 expressed in Escherichia coli BL21 (DE3) R3 pRARE cells by isothermal titration calorimetry	Discovery of ligands for ADP-ribosyltransferases via docking-based virtual screening. — J Med Chem
CHEMBL5723148	Functional	Affinity Biochemical interaction: (inhibition of histone ADP-ribosylation, detected using chemiluminescence assay kit) EUB0002249a PARP14	Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1GW	Abcam A-549 PARP14 KO 2	Cancer cell line	Male
CVCL_B2PE	Abcam A-549 PARP14 KO 1	Cancer cell line	Male

Clinical trials (associated diseases)

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