PARP10
gene geneOn this page
Also known as FLJ14464ARTD10
Summary
PARP10 (poly(ADP-ribose) polymerase family member 10, HGNC:25895) is a protein-coding gene on chromosome 8q24.3, encoding Protein mono-ADP-ribosyltransferase PARP10 (Q53GL7). ADP-ribosyltransferase that mediates mono-ADP-ribosylation of glutamate and aspartate residues on target proteins.
Poly(ADP-ribose) polymerases (PARPs), such as PARP10, regulate gene transcription by altering chromatin organization by adding ADP-ribose to histones. PARPs can also function as transcriptional cofactors (Yu et al., 2005 [PubMed 15674325]).
Source: NCBI Gene 84875 — RefSeq curated summary.
At a glance
- GWAS associations: 8
- Clinical variants (ClinVar): 219 total — 1 likely-pathogenic
- Druggable target: yes — 6 molecules with ChEMBL bioactivity
- MANE Select transcript:
NM_032789
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:25895 |
| Approved symbol | PARP10 |
| Name | poly(ADP-ribose) polymerase family member 10 |
| Location | 8q24.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | FLJ14464, ARTD10 |
| Ensembl gene | ENSG00000178685 |
| Ensembl biotype | protein_coding |
| OMIM | 609564 |
| Entrez | 84875 |
Gene structure
Transcript identifiers
Ensembl transcripts: 34 — 26 protein_coding, 4 retained_intron, 3 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay
ENST00000313028, ENST00000313059, ENST00000524918, ENST00000525486, ENST00000525773, ENST00000525879, ENST00000526007, ENST00000526985, ENST00000527262, ENST00000528136, ENST00000528580, ENST00000528625, ENST00000528914, ENST00000528963, ENST00000529311, ENST00000529842, ENST00000530478, ENST00000531537, ENST00000531707, ENST00000532311, ENST00000532660, ENST00000533665, ENST00000534737, ENST00000857398, ENST00000857399, ENST00000857400, ENST00000857401, ENST00000914214, ENST00000966741, ENST00000966742, ENST00000966743, ENST00000966744, ENST00000966745, ENST00000966746
RefSeq mRNA: 2 — MANE Select: NM_032789
NM_001317895, NM_032789
CCDS: CCDS34960, CCDS83331
Canonical transcript exons
ENST00000313028 — 11 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001250817 | 143983167 | 143983811 |
| ENSE00001250825 | 143984008 | 143984104 |
| ENSE00001306487 | 143986055 | 143986233 |
| ENSE00001309960 | 143984544 | 143985328 |
| ENSE00002140641 | 143977158 | 143977830 |
| ENSE00003460094 | 143986358 | 143986460 |
| ENSE00003467358 | 143984210 | 143984431 |
| ENSE00003526489 | 143982932 | 143983065 |
| ENSE00003528592 | 143985412 | 143985648 |
| ENSE00003529204 | 143977907 | 143978081 |
| ENSE00003565027 | 143985721 | 143985975 |
Expression profiles
Bgee: expression breadth ubiquitous, 243 present calls, max score 97.53.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 15.3317 / max 229.1574, expressed in 1630 samples.
FANTOM5 promoters (7 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 95596 | 9.8034 | 1492 |
| 95595 | 4.5695 | 1310 |
| 95598 | 0.4404 | 225 |
| 95600 | 0.2472 | 147 |
| 95597 | 0.1510 | 52 |
| 95601 | 0.0789 | 40 |
| 95599 | 0.0412 | 15 |
Top tissues by expression
252 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| granulocyte | CL:0000094 | 97.53 | gold quality |
| pancreatic ductal cell | CL:0002079 | 97.46 | gold quality |
| right uterine tube | UBERON:0001302 | 97.18 | gold quality |
| spleen | UBERON:0002106 | 95.61 | gold quality |
| vermiform appendix | UBERON:0001154 | 95.45 | gold quality |
| lymph node | UBERON:0000029 | 95.22 | gold quality |
| right testis | UBERON:0004534 | 95.01 | gold quality |
| tendon of biceps brachii | UBERON:0008188 | 94.75 | gold quality |
| left testis | UBERON:0004533 | 94.73 | gold quality |
| right lobe of liver | UBERON:0001114 | 94.53 | gold quality |
| right adrenal gland | UBERON:0001233 | 94.32 | gold quality |
| metanephros cortex | UBERON:0010533 | 94.31 | gold quality |
| right adrenal gland cortex | UBERON:0035827 | 94.24 | gold quality |
| monocyte | CL:0000576 | 93.79 | gold quality |
| leukocyte | CL:0000738 | 93.58 | gold quality |
| left adrenal gland cortex | UBERON:0035825 | 93.50 | gold quality |
| left adrenal gland | UBERON:0001234 | 93.45 | gold quality |
| small intestine Peyer’s patch | UBERON:0003454 | 93.16 | gold quality |
| blood | UBERON:0000178 | 93.14 | gold quality |
| adrenal cortex | UBERON:0001235 | 93.13 | gold quality |
| right ovary | UBERON:0002118 | 92.83 | gold quality |
| mucosa of transverse colon | UBERON:0004991 | 92.79 | gold quality |
| parotid gland | UBERON:0001831 | 92.72 | gold quality |
| upper lobe of left lung | UBERON:0008952 | 92.66 | gold quality |
| left ovary | UBERON:0002119 | 92.62 | gold quality |
| testis | UBERON:0000473 | 92.57 | gold quality |
| bone marrow cell | CL:0002092 | 92.19 | gold quality |
| right lobe of thyroid gland | UBERON:0001119 | 92.13 | gold quality |
| cortex of kidney | UBERON:0001225 | 92.08 | gold quality |
| muscle layer of sigmoid colon | UBERON:0035805 | 92.02 | gold quality |
Single-cell (SCXA)
Detected in 3 experiment(s), a significant marker in 2.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-MTAB-9067 | yes | 11.37 |
| E-MTAB-9801 | yes | 6.00 |
| E-ANND-3 | no | 3.36 |
Regulation
Is transcription factor: yes
Downstream targets (CollecTRI)
2 targets.
| Target | Regulation |
|---|---|
| CXCL8 | Repression |
| NFKBIA | Repression |
miRNA regulators (miRDB)
7 targeting PARP10, 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-661 | 99.09 | 65.94 | 2062 |
| HSA-MIR-6827-5P | 98.46 | 64.88 | 1256 |
| HSA-MIR-93-3P | 98.15 | 66.65 | 1309 |
| HSA-MIR-3192-5P | 96.98 | 65.76 | 1926 |
| HSA-MIR-4485-5P | 95.91 | 59.69 | 198 |
| HSA-MIR-6846-3P | 94.80 | 65.19 | 389 |
| HSA-MIR-6090 | 91.01 | 62.65 | 222 |
Literature-anchored findings (GeneRIF, showing 13)
- novel PARP enzyme involved in the control of cell proliferation (PMID:15674325)
- Overexpression of PARP10 results in loss of cell viability, although down-expression by short hairpin RNA leads to delayed G1 progression and concomitant cell death. (PMID:16455663)
- alternative catalytic mechanism for PARP10 compared to PARP1 in which the acidic target residue of the substrate functionally substitutes for the catalytic glutamate by using substrate-assisted catalysis to transfer ADP-ribose (PMID:18851833)
- study results show that the interaction between PARP10 and NS1 of H5N1 avian influenza virus can change cell cycle, and PARP10 can affect virus replication (PMID:22176891)
- PARP10 binding to PCNA is required for translesion DNA synthesis. (PMID:24695737)
- ARTD10 plays roles in immunity, metabolism ,apoptosis and DNA damage repair. [review] (PMID:24878761)
- PARP10 expression decreased upon fasting, a condition that is characterized by increases in mitochondrial biogenesis. Finally, lower PARP10 expression is associated with increased fatty acid oxidation (PMID:29293500)
- Study shows that PARP10 is downregulated in intrahepatic metastatic hepatocellular carcinoma. Further results provide evidence that deficiency of PARP10 markedly increased the migration and invasion of tumor cells through regulation of epithelial-mesenchymal transition, and that PARP10 expression inhibited tumor metastasis in vivo. (PMID:29515234)
- PARP10 promotes cellular proliferation, and its overexpression alleviates cellular sensitivity to replication stress and fosters the restart of stalled replication forks. In mouse xenograft studies, PARP10 loss reduces the tumorigenesis activity of HeLa cells. Its overexpression results in tumor formation by non-transformed RPE-1 cells. PARP10 may promote cellular transformation by alleviating replication stress. (PMID:30032250)
- PLK1/NF-kappaB feedforward circuit antagonizes the mono-ADP-ribosyltransferase activity of PARP10 and facilitates HCC progression. (PMID:32060423)
- [PARP10 Influences the Proliferation of Colorectal Carcinoma Cells, a Preliminary Study]. (PMID:32392194)
- The mono-ADP-ribosyltransferase ARTD10 regulates the voltage-gated K(+) channel Kv1.1 through protein kinase C delta. (PMID:33059680)
- PARP10 is highly expressed and associated with inferior outcomes in acute myeloid leukemia. (PMID:37506247)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | parp10 | ENSDARG00000087145 |
| mus_musculus | Parp10 | ENSMUSG00000063268 |
| rattus_norvegicus | Parp10 | ENSRNOG00000004361 |
Paralogs (8): PARP12 (ENSG00000059378), ZC3HAV1 (ENSG00000105939), PARP11 (ENSG00000111224), PARP9 (ENSG00000138496), ZC3HAV1L (ENSG00000146858), TIPARP (ENSG00000163659), PARP14 (ENSG00000173193), PARP15 (ENSG00000173200)
Protein
Protein identifiers
Protein mono-ADP-ribosyltransferase PARP10 — Q53GL7 (reviewed: Q53GL7)
Alternative names: ADP-ribosyltransferase diphtheria toxin-like 10, Poly [ADP-ribose] polymerase 10
All UniProt accessions (15): E9PIA6, E9PIK9, E9PJI2, Q53GL7, E9PK67, E9PLE8, E9PM86, E9PNI7, E9PPE7, E9PPU2, E9PPV8, E9PQQ6, E9PSE7, E9PSG8, F8W8G7
UniProt curated annotations — full annotation on UniProt →
Function. ADP-ribosyltransferase that mediates mono-ADP-ribosylation of glutamate and aspartate residues on target proteins. In contrast to PARP1 and PARP2, it is not able to mediate poly-ADP-ribosylation. Catalyzes mono-ADP-ribosylation of GSK3B, leading to negatively regulate GSK3B kinase activity. Involved in translesion DNA synthesis in response to DNA damage via its interaction with PCNA.
Subunit / interactions. Interacts with MYC. Interacts with PARP14. Interacts (via-PIP box and ubiquitin-interacting motifs) with PCNA.
Subcellular location. Nucleus. Nucleolus. Cytoplasm.
Tissue specificity. Highly expressed in spleen and thymus. Intermediate levels in liver, kidney, pancreas, prostate, testis, ovary, intestine, and leukocytes. Low expression in heart, brain, placenta, lung, skeletal muscle, and colon.
Post-translational modifications. Stimulated through its phosphorylation by CDK2. Acquires CDK-dependent phosphorylation through late-G1 to S phase, and from prometaphase to cytokinesis in the nucleolar organizing regions. Phosphorylation is suppressed in growth-arrested cells. Auto-mono-ADP-ribosylated on glutamate and lysine residues.
Domain organisation. The PIP-box mediates the interaction with PCNA.
Similarity. Belongs to the ARTD/PARP family.
RefSeq proteins (2): NP_001304824, NP_116178* (*=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR012317 | Poly(ADP-ribose)pol_cat_dom | Domain |
| IPR012677 | Nucleotide-bd_a/b_plait_sf | Homologous_superfamily |
| IPR034464 | PAR10_RRM1_2 | Domain |
| IPR052056 | Mono-ARTD/PARP | Family |
Pfam: PF00644, PF23085
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), 3 shown:
- L-aspartyl-[protein] + NAD(+) = 4-O-(ADP-D-ribosyl)-L-aspartyl-[protein] + nicotinamide (RHEA:54424)
- L-lysyl-[protein] + NAD(+) = N(6)-(ADP-D-ribosyl)-L-lysyl-[protein] + nicotinamide + H(+) (RHEA:58220)
- L-glutamyl-[protein] + NAD(+) = 5-O-(ADP-D-ribosyl)-L-glutamyl-[protein] + nicotinamide (RHEA:58224)
UniProt features (70 total): strand 19, modified residue 11, helix 9, mutagenesis site 8, region of interest 5, sequence conflict 5, sequence variant 3, turn 3, short sequence motif 3, compositionally biased region 2, chain 1, domain 1
Structure
Experimental structures (PDB)
7 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 5LX6 | X-RAY DIFFRACTION | 1.25 |
| 9FRP | X-RAY DIFFRACTION | 1.4 |
| 9FRS | X-RAY DIFFRACTION | 2.02 |
| 3HKV | X-RAY DIFFRACTION | 2.1 |
| 6FXI | X-RAY DIFFRACTION | 2.6 |
| 9RLS | X-RAY DIFFRACTION | 2.75 |
| 2DHX | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q53GL7-F1 | 68.85 | 0.22 |
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 (11): 101, 106, 140, 378, 423, 431, 663, 882, 916, 916, 1011
Mutagenesis-validated functional residues (8):
| Position | Phenotype |
|---|---|
| 650–690 | decreased interaction with pcna. |
| 831–838 | abolishes interaction with pcna. |
| 882 | decreased auto-mono-adp-ribosylation. |
| 888 | abolishes catalytic activity; abolishes interaction with parp14. |
| 980–982 | strongly decreased catalytic activity. |
| 985 | strongly decreased catalytic activity. |
| 987 | decreased catalytic activity. |
| 999 | does not affect catalytic activity. |
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: 144 (showing top):
GOZGIT_ESR1_TARGETS_DN, GOBP_DNA_DAMAGE_TOLERANCE, GOBP_MONOCARBOXYLIC_ACID_METABOLIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_FIBROBLAST_PROLIFERATION, GOBP_NEGATIVE_REGULATION_OF_NF_KAPPAB_TRANSCRIPTION_FACTOR_ACTIVITY, GOBP_NEGATIVE_REGULATION_OF_MOLECULAR_FUNCTION, GOBP_DNA_DAMAGE_RESPONSE, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GOBP_PROTEIN_POLYUBIQUITINATION, GOBP_DNA_BIOSYNTHETIC_PROCESS, GOBP_NEGATIVE_REGULATION_OF_PROTEIN_METABOLIC_PROCESS, GOBP_ORGANIC_ACID_METABOLIC_PROCESS, GOBP_PROTEIN_K63_LINKED_UBIQUITINATION, CCAGGGG_MIR331, GOBP_REGULATION_OF_PROTEIN_POLYUBIQUITINATION
GO Biological Process (14): DNA repair (GO:0006281), chromatin organization (GO:0006325), negative regulation of gene expression (GO:0010629), viral protein processing (GO:0019082), translesion synthesis (GO:0019985), obsolete negative regulation of NF-kappaB transcription factor activity (GO:0032088), negative regulation of fibroblast proliferation (GO:0048147), protein poly-ADP-ribosylation (GO:0070212), protein auto-ADP-ribosylation (GO:0070213), negative regulation of protein K63-linked ubiquitination (GO:1900045), nicotinate metabolic process (GO:1901847), DNA damage response (GO:0006974), NAD+ biosynthetic process via the salvage pathway (GO:0034355), negative regulation of DNA-templated transcription (GO:0045892)
GO Molecular Function (13): transcription corepressor activity (GO:0003714), NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), nucleotidyltransferase activity (GO:0016779), K63-linked polyubiquitin modification-dependent protein binding (GO:0070530), DNA-binding transcription factor binding (GO:0140297), NAD+-protein-lysine ADP-ribosyltransferase activity (GO:0140804), NAD+-protein-aspartate ADP-ribosyltransferase activity (GO:0140806), NAD+-protein-glutamate ADP-ribosyltransferase activity (GO:0140807), NAD+-protein mono-ADP-ribosyltransferase activity (GO:1990404), nucleic acid binding (GO:0003676), protein binding (GO:0005515), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757)
GO Cellular Component (5): nucleus (GO:0005634), nucleolus (GO:0005730), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794), cytosol (GO:0005829)
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 |
|---|---|
| NAD+-protein mono-ADP-ribosyltransferase activity | 3 |
| post-translational protein modification | 2 |
| pentosyltransferase activity | 2 |
| binding | 2 |
| intracellular membrane-bounded organelle | 2 |
| cellular anatomical structure | 2 |
| cytoplasm | 2 |
| DNA metabolic process | 1 |
| DNA damage response | 1 |
| cellular component organization | 1 |
| gene expression | 1 |
| regulation of gene expression | 1 |
| negative regulation of macromolecule biosynthetic process | 1 |
| viral process | 1 |
| viral gene expression | 1 |
| DNA damage tolerance | 1 |
| DNA synthesis involved in DNA replication | 1 |
| negative regulation of cell population proliferation | 1 |
| fibroblast proliferation | 1 |
| regulation of fibroblast proliferation | 1 |
| protein K63-linked ubiquitination | 1 |
| regulation of protein K63-linked ubiquitination | 1 |
| negative regulation of protein polyubiquitination | 1 |
| alkaloid metabolic process | 1 |
| monocarboxylic acid metabolic process | 1 |
| pyridine-containing compound metabolic process | 1 |
| cellular response to stress | 1 |
| NAD+ biosynthetic process | 1 |
| pyridine nucleotide salvage | 1 |
| purine nucleotide salvage | 1 |
| DNA-templated transcription | 1 |
| regulation of DNA-templated transcription | 1 |
| negative regulation of RNA biosynthetic process | 1 |
| transcription coregulator activity | 1 |
| negative regulation of DNA-templated transcription | 1 |
| transferase activity, transferring phosphorus-containing groups | 1 |
| polyubiquitin modification-dependent protein binding | 1 |
| transcription factor binding | 1 |
| catalytic activity, acting on a protein | 1 |
| catalytic activity | 1 |
Protein interactions and networks
STRING
1008 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PARP10 | MYC | P01106 | 874 |
| PARP10 | PLEC | Q15149 | 801 |
| PARP10 | PARP16 | Q8N5Y8 | 776 |
| PARP10 | PARP2 | Q9UGN5 | 766 |
| PARP10 | PARP1 | P09874 | 764 |
| PARP10 | PARP3 | Q9Y6F1 | 753 |
| PARP10 | TRPT1 | Q86TN4 | 732 |
| PARP10 | PARP6 | Q2NL67 | 716 |
| PARP10 | PARP4 | Q9UKK3 | 711 |
| PARP10 | PARP8 | Q8N3A8 | 699 |
| PARP10 | SNTB2 | Q13425 | 684 |
| PARP10 | MACROD2 | A1Z1Q3 | 662 |
| PARP10 | MACROD1 | Q9BQ69 | 661 |
| PARP10 | ADPRS | Q9NX46 | 656 |
| PARP10 | TNKS | O95271 | 625 |
IntAct
17 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| MACROD2 | PARP10 | psi-mi:“MI:1310”(de-ADP-ribosylation reaction) | 0.440 |
| PARP10 | psi-mi:“MI:1310”(de-ADP-ribosylation reaction) | 0.440 | |
| rep | PARP10 | psi-mi:“MI:1310”(de-ADP-ribosylation reaction) | 0.440 |
| POA1 | PARP10 | psi-mi:“MI:1310”(de-ADP-ribosylation reaction) | 0.440 |
| PARP10 | psi-mi:“MI:0557”(adp ribosylation reaction) | 0.440 | |
| CASP6 | PARP10 | psi-mi:“MI:0194”(cleavage reaction) | 0.440 |
| CASP8 | PARP10 | psi-mi:“MI:0194”(cleavage reaction) | 0.440 |
| OARD1 | PARP10 | psi-mi:“MI:0414”(enzymatic reaction) | 0.440 |
| PARP10 | OARD1 | psi-mi:“MI:0414”(enzymatic reaction) | 0.440 |
| CA10 | ENTPD5 | psi-mi:“MI:0914”(association) | 0.350 |
| RNF114 | DST | psi-mi:“MI:0914”(association) | 0.350 |
| RNF166 | WASL | psi-mi:“MI:0914”(association) | 0.350 |
| PARP10 | psi-mi:“MI:0915”(physical association) | 0.000 |
BioGRID (65): UBC (Reconstituted Complex), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), PARP10 (Affinity Capture-MS), Parp14 (Co-localization), PARP10 (Reconstituted Complex), PARP10 (Reconstituted Complex), PARP10 (Affinity Capture-Western), RAN (Biochemical Activity), PARP10 (Affinity Capture-RNA)
ESM2 similar proteins: A1L3T7, A2A3L6, A4IFI1, A7E3N7, A8MYJ7, A8VU90, O94761, O94812, O95153, O95382, P97680, Q0P5G1, Q13671, Q14154, Q3UYR4, Q4V896, Q53GL7, Q569K6, Q58CQ5, Q58EX7, Q66H85, Q6DT37, Q6F5E8, Q6ZVH7, Q76MJ5, Q7TNF8, Q7Z3H0, Q80UU1, Q80UW5, Q8BWA8, Q8BXP5, Q8BYG0, Q8CIE4, Q8CJ00, Q8IYJ3, Q8NAG6, Q8TE82, Q91WA6, Q91WE1, Q921Q7
Diamond homologs: A1Z1Q3, A4W960, A7MG20, A8AI35, B4T2X8, B5F961, B5RBF3, B5XXK9, B7LT90, C9Y0V8, D2TT52, D3RKJ0, D5CE05, E1PL40, E1SDF1, O28751, O59182, O75367, O93327, P0A8D6, P0A8D7, P0A8D8, P0C6F6, P0C6T4, P0C6T6, P0C6T8, P0C6T9, P0C6U0, P0C6U1, P0C6U7, P0C6W3, P0C6W5, P0C6W7, P0C6W8, P0C6W9, P0C6X0, P0C6X6, P67341, P67342, P9WK28
SIGNOR signaling
3 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PARP10 | “up-regulates activity” | G3BP1 | “post translational modification” |
| PLK1 | “up-regulates activity” | PARP10 | phosphorylation |
| CyclinE/CDK2 | “up-regulates activity” | PARP10 | phosphorylation |
Disease & clinical
Clinical variants and AI predictions
ClinVar
219 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 1 |
| Uncertain significance | 165 |
| Likely benign | 24 |
| Benign | 1 |
Top pathogenic / likely-pathogenic (1)
| Variant ID | HGVS | Classification |
|---|---|---|
| 804412 | NM_032789.5(PARP10):c.647_648del (p.Thr216fs) | Likely pathogenic |
SpliceAI
2915 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 8:143977826:CGTGG:C | acceptor_gain | 1.0000 |
| 8:143977831:C:CC | acceptor_gain | 1.0000 |
| 8:143977901:CCTCA:C | donor_loss | 1.0000 |
| 8:143977902:CTCAC:C | donor_loss | 1.0000 |
| 8:143977903:TCAC:T | donor_loss | 1.0000 |
| 8:143977904:CAC:C | donor_loss | 1.0000 |
| 8:143977905:A:AC | donor_gain | 1.0000 |
| 8:143977905:ACCG:A | donor_loss | 1.0000 |
| 8:143977906:C:CC | donor_gain | 1.0000 |
| 8:143978077:TCCAC:T | acceptor_gain | 1.0000 |
| 8:143978078:CCAC:C | acceptor_gain | 1.0000 |
| 8:143978078:CCACC:C | acceptor_gain | 1.0000 |
| 8:143978079:CAC:C | acceptor_gain | 1.0000 |
| 8:143978079:CACC:C | acceptor_gain | 1.0000 |
| 8:143978080:AC:A | acceptor_gain | 1.0000 |
| 8:143978080:ACC:A | acceptor_loss | 1.0000 |
| 8:143978081:CC:C | acceptor_gain | 1.0000 |
| 8:143978082:C:CA | acceptor_loss | 1.0000 |
| 8:143978082:C:CC | acceptor_gain | 1.0000 |
| 8:143978083:T:G | acceptor_loss | 1.0000 |
| 8:143982927:CTCA:C | donor_loss | 1.0000 |
| 8:143982929:CA:C | donor_loss | 1.0000 |
| 8:143982930:A:AC | donor_gain | 1.0000 |
| 8:143982930:ACACG:A | donor_loss | 1.0000 |
| 8:143982931:C:CC | donor_gain | 1.0000 |
| 8:143982931:CA:C | donor_gain | 1.0000 |
| 8:143983063:CCA:C | acceptor_gain | 1.0000 |
| 8:143983064:CA:C | acceptor_gain | 1.0000 |
| 8:143983064:CAC:C | acceptor_gain | 1.0000 |
| 8:143983066:C:CC | acceptor_gain | 1.0000 |
AlphaMissense
6503 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 8:143977589:G:C | F991L | 0.997 |
| 8:143977589:G:T | F991L | 0.997 |
| 8:143977591:A:G | F991L | 0.997 |
| 8:143977932:G:C | F902L | 0.997 |
| 8:143977932:G:T | F902L | 0.997 |
| 8:143977933:A:G | F902S | 0.997 |
| 8:143977934:A:G | F902L | 0.997 |
| 8:143977731:A:G | F944S | 0.995 |
| 8:143977802:G:C | F920L | 0.995 |
| 8:143977802:G:T | F920L | 0.995 |
| 8:143977803:A:G | F920S | 0.995 |
| 8:143977804:A:G | F920L | 0.995 |
| 8:143977598:G:C | F988L | 0.994 |
| 8:143977598:G:T | F988L | 0.994 |
| 8:143977600:A:G | F988L | 0.994 |
| 8:143977982:A:C | Y886D | 0.994 |
| 8:143977631:G:C | S977R | 0.993 |
| 8:143977631:G:T | S977R | 0.993 |
| 8:143977633:T:G | S977R | 0.993 |
| 8:143977730:G:C | F944L | 0.993 |
| 8:143977730:G:T | F944L | 0.993 |
| 8:143977732:A:G | F944L | 0.993 |
| 8:143977557:A:T | I1002N | 0.992 |
| 8:143977560:A:G | L1001P | 0.992 |
| 8:143977584:T:A | D993V | 0.992 |
| 8:143977590:A:G | F991S | 0.992 |
| 8:143977596:A:T | V989D | 0.992 |
| 8:143977739:C:A | K941N | 0.992 |
| 8:143977739:C:G | K941N | 0.992 |
| 8:143977557:A:G | I1002T | 0.991 |
dbSNP variants (sampled 300 via entrez): RS1000129401 (8:144001650 G>A), RS1000247414 (8:144001509 C>A), RS1000410038 (8:144008243 G>C), RS1000602570 (8:143990929 A>G), RS1000670787 (8:143995847 G>A), RS1000881324 (8:143979100 A>G), RS1000954880 (8:143984394 T>C), RS1000974009 (8:143978829 A>C,G), RS1001264450 (8:143993141 G>A,T), RS1001610286 (8:143986771 C>G,T), RS1001763387 (8:143987022 T>G), RS1001796389 (8:144003389 A>G), RS1001911072 (8:144003018 C>A), RS1002023312 (8:144009384 G>C,T), RS1002271584 (8:143992192 A>C)
Disease associations
OMIM: gene MIM:609564 | disease phenotypes:
GenCC curated gene-disease
Mondo (0):
Orphanet (0):
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
8 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST002541_68 | Menarche (age at onset) | 1.000000e-08 |
| GCST008103_86 | Bipolar disorder | 1.000000e-06 |
| GCST008115_8 | Bipolar I disorder | 2.000000e-08 |
| GCST010703_132 | Brain morphology (MOSTest) | 3.000000e-08 |
| GCST90002390_617 | Mean corpuscular hemoglobin | 4.000000e-13 |
| GCST90002392_525 | Mean corpuscular volume | 2.000000e-15 |
| GCST90002404_105 | Red cell distribution width | 1.000000e-22 |
| GCST90020026_753 | Hip index | 3.000000e-09 |
EFO canonical traits (6, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0004703 | age at menarche |
| EFO:0009963 | bipolar I disorder |
| EFO:0004346 | neuroimaging measurement |
| EFO:0004527 | mean corpuscular hemoglobin |
| EFO:0009188 | Red cell distribution width |
| EFO:0008039 | BMI-adjusted hip circumference |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2429708 (SINGLE PROTEIN)
Molecules with ChEMBL bioactivity
6 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 39,549 (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 |
| CHEMBL3137320 | TALAZOPARIB | 4 | 5,534 |
| CHEMBL521686 | OLAPARIB | 4 | 13,038 |
| CHEMBL4112930 | PAMIPARIB | 3 | 2,114 |
| CHEMBL506871 | VELIPARIB | 3 | 5,421 |
PharmGKB: 1 entry (VIP=true, CPIC=false)
GtoPdb / IUPHAR curated pharmacology
(IUPHAR/BPS Guide to Pharmacology — expert-curated)
Target class: enzyme — Mono-ADP-ribosylating PARPs
Most potent curated ligand interactions (3 total), top 3:
| Ligand | Action | Affinity | Parameter |
|---|---|---|---|
| compound 8a [PMID: 35500474] | Inhibition | 6.85 | pIC50 |
| compound 32 [PMID: 30006177] | Inhibition | 6.64 | pIC50 |
| OUL35 | Inhibition | 6.48 | pIC50 |
ChEMBL bioactivities
286 potent at pChembl≥5 of 331 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 8.11 | IC50 | 7.8 | nM | CHEMBL5404785 |
| 8.11 | IC50 | 7.762 | nM | CHEMBL5404785 |
| 7.97 | IC50 | 10.8 | nM | CHEMBL5402698 |
| 7.60 | IC50 | 25 | nM | CHEMBL5431108 |
| 7.60 | IC50 | 25.12 | nM | CHEMBL5431108 |
| 6.93 | IC50 | 117.5 | nM | CHEMBL5404785 |
| 6.92 | IC50 | 120 | nM | CHEMBL5404785 |
| 6.89 | IC50 | 130 | nM | CHEMBL5192839 |
| 6.87 | IC50 | 134.9 | nM | CHEMBL5181947 |
| 6.87 | IC50 | 134.9 | nM | CHEMBL5192839 |
| 6.85 | IC50 | 140 | nM | CHEMBL5181947 |
| 6.85 | IC50 | 140 | nM | CHEMBL5176874 |
| 6.82 | IC50 | 150 | nM | CHEMBL5200358 |
| 6.82 | IC50 | 151.4 | nM | CHEMBL5200358 |
| 6.81 | IC50 | 154.9 | nM | CHEMBL5187187 |
| 6.81 | IC50 | 156 | nM | CHEMBL5207717 |
| 6.80 | IC50 | 160 | nM | CHEMBL5187187 |
| 6.80 | IC50 | 160 | nM | CHEMBL5200521 |
| 6.80 | IC50 | 158.5 | nM | CHEMBL5200521 |
| 6.75 | IC50 | 180 | nM | CHEMBL4287262 |
| 6.75 | IC50 | 180 | nM | CHEMBL5431108 |
| 6.73 | IC50 | 186.2 | nM | CHEMBL4287262 |
| 6.73 | IC50 | 186.2 | nM | CHEMBL5431108 |
| 6.65 | IC50 | 223.9 | nM | CHEMBL6170252 |
| 6.64 | IC50 | 230 | nM | CHEMBL4208737 |
| 6.63 | IC50 | 234.4 | nM | CHEMBL4208737 |
| 6.61 | IC50 | 245.5 | nM | CHEMBL4128574 |
| 6.60 | IC50 | 250 | nM | CHEMBL4128574 |
| 6.54 | IC50 | 290 | nM | CHEMBL5186967 |
| 6.54 | IC50 | 288.4 | nM | CHEMBL5186967 |
| 6.51 | IC50 | 310 | nM | CHEMBL5181107 |
| 6.51 | IC50 | 309 | nM | CHEMBL5181107 |
| 6.50 | IC50 | 320 | nM | CHEMBL5421878 |
| 6.50 | IC50 | 316.2 | nM | CHEMBL5421878 |
| 6.49 | IC50 | 325 | nM | CHEMBL5395820 |
| 6.48 | IC50 | 329 | nM | CHEMBL1438938 |
| 6.48 | IC50 | 330 | nM | CHEMBL1438938 |
| 6.46 | IC50 | 350 | nM | OLAPARIB |
| 6.42 | IC50 | 382 | nM | OLAPARIB |
| 6.42 | IC50 | 377 | nM | CHEMBL5571636 |
| 6.41 | IC50 | 390 | nM | CHEMBL4125748 |
| 6.41 | IC50 | 387.3 | nM | CHEMBL4125748 |
| 6.40 | IC50 | 398.1 | nM | CHEMBL4129789 |
| 6.40 | IC50 | 400 | nM | CHEMBL4129789 |
| 6.34 | IC50 | 460 | nM | CHEMBL4130035 |
| 6.34 | IC50 | 460 | nM | CHEMBL4127497 |
| 6.34 | IC50 | 457.1 | nM | CHEMBL4127497 |
| 6.33 | IC50 | 467.7 | nM | CHEMBL4129923 |
| 6.33 | IC50 | 467.7 | nM | CHEMBL4130035 |
| 6.33 | IC50 | 470 | nM | CHEMBL4129923 |
PubChem BioAssay actives
287 with measured affinity, of 484 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 |
|---|---|---|---|---|
| 5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine | 1965928: Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay | ic50 | 0.0078 | uM |
| 4-[[3-[3-(5-bromofuran-2-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one | 2012702: Inhibition of PARP10 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay | ic50 | 0.0108 | uM |
| 6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine | 1965928: Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay | ic50 | 0.0250 | uM |
| 6-(cyclopentylmethoxy)-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.1300 | uM |
| 6-(cyclohexylmethoxy)-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.1349 | uM |
| 4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]-N-[4-[(4-methoxyphenyl)carbamoyl]phenyl]piperazine-1-carboxamide | 1868363: Inhibition of PARP-10 (unknown origin) | ic50 | 0.1400 | uM |
| 6-[(2-fluorophenyl)methoxy]-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.1500 | uM |
| 6-(cyclobutylmethoxy)-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.1549 | uM |
| 4-[(8-methyl-4-oxo-7-prop-1-ynyl-3H-quinazolin-2-yl)methylsulfanyl]benzoic acid | 1869173: Inhibition of PARP10 (unknown origin) | ic50 | 0.1560 | uM |
| 6-(thiophen-3-ylmethoxy)-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.1585 | uM |
| 4-(4-carbamoylphenoxy)benzoic acid | 1405638: Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | ic50 | 0.1800 | uM |
| 4-[(2-fluorophenyl)methoxy]benzamide | 1405638: Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | ic50 | 0.2300 | uM |
| 4-[3-[4-(3-fluorophenyl)piperidine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.2455 | uM |
| 4-(cyclobutylmethoxy)benzamide | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.2884 | uM |
| 6-(cyclopropylmethoxy)-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.3090 | uM |
| [1,2,4]triazolo[3,4-b][1,3]benzothiazole-5,8-diol | 1965915: Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+ | ic50 | 0.3162 | uM |
| 5-(trifluoromethyl)-4-[[(2S)-1-[3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazine-1-carbonyl]azetidin-1-yl]propan-2-yl]amino]-1H-pyridazin-6-one | 1965304: Inhibition of human recombinant N-terminal FLAG-tagged / C-terminal Strep-tagged PARP10 (805 to 1025 end residues) expressed in baculovirus infected Sf9 cells expression system incubated for 1 hr by ELISA assay | ic50 | 0.3250 | uM |
| 4-(4-carbamoylphenoxy)benzamide | 1496070: Inhibition of full length recombinant His6-tagged PARP10 catalytic domain (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence based assay | ic50 | 0.3290 | uM |
| Olaparib | 2019996: Inhibition of human N-terminal FLAG-tagged/C-terminal Strep-tagged recombinant PARP10 (805 to 1025 residues) expressed in Sf9 cells | ic50 | 0.3500 | uM |
| 2-[(2S)-1-oxo-1-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propan-2-yl]indazole-7-carboxamide | 2096830: Inhibition of PARP10 (unknown origin) measured after 1 hr incubation by microplate reader assay | ic50 | 0.3770 | uM |
| 4-[3-[4-(4-fluorophenyl)-4-hydroxypiperidine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.3873 | uM |
| 4-[3-[4-(4-fluorophenyl)piperidine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.3981 | uM |
| 4-[3-[4-(2-fluorophenyl)piperazine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.4571 | uM |
| 4-[3-[4-(3-fluorophenyl)piperazine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.4600 | uM |
| 4-[3-[4-(2-fluorophenyl)piperidine-1-carbonyl]phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.4677 | uM |
| 3-(4-carbamoylphenoxy)benzamide | 1869165: Inhibition of C-terminal his-tagged human PARP10 expressed in Escherichia coli Rosette2 (DE3) | ic50 | 0.4800 | uM |
| 5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole | 1965915: Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+ | ic50 | 0.4898 | uM |
| Rucaparib | 1428394: Inhibition of full length recombinant human His6-tagged PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.5623 | uM |
| 4-[3-(4-phenylpiperidine-1-carbonyl)phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.5754 | uM |
| 4-(cyclopentylmethoxy)benzamide | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.5888 | uM |
| 4-[3-(3-phenylpiperidine-1-carbonyl)phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.6000 | uM |
| 4-(cyclopropylmethoxy)benzamide | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.6000 | uM |
| 4-(cyclobutylmethoxy)-2-fluorobenzamide | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.6166 | uM |
| 4-(4-formylphenoxy)benzamide | 1405638: Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | ic50 | 0.6166 | uM |
| 5-methyl-6-(1H-pyrrolo[2,3-b]pyridin-5-yl)-3,4-dihydro-2H-isoquinolin-1-one | 1515545: Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | ic50 | 0.7079 | uM |
| 4-cyclobutyloxybenzamide | 1405638: Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | ic50 | 0.7200 | uM |
| methyl (Z)-4-(3-carbamoylanilino)-4-oxobut-2-enoate | 1202205: Inhibition of hexahistidine-tagged full length human recombinant ARTD10 expressed in Escherichia coli BL21(DE3) assessed as Inhibition of ADP-ribosyltransferase activity incubated for 15 mins using biotin-NAD+ by chemiluminescence detection based assay | ic50 | 0.7586 | uM |
| 4-[3-(3-phenylpyrrolidine-1-carbonyl)phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 0.7762 | uM |
| 8-methoxy-4H-thieno[2,3-c]isoquinolin-5-one | 1833808: Inhibition of PARP10 (809 to 1017 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 13 hrs by fluorescence based assay | ic50 | 0.7800 | uM |
| 8-ethoxy-4H-thieno[2,3-c]isoquinolin-5-one | 1833808: Inhibition of PARP10 (809 to 1017 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 13 hrs by fluorescence based assay | ic50 | 0.9200 | uM |
| 4-(cyclohexylmethoxy)-2-fluorobenzamide | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 0.9550 | uM |
| ethyl 1-[3-(4-carbamoylphenoxy)benzoyl]piperidine-4-carboxylate | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 1.0600 | uM |
| 4-[3-(4-phenylpiperazine-1-carbonyl)phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 1.0715 | uM |
| 6-(1H-indol-5-yl)-5-methyl-3,4-dihydro-2H-isoquinolin-1-one | 1515545: Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | ic50 | 1.0965 | uM |
| 4-[3-(2-phenylpiperidine-1-carbonyl)phenoxy]benzamide | 1496062: Inhibition of full length recombinant His6-tagged human PARP10 expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay | ic50 | 1.0965 | uM |
| 5,7-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole | 1965915: Inhibition of N-terminal MBP tagged/C-terminal PARP10 (unknown origin) expressed in Escherichia coli in presence of NAD+ | ic50 | 1.1000 | uM |
| 4-phenoxybenzamide | 1405638: Inhibition of C-terminal His-tagged human ARTD10 (809 to 1017 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 13 hrs in presence of NAD+ | ic50 | 1.1000 | uM |
| 6-(3-chlorophenyl)-3,4-dihydro-2H-isoquinolin-1-one | 1515545: Inhibition of human PARP10 catalytic domain assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay | ic50 | 1.1000 | 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 | 2080542: Inhibition of PARP10 (unknown origin) | ic50 | 1.1030 | uM |
| 6-[(3-bromophenyl)methoxy]-2,3-dihydrophthalazine-1,4-dione | 1868249: Inhibition of human PARP-10 using NAD+ as substrate incubated for 10 mins by fluorescence based analysis | ic50 | 1.1482 | uM |
CTD chemical–gene interactions
39 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Air Pollutants | affects expression, increases abundance, decreases expression | 2 |
| Nickel | increases expression | 2 |
| Tobacco Smoke Pollution | decreases expression | 2 |
| Valproic Acid | increases methylation, decreases expression | 2 |
| Particulate Matter | decreases expression, increases abundance | 2 |
| aristolochic acid I | increases expression | 1 |
| FR900359 | increases phosphorylation | 1 |
| SBI-797812 | increases activity | 1 |
| bisphenol A | decreases methylation | 1 |
| diisononyl phthalate | increases methylation | 1 |
| beta-lapachone | increases expression, decreases expression | 1 |
| sodium arsenite | increases expression | 1 |
| pentanal | increases expression | 1 |
| di-n-butylphosphoric acid | affects expression | 1 |
| veliparib | affects binding | 1 |
| jinfukang | increases expression, affects cotreatment | 1 |
| (+)-JQ1 compound | decreases expression | 1 |
| Temozolomide | increases expression | 1 |
| Sunitinib | increases expression | 1 |
| Acetaminophen | decreases expression | 1 |
| Arsenic | affects expression | 1 |
| Vehicle Emissions | decreases expression, increases abundance | 1 |
| Benzo(a)pyrene | decreases methylation | 1 |
| Cisplatin | affects cotreatment, increases expression | 1 |
| Doxorubicin | decreases expression | 1 |
| Estradiol | decreases expression | 1 |
| Ethyl Methanesulfonate | increases expression | 1 |
| Formaldehyde | increases expression | 1 |
| Methyl Methanesulfonate | increases expression | 1 |
| NAD | decreases abundance | 1 |
ChEMBL screening assays
70 unique, capped per target: 69 binding, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL2433125 | Binding | Inhibition of human ARTD10 (809 to 1017) using NAD+ as substrate at 1 uM by fluorescence assay | Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. — J Med Chem |
| CHEMBL4345424 | ADMET | Inhibition of human recombinant N-terminal TEV-cleavgae site-fused-FLAG/Polyhis-tagged PARP10 (2 to 583 residues) expressed in Escherichia coli assessed as reduction in auto-PARylation using histone as substrate measured after 45 mins in pr | Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. — J Med Chem |
Cellosaurus cell lines
2 cell lines: 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B1GU | Abcam A-549 PARP10 KO 1 | Cancer cell line | Male |
| CVCL_B2PD | Abcam A-549 PARP10 KO 2 | Cancer cell line | Male |
Clinical trials (associated diseases)
0 trials via MONDO — disease-level, not drug-specific.
Related Atlas pages
No linked Atlas pages yet — the cross-entity mesh grows as the corpus expands.