PARP15

Summary

PARP15 (poly(ADP-ribose) polymerase family member 15, HGNC:26876) is a protein-coding gene on chromosome 3q21.1, encoding Protein mono-ADP-ribosyltransferase PARP15 (Q460N3). Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins.

Enables NAD+ binding activity; pentosyltransferase activity; and transcription corepressor activity. Involved in negative regulation of transcription by RNA polymerase II and protein poly-ADP-ribosylation. Predicted to be active in cytoplasm and nucleus. Biomarker of atherosclerosis.

Source: NCBI Gene 165631 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 81 total
• Druggable target: yes — 3 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001113523

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:26876
Approved symbol	PARP15
Name	poly(ADP-ribose) polymerase family member 15
Location	3q21.1
Locus type	gene with protein product
Status	Approved
Aliases	FLJ40597, pART7, ARTD7, BAL3
Ensembl gene	ENSG00000173200
Ensembl biotype	protein_coding
OMIM	612066
Entrez	165631

Gene structure

Transcript identifiers

Ensembl transcripts: 11 — 9 protein_coding, 2 protein_coding_CDS_not_defined

ENST00000310366, ENST00000464300, ENST00000465304, ENST00000473627, ENST00000483793, ENST00000493645, ENST00000900351, ENST00000900352, ENST00000900353, ENST00000900354, ENST00000900355

RefSeq mRNA: 4 — MANE Select: NM_001113523 NM_001113523, NM_001308320, NM_001308321, NM_152615

CCDS: CCDS3016, CCDS46893, CCDS77803, CCDS77804

Canonical transcript exons

ENST00000464300 — 12 exons

Exon	Start	End
ENSE00001498033	122577650	122577853
ENSE00001864722	122635811	122639047
ENSE00003503567	122605936	122606055
ENSE00003512268	122635020	122635194
ENSE00003526178	122610494	122610730
ENSE00003528227	122615779	122615857
ENSE00003534342	122617015	122617164
ENSE00003619027	122613041	122613268
ENSE00003625732	122619781	122619843
ENSE00003661228	122632086	122632219
ENSE00003671076	122626827	122627033
ENSE00003692980	122621444	122621611

Expression profiles

Bgee: expression breadth ubiquitous, 149 present calls, max score 93.35.

FANTOM5 (CAGE): breadth broad, TPM avg 3.4371 / max 153.6954, expressed in 328 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
38244	2.7633	278
38243	0.3720	132
38242	0.3018	133

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
spleen	UBERON:0002106	93.35	gold quality
granulocyte	CL:0000094	92.82	gold quality
vermiform appendix	UBERON:0001154	90.79	gold quality
lymph node	UBERON:0000029	87.69	gold quality
small intestine Peyer’s patch	UBERON:0003454	84.29	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	80.30	gold quality
caecum	UBERON:0001153	80.03	gold quality
small intestine	UBERON:0002108	78.91	gold quality
upper lobe of left lung	UBERON:0008952	78.49	gold quality
right lung	UBERON:0002167	76.90	gold quality
blood	UBERON:0000178	76.15	gold quality
right lobe of liver	UBERON:0001114	76.12	gold quality
upper lobe of lung	UBERON:0008948	76.10	gold quality
bone marrow cell	CL:0002092	75.56	gold quality
rectum	UBERON:0001052	75.50	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	75.24	gold quality
leukocyte	CL:0000738	74.74	gold quality
tonsil	UBERON:0002372	73.91	gold quality
gall bladder	UBERON:0002110	73.84	gold quality
monocyte	CL:0000576	73.71	gold quality
hindlimb stylopod muscle	UBERON:0004252	72.57	gold quality
omental fat pad	UBERON:0010414	71.70	gold quality
peritoneum	UBERON:0002358	71.61	gold quality
buccal mucosa cell	CL:0002336	71.36	silver quality
right coronary artery	UBERON:0001625	70.07	gold quality
adipose tissue of abdominal region	UBERON:0007808	70.00	gold quality
colonic epithelium	UBERON:0000397	69.70	silver quality
transverse colon	UBERON:0001157	69.56	gold quality
left uterine tube	UBERON:0001303	68.80	gold quality
smooth muscle tissue	UBERON:0001135	68.31	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	32.10
E-CURD-122	yes	21.25
E-MTAB-9067	yes	13.11

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

108 targeting PARP15, 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-5692A	100.00	74.40	6850
HSA-MIR-10401-5P	99.99	65.79	948
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-4531	99.99	69.70	3181
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-512-3P	99.97	67.35	1049
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-96-5P	99.95	72.80	2140
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-381-3P	99.93	71.87	2854
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-539-5P	99.93	70.30	2855
HSA-MIR-300	99.92	71.76	2856
HSA-MIR-12133	99.92	71.82	2006
HSA-MIR-6768-5P	99.92	67.36	1942
HSA-MIR-10523-5P	99.91	69.22	2038
HSA-MIR-1271-5P	99.91	71.99	1972
HSA-MIR-7-1-3P	99.91	71.53	4384
HSA-MIR-7-2-3P	99.91	71.40	4394
HSA-MIR-589-3P	99.91	69.62	2088
HSA-MIR-5680	99.91	69.83	3421
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-3529-3P	99.90	73.55	3045

Literature-anchored findings (GeneRIF, showing 2)

• BAL macro domains repress transcription when tethered to a promoter; BAL2 and BAL3, but not BAL1, exhibit PARP activity (PMID:16061477)
• The current study investigated the possible association between PARP15 single-nucleotide polymorphisms and the risk of acute myeloid leukemia (AML). The results from a Cox regression analysis for overall survival revealed that two polymorphisms associated with increased overall survival and the signal for rs17208928 was retained after correcting for multiple tests. rs17208928 showed a significant association with survival (PMID:27610459)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	si:ch211-244b2.4	ENSDARG00000045530
danio_rerio	parp12b	ENSDARG00000057974
danio_rerio	si:ch211-244b2.3	ENSDARG00000069244
danio_rerio	parp14rs3	ENSDARG00000098398
danio_rerio		ENSDARG00000107280
danio_rerio		ENSDARG00000112454

Paralogs (8): PARP12 (ENSG00000059378), ZC3HAV1 (ENSG00000105939), PARP11 (ENSG00000111224), PARP9 (ENSG00000138496), ZC3HAV1L (ENSG00000146858), TIPARP (ENSG00000163659), PARP14 (ENSG00000173193), PARP10 (ENSG00000178685)

Protein

Protein identifiers

Protein mono-ADP-ribosyltransferase PARP15 — Q460N3 (reviewed: Q460N3)

Alternative names: ADP-ribosyltransferase diphtheria toxin-like 7, B-aggressive lymphoma protein 3, Poly [ADP-ribose] polymerase 15

All UniProt accessions (3): Q460N3, B7ZL48, C9J7L3

UniProt curated annotations — full annotation on UniProt →

Function. Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins. Acts as a negative regulator of transcription.

Subcellular location. Nucleus.

Similarity. Belongs to the ARTD/PARP family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q460N3-1	1	yes
Q460N3-2	2

RefSeq proteins (4): NP_001106995, NP_001295249, NP_001295250, NP_689828 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002589	Macro_dom	Domain
IPR012317	Poly(ADP-ribose)pol_cat_dom	Domain
IPR043472	Macro_dom-like	Homologous_superfamily
IPR052056	Mono-ARTD/PARP	Family

Pfam: PF00644, PF01661

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), 2 shown:

• L-aspartyl-[protein] + NAD(+) = 4-O-(ADP-D-ribosyl)-L-aspartyl-[protein] + nicotinamide (RHEA:54424)
• L-glutamyl-[protein] + NAD(+) = 5-O-(ADP-D-ribosyl)-L-glutamyl-[protein] + nicotinamide (RHEA:58224)

UniProt features (55 total): strand 20, helix 12, binding site 6, domain 3, sequence variant 3, mutagenesis site 3, splice variant 2, compositionally biased region 2, chain 1, sequence conflict 1, region of interest 1, turn 1

Structure

Experimental structures (PDB)

48 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
7OTF	X-RAY DIFFRACTION	1.3
7PWM	X-RAY DIFFRACTION	1.35
7F41	X-RAY DIFFRACTION	1.4
7PW3	X-RAY DIFFRACTION	1.4
7F42	X-RAY DIFFRACTION	1.41
9IFV	X-RAY DIFFRACTION	1.43
7OSP	X-RAY DIFFRACTION	1.44
7OSS	X-RAY DIFFRACTION	1.5
7PWC	X-RAY DIFFRACTION	1.5
7Z1V	X-RAY DIFFRACTION	1.5
7Z2O	X-RAY DIFFRACTION	1.5
6EK3	X-RAY DIFFRACTION	1.6
7OSX	X-RAY DIFFRACTION	1.6
7OUW	X-RAY DIFFRACTION	1.6
7PWA	X-RAY DIFFRACTION	1.6
7PWR	X-RAY DIFFRACTION	1.6
7PX7	X-RAY DIFFRACTION	1.6
7F43	X-RAY DIFFRACTION	1.62
7PX6	X-RAY DIFFRACTION	1.65
7OTH	X-RAY DIFFRACTION	1.7
7PWQ	X-RAY DIFFRACTION	1.7
7Z1Y	X-RAY DIFFRACTION	1.75
9FEG	X-RAY DIFFRACTION	1.75
7PWK	X-RAY DIFFRACTION	1.8
7PWS	X-RAY DIFFRACTION	1.8
9RLP	X-RAY DIFFRACTION	1.8
9RLQ	X-RAY DIFFRACTION	1.8
7PWU	X-RAY DIFFRACTION	1.9
7R4A	X-RAY DIFFRACTION	1.9
7Z1W	X-RAY DIFFRACTION	1.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q460N3-F1	79.72	0.46

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 (6): 335; 409–413; 449; 312–313; 324–325; 331

Mutagenesis-validated functional residues (3):

Position	Phenotype
559	abolishes catalytic activity.
560	slightly reduces catalytic activity. abolishes activity; when associated with y-559 and c-604.
604	reduces catalytic activity 20-fold. abolishes activity; when associated with y-559 and a-560.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 71 (showing top): GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, ZHAN_MULTIPLE_MYELOMA_LB_UP, chr3q21, GOMF_GLYCOSYLTRANSFERASE_ACTIVITY, GOMF_NAD_BINDING, SENGUPTA_EBNA1_ANTICORRELATED, GOMF_TRANSCRIPTION_COREPRESSOR_ACTIVITY, GOMF_ADENYL_NUCLEOTIDE_BINDING, GOMF_PENTOSYLTRANSFERASE_ACTIVITY, GOMF_TRANSFERASE_ACTIVITY_TRANSFERRING_PHOSPHORUS_CONTAINING_GROUPS, GOBP_NEGATIVE_REGULATION_OF_TRANSCRIPTION_BY_RNA_POLYMERASE_II, GOBP_NEGATIVE_REGULATION_OF_NUCLEOBASE_CONTAINING_COMPOUND_METABOLIC_PROCESS, GOBP_PROTEIN_POLY_ADP_RIBOSYLATION, GOMF_TRANSCRIPTION_COREGULATOR_ACTIVITY, GOMF_NADPLUS_BINDING

GO Biological Process (3): negative regulation of transcription by RNA polymerase II (GO:0000122), negative regulation of gene expression (GO:0010629), protein poly-ADP-ribosylation (GO:0070212)

GO Molecular Function (10): transcription corepressor activity (GO:0003714), NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), nucleotidyltransferase activity (GO:0016779), NAD+ binding (GO:0070403), NAD+-protein-aspartate ADP-ribosyltransferase activity (GO:0140806), 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 (2): nucleus (GO:0005634), cytoplasm (GO:0005737)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
negative regulation of DNA-templated transcription	2
pentosyltransferase activity	2
NAD+-protein mono-ADP-ribosyltransferase activity	2
regulation of transcription by RNA polymerase II	1
transcription by RNA polymerase II	1
gene expression	1
regulation of gene expression	1
negative regulation of macromolecule biosynthetic process	1
post-translational protein modification	1
transcription coregulator activity	1
transferase activity, transferring phosphorus-containing groups	1
anion binding	1
NAD binding	1
catalytic activity, acting on a protein	1
binding	1
catalytic activity	1
transferase activity	1
intracellular membrane-bounded organelle	1
intracellular anatomical structure	1
cellular anatomical structure	1

Protein interactions and networks

STRING

838 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARP15	DTX3L	Q8TDB6	862
PARP15	PARP16	Q8N5Y8	806
PARP15	PARP1	P09874	784
PARP15	PARP3	Q9Y6F1	749
PARP15	PARP4	Q9UKK3	745
PARP15	PARP6	Q2NL67	705
PARP15	PARP2	Q9UGN5	690
PARP15	PARP8	Q8N3A8	675
PARP15	TRPT1	Q86TN4	673
PARP15	PARG	Q86W56	623
PARP15	ADPRS	Q9NX46	622
PARP15	OARD1	Q9Y530	601
PARP15	GDAP2	Q9NXN4	584
PARP15	PARP12	Q9H0J9	558
PARP15	ART5	Q96L15	488

IntAct

1 interactions, top by confidence:

BioGRID (4): PARP15 (Two-hybrid), PARP15 (Affinity Capture-RNA), PARP15 (Cross-Linking-MS (XL-MS)), APP (Reconstituted Complex)

ESM2 similar proteins: A5D6R3, A5PJN5, A6X935, B3DLB3, D9IVE5, E9PYK3, O00329, O00534, O02668, O35904, O43548, O46510, P16452, P19687, P19827, P21671, P49222, P79263, P97278, P97279, Q02108, Q0VCM5, Q14624, Q29052, Q3T052, Q3TDX8, Q460N3, Q4R6L3, Q4ZHS0, Q501S4, Q502I6, Q5R8R3, Q5XHI4, Q61702, Q61703, Q62711, Q68EJ0, Q6NTR1, Q6P6V7, Q6PCI6

Diamond homologs: A0A166ACJ5, A0A559KX76, A1Z1Q3, A4W960, A7MG20, A7T167, A8AI35, B4T2X8, B5F961, B5RBF3, B5XXK9, B7LT90, C9Y0V8, D2TT52, D3RKJ0, D5CE05, E1PL40, E1SDF1, O28751, O59182, O67112, O75367, O93327, P0A8D6, P0A8D7, P0A8D8, P0DC28, P0DC29, P0DN70, P67341, P67342, P67343, P67344, P9WK28, P9WK29, Q02874, Q0T5Z6, Q2EMV9, Q2KHU5, Q2KIX2

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	61
Likely benign	8
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

2537 predictions. Top by Δscore:

Variant	Effect	Δscore
3:122610492:A:G	acceptor_gain	1.0000
3:122621574:G:GT	donor_gain	1.0000
3:122635016:GCAGA:G	acceptor_loss	1.0000
3:122635018:A:AG	acceptor_gain	1.0000
3:122635019:G:A	acceptor_loss	1.0000
3:122635019:G:GG	acceptor_gain	1.0000
3:122635019:GATT:G	acceptor_gain	1.0000
3:122635174:G:GT	donor_gain	1.0000
3:122635808:CAGCT:C	acceptor_loss	1.0000
3:122635809:A:AG	acceptor_gain	1.0000
3:122635809:A:C	acceptor_loss	1.0000
3:122635809:AGCT:A	acceptor_gain	1.0000
3:122635810:G:GA	acceptor_gain	1.0000
3:122635810:GC:G	acceptor_gain	1.0000
3:122635810:GCT:G	acceptor_gain	1.0000
3:122635810:GCTG:G	acceptor_gain	1.0000
3:122635810:GCTGT:G	acceptor_gain	1.0000
3:122577846:G:GT	donor_gain	0.9900
3:122577849:GTATG:G	donor_gain	0.9900
3:122605934:A:AG	acceptor_gain	0.9900
3:122605935:G:GG	acceptor_gain	0.9900
3:122605935:GTCCA:G	acceptor_gain	0.9900
3:122606029:A:G	donor_gain	0.9900
3:122606054:GG:G	donor_gain	0.9900
3:122606055:GG:G	donor_gain	0.9900
3:122610489:TTAA:T	acceptor_loss	0.9900
3:122610490:TAA:T	acceptor_loss	0.9900
3:122610493:G:GG	acceptor_gain	0.9900
3:122610496:C:A	acceptor_gain	0.9900
3:122613126:G:GT	donor_gain	0.9900

AlphaMissense

4448 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
3:122613137:T:C	F214L	0.979
3:122613139:T:A	F214L	0.979
3:122613139:T:G	F214L	0.979
3:122621588:T:A	V403D	0.975
3:122610507:T:A	V107D	0.971
3:122626874:G:C	A427P	0.964
3:122635119:T:C	F558L	0.964
3:122635121:C:A	F558L	0.964
3:122635121:C:G	F558L	0.964
3:122636081:T:C	L673P	0.964
3:122613065:T:C	C190R	0.962
3:122635837:T:C	F592L	0.962
3:122635839:T:A	F592L	0.962
3:122635839:T:G	F592L	0.962
3:122636089:T:C	F676L	0.959
3:122636091:C:A	F676L	0.959
3:122636091:C:G	F676L	0.959
3:122635167:T:C	F574L	0.955
3:122635169:T:A	F574L	0.955
3:122635169:T:G	F574L	0.955
3:122636041:T:C	F660L	0.955
3:122636043:T:A	F660L	0.955
3:122636043:T:G	F660L	0.955
3:122617149:T:C	F329L	0.952
3:122617151:T:A	F329L	0.952
3:122617151:T:G	F329L	0.952
3:122621584:T:C	S402P	0.951
3:122626923:T:A	V443D	0.951
3:122636050:T:C	F663L	0.951
3:122636052:C:A	F663L	0.951

dbSNP variants (sampled 300 via entrez): RS1000004831 (3:122622714 T>G), RS1000028196 (3:122609045 C>T), RS1000044232 (3:122627809 C>G), RS1000049615 (3:122634780 C>G), RS1000101516 (3:122635107 G>A), RS1000112731 (3:122586069 A>G), RS1000206379 (3:122619660 G>A), RS1000224660 (3:122583722 C>T), RS1000225213 (3:122609835 C>A), RS1000297455 (3:122578040 C>G,T), RS1000320762 (3:122631532 T>C), RS1000354912 (3:122595854 T>C), RS1000431364 (3:122622430 G>A,T), RS1000450770 (3:122589899 T>C), RS1000536978 (3:122579091 T>C)

Disease associations

OMIM: gene MIM:612066 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST001469_2	Major depressive disorder	6.000000e-06
GCST002126_25	Periodontitis (CDC/AAP)	3.000000e-06

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2176778 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

3 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 26,480 (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

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 (2 total), top 2:

Ligand	Action	Affinity	Parameter
A101-(CONH2)-B322	Inhibition	6.7	pIC50
compound 8a [PMID: 35500474]	Inhibition	6.4	pIC50

ChEMBL bioactivities

106 potent at pChembl≥5 of 134 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.25	IC50	56	nM	CHEMBL5404785
7.25	IC50	56.23	nM	CHEMBL5404785
6.92	IC50	120	nM	CHEMBL5404785
6.91	IC50	123	nM	CHEMBL5404785
6.70	IC50	200	nM	CHEMBL5195249
6.70	IC50	200	nM	CHEMBL5190289
6.67	IC50	213.8	nM	CHEMBL6149709
6.65	IC50	223.9	nM	CHEMBL6147827
6.64	IC50	230	nM	CHEMBL3108871
6.59	IC50	257	nM	CHEMBL5431108
6.58	IC50	260	nM	CHEMBL5431108
6.54	IC50	290	nM	CHEMBL5421878
6.53	IC50	295.1	nM	CHEMBL5431108
6.52	IC50	300	nM	CHEMBL5431108
6.50	IC50	320	nM	CHEMBL5192839
6.49	IC50	323.6	nM	CHEMBL5192839
6.47	IC50	338.8	nM	CHEMBL6170252
6.44	IC50	363.1	nM	CHEMBL5200358
6.43	IC50	370	nM	CHEMBL5187187
6.43	IC50	370	nM	CHEMBL5200358
6.40	IC50	400	nM	CHEMBL5181947
6.40	IC50	400	nM	CHEMBL5200521
6.40	IC50	398.1	nM	CHEMBL5181947
6.40	IC50	398.1	nM	CHEMBL5200521
6.32	IC50	478.6	nM	CHEMBL5187187
6.30	IC50	496	nM	CHEMBL5207717
6.29	IC50	510	nM	CHEMBL5187652
6.28	IC50	520	nM	CHEMBL4089522
6.28	IC50	527	nM	CHEMBL5084343
6.28	IC50	524.8	nM	CHEMBL5084343
6.23	IC50	588.8	nM	CHEMBL5186481
6.22	IC50	600	nM	CHEMBL5186481
6.11	IC50	780	nM	CHEMBL5402584
6.11	IC50	776.2	nM	CHEMBL5402584
6.04	IC50	916	nM	CHEMBL6170737
6.01	IC50	970	nM	CHEMBL5200663
5.97	IC50	1081	nM	CHEMBL6149971
5.96	IC50	1100	nM	CHEMBL5083566
5.95	IC50	1122	nM	CHEMBL5083566
5.93	IC50	1175	nM	CHEMBL5434061
5.92	IC50	1200	nM	CHEMBL4293771
5.92	IC50	1200	nM	CHEMBL5181107
5.92	IC50	1202	nM	CHEMBL5181107
5.92	IC50	1200	nM	CHEMBL5434061
5.90	IC50	1267	nM	OLAPARIB
5.89	IC50	1300	nM	CHEMBL5171357
5.87	IC50	1349	nM	CHEMBL5171357
5.85	IC50	1400	nM	CHEMBL5077731
5.80	IC50	1600	nM	CHEMBL3414768
5.80	IC50	1600	nM	CHEMBL5416085

PubChem BioAssay actives

93 with measured affinity, of 215 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	1965932: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.0560	uM
N-[(2S)-3-amino-2-[(3-methylbenzoyl)amino]-3-oxopropyl]-1,4-dioxo-2,3-dihydrophthalazine-6-carboxamide	1869184: Inhibition of biotinylated recombinant human PARP15 expressed in Escherichia coli BL21 (DE3)	ic50	0.2000	uM
N-[(2S)-1-amino-3-(1,4-dioxo-2,3-dihydrophthalazin-6-yl)-1,3-dioxopropan-2-yl]-3-methylbenzamide	1868269: Inhibition of PARP15 (unknown origin)	ic50	0.2000	uM
4H-thieno[2,3-c]isoquinolin-5-one	1833813: Inhibition of TEV cleavage site fused N-terminal 6His-tagged PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli Rosetta2 (DE3)	ic50	0.2300	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965932: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.2570	uM
[1,2,4]triazolo[3,4-b][1,3]benzothiazole-5,8-diol	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	0.2900	uM
4-(4-carbamoylphenoxy)benzamide	1802079: Enzymatic Activity Assay from Article 10.1016/j.chembiol.2016.08.012: “Small-Molecule Chemical Probe Rescues Cells from Mono-ADP-Ribosyltransferase ARTD10/PARP10-Induced Apoptosis and Sensitizes Cancer Cells to DNA Damage.”	ic50	0.2950	uM
6-(cyclopentylmethoxy)-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.3200	uM
6-[(2-fluorophenyl)methoxy]-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.3631	uM
6-(cyclobutylmethoxy)-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.3700	uM
6-(thiophen-3-ylmethoxy)-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.3981	uM
6-(cyclohexylmethoxy)-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.3981	uM
4-[(8-methyl-4-oxo-7-prop-1-ynyl-3H-quinazolin-2-yl)methylsulfanyl]benzoic acid	1869183: Inhibition of PARP15 (unknown origin)	ic50	0.4960	uM
N-[(2S)-3-(methylamino)-2-[(3-methylbenzoyl)amino]-3-oxopropyl]-1,4-dioxo-2,3-dihydrophthalazine-6-carboxamide	1869184: Inhibition of biotinylated recombinant human PARP15 expressed in Escherichia coli BL21 (DE3)	ic50	0.5100	uM
3-[[(Z)-4-[4-(4-fluorophenyl)piperazin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467143: Inhibition of His6-tagged PARP15 (unknown origin) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.5200	uM
8-methoxy-4H-thieno[2,3-c]isoquinolin-5-one	1833806: Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay	ic50	0.5248	uM
4-[(3-bromophenyl)methoxy]-2-fluorobenzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	0.5888	uM
6,8-dimethyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	0.7762	uM
N-[(2S)-3-amino-3-oxo-2-[[2-(2-oxochromen-7-yl)oxyacetyl]amino]propyl]-1,4-dioxo-2,3-dihydrophthalazine-6-carboxamide	1869184: Inhibition of biotinylated recombinant human PARP15 expressed in Escherichia coli BL21 (DE3)	ic50	0.9700	uM
8-propan-2-yloxy-4H-thieno[2,3-c]isoquinolin-5-one	1833806: Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay	ic50	1.1000	uM
5-methoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	1.1749	uM
6-(cyclopropylmethoxy)-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	1.2000	uM
4-[(3-bromophenyl)methoxy]benzamide	1833806: Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay	ic50	1.2000	uM
6-[(3-bromophenyl)methoxy]-2,3-dihydrophthalazine-1,4-dione	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	1.3000	uM
8-hydroxy-4H-thieno[2,3-c]isoquinolin-5-one	1833806: Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay	ic50	1.4000	uM
2-[(3-carbamoylphenyl)carbamoyl]cyclopentene-1-carboxylic acid	1202207: Inhibition of hexahistidine-tagged human recombinant ARTD7 catalytic domain (459 to 656 amino acids) 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	1.6000	uM
5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	1.6000	uM
5,7-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	1.6000	uM
methyl (Z)-4-(3-carbamoylanilino)-4-oxobut-2-enoate	1202207: Inhibition of hexahistidine-tagged human recombinant ARTD7 catalytic domain (459 to 656 amino acids) 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	1.7000	uM
3-(4-carbamoylphenoxy)benzamide	1869166: Inhibition of N-terminal his-tagged human PARP15 expressed in Escherichia coli Rosette2 (DE3)	ic50	1.7000	uM
6-ethyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	1.9953	uM
[1,2,4]triazolo[3,4-b][1,3]benzothiazol-6-ol	1965932: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	2.0000	uM
8-methoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	2.1000	uM
8-ethoxy-4H-thieno[2,3-c]isoquinolin-5-one	1833806: Inhibition of PARP15 (482 to 678 residues) (unknown origin) expressed in Escherichia coli using NAD+ as substrate incubated for 3 hrs by fluorescence based assay	ic50	2.1000	uM
2-methoxy-4-(naphthalen-1-ylmethoxy)benzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	2.2000	uM
(Z)-4-(3-carbamoylanilino)-2-methyl-4-oxobut-2-enoic acid	1202207: Inhibition of hexahistidine-tagged human recombinant ARTD7 catalytic domain (459 to 656 amino acids) 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	2.3000	uM
4-(cyclobutylmethoxy)benzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	2.3988	uM
4-(1,3-thiazol-5-ylmethoxy)benzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	2.4000	uM
4-[(3-bromophenyl)methoxy]-2-methoxybenzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	2.5000	uM
4-[(2-fluorophenyl)methoxy]-2-methoxybenzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	2.6000	uM
Olaparib	2020000: Inhibition of human N-terminal GST-tagged recombinant PARP15 (221 to 444(end) residues) expressed in Escherichia coli	ic50	2.6000	uM
4-(4-carbamoylphenoxy)benzoic acid	1405647: Inhibition of N-terminal His-tagged human ARTD7 (482 to 678 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 3 hrs in presence of NAD+	ic50	2.6000	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	3.2000	uM
8-methyl-6-prop-1-ynyl-2-(pyrimidin-2-ylsulfanylmethyl)-3H-quinazolin-4-one	1853441: Inhibition of N-terminal His-tagged human PARP15 catalytic domain expressed in Escherichia coli BL21 (DE3) preincubated with 6-a-NAD+ for 5 to 10 mins followed by enzyme addition and measured after 60 mins using NAD+ as substrate byHRP based chemiluminescence assay	ic50	3.3000	uM
4-[(2-fluorophenyl)methoxy]benzamide	1405647: Inhibition of N-terminal His-tagged human ARTD7 (482 to 678 residues) expressed in Escherichia coli Rosetta2 (DE3) using SRPK2 as substrate after 3 hrs in presence of NAD+	ic50	3.3000	uM
4-(cyclohexylmethoxy)benzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	3.6000	uM
4-(cyclopentylmethoxy)benzamide	1868250: Inhibition of human N-terminal 6His-tagged PARP15 (460 to 656 residues) expressed in Escherichia coli Rosetta2 (DE3) cells using NAD+ as substrate incubated for 10 mins by fluorescence based analysis	ic50	3.8000	uM
6-propan-2-yl-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	3.8904	uM
6-methoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazole	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	4.0000	uM
[1,2,4]triazolo[3,4-b][1,3]benzothiazol-5-ol	1965916: Inhibition of N-terminal MBP tagged/C-terminal PARP15 (unknown origin) expressed in Escherichia coli in presence of NAD+	ic50	4.6773	uM

CTD chemical–gene interactions

17 total (human), top 17 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N-dimethylacetamide hydrochloride	affects binding	2
bisphenol F	affects cotreatment, increases methylation	1
triphenyl phosphate	affects expression	1
bisphenol A	affects cotreatment, increases methylation	1
2-methyl-4-isothiazolin-3-one	increases expression	1
CGP 52608	affects binding, increases reaction	1
2-palmitoylglycerol	increases expression	1
(+)-JQ1 compound	decreases expression	1
Fulvestrant	affects cotreatment, increases methylation	1
Air Pollutants	increases abundance, increases expression	1
Benzo(a)pyrene	increases methylation	1
Nickel	increases expression	1
Tobacco Smoke Pollution	decreases expression	1
Aflatoxin M1	decreases expression	1
Fluorescein-5-isothiocyanate	affects binding	1
Antirheumatic Agents	decreases expression	1
Particulate Matter	increases abundance, increases expression	1

ChEMBL screening assays

39 unique, capped per target: 39 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2187441	Binding	Binding affinity at human recombinant ARTD7 expressed in Escherichia coli BL21 (DE3) R3 pRARE cells assessed as thermal stability shift by differential scanning fluorimetry	Discovery of ligands for ADP-ribosyltransferases via docking-based virtual screening. — J Med Chem

Clinical trials (associated diseases)

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