PARP11

Summary

PARP11 (poly(ADP-ribose) polymerase family member 11, HGNC:1186) is a protein-coding gene on chromosome 12p13.32, encoding Protein mono-ADP-ribosyltransferase PARP11 (Q9NR21). Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins.

Enables NAD+ poly-ADP-ribosyltransferase activity and NAD+-protein mono-ADP-ribosyltransferase activity. Involved in protein auto-ADP-ribosylation. Located in cytosol; nuclear body; and nuclear envelope.

Source: NCBI Gene 57097 — RefSeq curated summary.

At a glance

• GWAS associations: 17
• Clinical variants (ClinVar): 44 total
• Druggable target: yes — 4 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_020367

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:1186
Approved symbol	PARP11
Name	poly(ADP-ribose) polymerase family member 11
Location	12p13.32
Locus type	gene with protein product
Status	Approved
Aliases	ARTD11
Ensembl gene	ENSG00000111224
Ensembl biotype	protein_coding
OMIM	616706
Entrez	57097

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 5 protein_coding, 3 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000228820, ENST00000416739, ENST00000427057, ENST00000447133, ENST00000450737, ENST00000453942, ENST00000458162, ENST00000476985, ENST00000939306

RefSeq mRNA: 3 — MANE Select: NM_020367 NM_001286521, NM_001286522, NM_020367

CCDS: CCDS66281, CCDS8523

Canonical transcript exons

ENST00000228820 — 8 exons

Exon	Start	End
ENSE00000713811	3828910	3829030
ENSE00001822303	3873212	3873399
ENSE00003462351	3814037	3814188
ENSE00003584086	3822085	3822157
ENSE00003592772	3821873	3822003
ENSE00003608133	3826158	3826233
ENSE00003620905	3829890	3830018
ENSE00003663393	3808861	3812439

Expression profiles

Bgee: expression breadth ubiquitous, 242 present calls, max score 94.22.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 5.7832 / max 97.8735, expressed in 1615 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
129002	2.2629	1164
129001	2.0959	1102
129000	0.8547	426
128998	0.4066	195
128999	0.1631	44

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
buccal mucosa cell	CL:0002336	94.22	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	87.22	gold quality
ganglionic eminence	UBERON:0004023	83.58	gold quality
adrenal tissue	UBERON:0018303	83.01	gold quality
monocyte	CL:0000576	82.42	gold quality
mononuclear cell	CL:0000842	82.12	gold quality
leukocyte	CL:0000738	82.01	gold quality
calcaneal tendon	UBERON:0003701	81.52	gold quality
cortical plate	UBERON:0005343	80.80	gold quality
corpus epididymis	UBERON:0004359	80.72	gold quality
germinal epithelium of ovary	UBERON:0001304	80.51	gold quality
ventricular zone	UBERON:0003053	80.19	gold quality
pigmented layer of retina	UBERON:0001782	79.76	gold quality
retina	UBERON:0000966	79.74	gold quality
right adrenal gland cortex	UBERON:0035827	79.37	gold quality
esophagus squamous epithelium	UBERON:0006920	79.21	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	78.85	gold quality
parietal pleura	UBERON:0002400	78.83	gold quality
right adrenal gland	UBERON:0001233	78.81	gold quality
tibia	UBERON:0000979	78.48	gold quality
visceral pleura	UBERON:0002401	78.32	gold quality
adrenal gland	UBERON:0002369	78.10	gold quality
stromal cell of endometrium	CL:0002255	78.04	gold quality
caput epididymis	UBERON:0004358	78.00	gold quality
left adrenal gland	UBERON:0001234	77.96	gold quality
pleura	UBERON:0000977	77.71	gold quality
islet of Langerhans	UBERON:0000006	77.68	gold quality
tonsil	UBERON:0002372	77.57	gold quality
left adrenal gland cortex	UBERON:0035825	77.36	gold quality
lymph node	UBERON:0000029	77.17	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.15

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

164 targeting PARP11, 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-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-4262	100.00	73.26	3931
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-6833-3P	100.00	70.63	3197
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-3134	100.00	66.43	777
HSA-MIR-7110-3P	100.00	73.18	2486
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6873-3P	100.00	71.42	2626
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-6867-5P	100.00	82.21	3464
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-196A-1-3P	99.99	72.15	2772
HSA-MIR-6077	99.99	68.04	2299
HSA-MIR-181A-5P	99.99	72.96	2995
HSA-MIR-181B-5P	99.99	72.97	2996
HSA-MIR-181C-5P	99.99	72.95	2996
HSA-MIR-181D-5P	99.99	73.04	2997
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-150-5P	99.99	66.69	1976

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	parp11	ENSDARG00000098716
mus_musculus	Parp11	ENSMUSG00000037997
rattus_norvegicus	Parp11	ENSRNOG00000060689

Paralogs (8): PARP12 (ENSG00000059378), ZC3HAV1 (ENSG00000105939), PARP9 (ENSG00000138496), ZC3HAV1L (ENSG00000146858), TIPARP (ENSG00000163659), PARP14 (ENSG00000173193), PARP15 (ENSG00000173200), PARP10 (ENSG00000178685)

Protein

Protein identifiers

Protein mono-ADP-ribosyltransferase PARP11 — Q9NR21 (reviewed: Q9NR21)

Alternative names: ADP-ribosyltransferase diphtheria toxin-like 11, Poly [ADP-ribose] polymerase 11

All UniProt accessions (4): Q9NR21, F5H8L8, F8WFA3, G3V0I3

UniProt curated annotations — full annotation on UniProt →

Function. Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins. Plays a role in nuclear envelope stability and nuclear remodeling during spermiogenesis. Inhibits the type I interferon activated signaling pathway. Mechanistically, mono-ADP-ribosylates beta-TrCP/BTRC to promote IFNAR1 ubiquitination and protect BTRC from ubiquitin-proteasome degradation. Additionally, acts as an antiviral factor by cooperating with PARP12 to suppress Zika virus replication, independent of IFNAR1 regulation or intrinsic PARP enzymatic activity. Instead, facilitates the degradation of viral NS1 and NS3 proteins, potentially disrupting viral replication.

Subunit / interactions. Interacts with PARP12; this interaction plays a role in zika virus suppression.

Subcellular location. Nucleus. Nuclear pore complex.

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

Induction. By type I interferon or viral infection including zika virus infection.

Miscellaneous. May be produced at very low levels due to a premature stop codon in the mRNA, leading to nonsense-mediated mRNA decay.

Similarity. Belongs to the ARTD/PARP family.

Isoforms (4)

UniProt ID	Names	Canonical?
Q9NR21-4	1	yes
Q9NR21-2	2
Q9NR21-1	3
Q9NR21-5	4

RefSeq proteins (3): NP_001273450, NP_001273451, NP_065100* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004170	WWE_dom	Domain
IPR012317	Poly(ADP-ribose)pol_cat_dom	Domain
IPR037197	WWE_dom_sf	Homologous_superfamily
IPR051712	ARTD-AVP	Family

Pfam: PF00644, PF02825

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), 4 shown:

• L-aspartyl-[protein] + NAD(+) = 4-O-(ADP-D-ribosyl)-L-aspartyl-[protein] + nicotinamide (RHEA:54424)
• L-cysteinyl-[protein] + NAD(+) = S-(ADP-D-ribosyl)-L-cysteinyl-[protein] + nicotinamide + H(+) (RHEA:56612)
• 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 (31 total): mutagenesis site 9, strand 7, splice variant 5, modified residue 5, domain 2, chain 1, helix 1, turn 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
2DK6	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NR21-F1	81.73	0.55

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 (5): 13, 18, 56, 72, 87

Mutagenesis-validated functional residues (9):

Position	Phenotype
38	no effect on subcellular location at the nuclear envelope.
48	no effect on subcellular location at the nuclear envelope.
84	loss of subcellular location at the nuclear envelope.
93	loss of subcellular location at the nuclear envelope.
102	loss of subcellular location at the nuclear envelope.
204	catalytically inactive mutant; when associated with s-236.
205	catalytically inactive mutant.
205	no effect on subcellular location at the nuclear envelope.
236	catalytically inactive mutant; when associated with s-204.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 172 (showing top): GOBP_MALE_GAMETE_GENERATION, GOBP_NUCLEUS_ORGANIZATION, GOBP_NUCLEOBASE_CONTAINING_COMPOUND_TRANSPORT, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, GOBP_ENDOMEMBRANE_SYSTEM_ORGANIZATION, GOBP_DEVELOPMENTAL_PROCESS_INVOLVED_IN_REPRODUCTION, GOBP_NUCLEAR_ENVELOPE_ORGANIZATION, GOBP_MEMBRANE_ORGANIZATION, GOBP_RNA_LOCALIZATION, GOCC_NUCLEAR_ENVELOPE, GOCC_NUCLEAR_BODY, ZHENG_BOUND_BY_FOXP3, GOCC_NUCLEAR_PORE, SCGGAAGY_ELK1_02, GOMF_GLYCOSYLTRANSFERASE_ACTIVITY

GO Biological Process (6): nuclear envelope organization (GO:0006998), spermatogenesis (GO:0007283), protein transport (GO:0015031), cell differentiation (GO:0030154), mRNA transport (GO:0051028), protein auto-ADP-ribosylation (GO:0070213)

GO Molecular Function (10): NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), nucleotidyltransferase activity (GO:0016779), NAD+-protein-cysteine ADP-ribosyltransferase activity (GO:0140803), 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), protein binding (GO:0005515), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757)

GO Cellular Component (6): nucleus (GO:0005634), nuclear envelope (GO:0005635), nuclear pore (GO:0005643), nucleoplasm (GO:0005654), cytosol (GO:0005829), nuclear body (GO:0016604)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
NAD+-protein mono-ADP-ribosyltransferase activity	4
pentosyltransferase activity	2
cellular anatomical structure	2
nucleus organization	1
endomembrane system organization	1
membrane organization	1
developmental process involved in reproduction	1
male gamete generation	1
transport	1
intracellular protein localization	1
establishment of protein localization	1
cellular developmental process	1
RNA transport	1
post-translational protein modification	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity, acting on a protein	1
binding	1
catalytic activity	1
transferase activity	1
intracellular membrane-bounded organelle	1
nucleus	1
endomembrane system	1
organelle envelope	1
nuclear envelope	1
nuclear protein-containing complex	1
nuclear lumen	1
cytoplasm	1
nucleoplasm	1
intracellular membraneless organelle	1

Protein interactions and networks

STRING

520 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARP11	PARP16	Q8N5Y8	707
PARP11	PARP8	Q8N3A8	705
PARP11	TRPT1	Q86TN4	687
PARP11	PARP6	Q2NL67	684
PARP11	PARP3	Q9Y6F1	658
PARP11	PARP4	Q9UKK3	619
PARP11	PARP2	Q9UGN5	605
PARP11	ADPRS	Q9NX46	500
PARP11	RNF146	Q9NTX7	485
PARP11	PARP1	P09874	476
PARP11	PARG	Q86W56	470
PARP11	MACROD1	Q9BQ69	461
PARP11	MACROD2	A1Z1Q3	445
PARP11	HPF1	Q9NWY4	444
PARP11	NUDT16	Q96DE0	405

IntAct

7 interactions, top by confidence:

A	B	Type	Score
PARP11	TRIP13	psi-mi:“MI:0915”(physical association)	0.490
PARP11	MDFI	psi-mi:“MI:0915”(physical association)	0.370
PARP11	GTPBP3	psi-mi:“MI:0915”(physical association)	0.370
PARP11	LYZ	psi-mi:“MI:0914”(association)	0.350
PARP11	MAPK12	psi-mi:“MI:0914”(association)	0.350

BioGRID (25): PARP11 (Two-hybrid), RNF114 (Affinity Capture-MS), MAPK12 (Affinity Capture-MS), RNF166 (Affinity Capture-MS), GTPBP3 (Two-hybrid), PARP11 (Biochemical Activity), RNF166 (Affinity Capture-MS), MAPK12 (Affinity Capture-MS), RNF114 (Affinity Capture-MS), PARP11 (Affinity Capture-MS), CTNNB1 (Affinity Capture-Western), PARP11 (Two-hybrid), PARP11 (Two-hybrid), LHX4 (Two-hybrid), GTPBP3 (Two-hybrid)

ESM2 similar proteins: A9JRL3, D2HRF1, E1C3P4, E9PYK3, F4IVI0, O35099, O43148, Q149N8, Q1RMU2, Q3UD82, Q3ULW8, Q4R7K1, Q5JPI3, Q5M8G6, Q5RED8, Q5U2Q4, Q5ZJX5, Q66H62, Q6DD21, Q6P1E7, Q7SY78, Q7TMM8, Q7TPQ3, Q7Z3E1, Q80TQ2, Q811C2, Q8BZ20, Q8C1B2, Q8CFF0, Q8IXQ6, Q8IZC4, Q8K4M9, Q8N3A8, Q8N5Y8, Q91XL9, Q940Y1, Q96DT6, Q99683, Q9BXB4, Q9BXT6

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

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	37
Likely benign	1
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1746 predictions. Top by Δscore:

Variant	Effect	Δscore
12:3814032:ATTAC:A	donor_loss	1.0000
12:3814033:TTA:T	donor_loss	1.0000
12:3814034:TACCT:T	donor_loss	1.0000
12:3814036:C:T	donor_loss	1.0000
12:3821867:TCTCA:T	donor_loss	1.0000
12:3821868:CTCA:C	donor_loss	1.0000
12:3821869:TCA:T	donor_loss	1.0000
12:3821870:CA:C	donor_loss	1.0000
12:3821872:CC:C	donor_loss	1.0000
12:3822000:TAAG:T	acceptor_gain	1.0000
12:3822000:TAAGC:T	acceptor_loss	1.0000
12:3822002:AG:A	acceptor_gain	1.0000
12:3822004:C:CC	acceptor_gain	1.0000
12:3822005:T:G	acceptor_loss	1.0000
12:3822079:TCTTA:T	donor_loss	1.0000
12:3822080:CTTA:C	donor_loss	1.0000
12:3822081:TTA:T	donor_loss	1.0000
12:3822082:TAC:T	donor_loss	1.0000
12:3822083:AC:A	donor_loss	1.0000
12:3822084:C:CG	donor_loss	1.0000
12:3822153:TGTAA:T	acceptor_gain	1.0000
12:3822155:TAA:T	acceptor_gain	1.0000
12:3822158:C:CC	acceptor_gain	1.0000
12:3822159:T:C	acceptor_gain	1.0000
12:3822159:T:TC	acceptor_gain	1.0000
12:3822165:C:CT	acceptor_gain	1.0000
12:3822166:A:T	acceptor_gain	1.0000
12:3822168:C:CT	acceptor_gain	1.0000
12:3822169:A:T	acceptor_gain	1.0000
12:3829885:GGTA:G	donor_loss	1.0000

AlphaMissense

2314 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:3812148:G:T	P331H	1.000
12:3812152:A:C	Y330D	1.000
12:3812168:A:C	F324L	1.000
12:3812168:A:T	F324L	1.000
12:3812170:A:G	F324L	1.000
12:3812207:A:C	C311W	1.000
12:3812271:C:T	G290E	1.000
12:3812286:C:T	G285E	1.000
12:3812298:C:G	R281P	1.000
12:3812439:C:T	G234E	1.000
12:3814037:C:G	G234R	1.000
12:3814037:C:T	G234R	1.000
12:3814042:C:A	G232V	1.000
12:3814042:C:T	G232E	1.000
12:3814043:C:G	G232R	1.000
12:3814043:C:T	G232R	1.000
12:3814071:T:A	R222S	1.000
12:3814071:T:G	R222S	1.000
12:3814072:C:A	R222I	1.000
12:3814072:C:G	R222T	1.000
12:3814129:A:G	F203S	1.000
12:3821899:G:C	N174K	1.000
12:3821899:G:T	N174K	1.000
12:3822117:A:G	W129R	1.000
12:3822117:A:T	W129R	1.000
12:3826184:T:A	R106S	1.000
12:3826184:T:G	R106S	1.000
12:3826185:C:G	R106T	1.000
12:3829904:A:G	W45R	1.000
12:3829904:A:T	W45R	1.000

dbSNP variants (sampled 300 via entrez): RS1000037168 (12:3816501 T>G), RS1000104232 (12:3829315 C>A), RS1000284868 (12:3853744 A>C), RS1000329172 (12:3867632 A>G), RS1000408968 (12:3811161 C>T), RS1000458142 (12:3822078 C>T), RS1000465513 (12:3859967 A>T), RS1000512667 (12:3824327 C>T), RS1000557470 (12:3847079 G>A), RS1000568065 (12:3824585 A>T), RS1000577625 (12:3874158 A>G), RS1000631718 (12:3817756 G>C), RS1000702389 (12:3852351 G>T), RS1000714832 (12:3830709 G>A,T), RS1000840427 (12:3837001 A>C)

Disease associations

OMIM: gene MIM:616706 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

17 associations (top):

Study	Trait	p-value
GCST000579_28	Cognitive performance	8.000000e-06
GCST001792_1	Colorectal cancer	3.000000e-08
GCST001792_2	Colorectal cancer	5.000000e-10
GCST002248_9	Fasting insulin (dietary factor interaction)	8.000000e-06
GCST002253_1	Homeostasis model assessment of insulin resistance (dietary factor interaction)	9.000000e-06
GCST005993_55	Mean corpuscular hemoglobin	1.000000e-26
GCST005994_11	Hematocrit	1.000000e-09
GCST005996_37	Red blood cell count	5.000000e-28
GCST006011_85	Mean corpuscular volume	1.000000e-29
GCST006871_4	Total hippocampal volume	1.000000e-09
GCST007096_149	Pulse pressure	1.000000e-08
GCST007880_4	Emotional lability in attention deficit hyperactivity disorder	4.000000e-06
GCST008969_3	White coat effect (clinic diastolic blood pressure minus ambulatory diastolic blood pressure)	4.000000e-06
GCST011956_132	Systemic lupus erythematosus	4.000000e-08
GCST90002390_46	Mean corpuscular hemoglobin	8.000000e-11
GCST90002392_367	Mean corpuscular volume	2.000000e-09
GCST90016675_9	Pancreas fat	2.000000e-11

EFO canonical traits (10, from GWAS)

EFO ID	Trait name
EFO:0003926	neuropsychological test
EFO:0008111	diet measurement
EFO:0004501	HOMA-IR
EFO:0004527	mean corpuscular hemoglobin
EFO:0004348	hematocrit
EFO:0004305	erythrocyte count
EFO:0005035	hippocampal volume
EFO:0005763	pulse pressure measurement
EFO:0008475	mood instability measurement
EFO:0006945	diastolic blood pressure change measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2380189 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

4 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 20,932 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL3137320	TALAZOPARIB	4	5,534
CHEMBL521686	OLAPARIB	4	13,038
CHEMBL4112930	PAMIPARIB	3	2,114
CHEMBL5095043	ATAMPARIB	1	246

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

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs2532560	Efficacy	3	antidepressants	Major Depressive Disorder

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2532560	PARP11	3	0.00	1	antidepressants

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
ITK7	Inhibition	7.85	pIC50

ChEMBL bioactivities

41 potent at pChembl≥5 of 70 total, top 39 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.85	IC50	14	nM	CHEMBL5191676
7.17	IC50	67	nM	CHEMBL5199558
7.00	IC50	99	nM	CHEMBL5207717
6.85	IC50	140	nM	TALAZOPARIB
6.70	IC50	200	nM	CHEMBL5187963
6.62	IC50	240	nM	CHEMBL5404785
6.61	IC50	245.5	nM	CHEMBL5404785
6.33	IC50	470	nM	CHEMBL5431108
6.33	IC50	467.7	nM	CHEMBL5431108
6.26	IC50	550	nM	CHEMBL5186007
5.93	IC50	1175	nM	CHEMBL4580007
5.92	IC50	1200	nM	CHEMBL4580007
5.68	IC50	2100	nM	CHEMBL125200
5.68	IC50	2100	nM	CHEMBL1438938
5.68	IC50	2089	nM	CHEMBL1438938
5.67	IC50	2138	nM	CHEMBL125200
5.66	IC50	2166	nM	CHEMBL5402698
5.64	IC50	2281	nM	ATAMPARIB
5.64	IC50	2300	nM	ATAMPARIB
5.57	IC50	2700	nM	PAMIPARIB
5.54	IC50	2900	nM	CHEMBL4470303
5.54	IC50	2884	nM	CHEMBL4470303
5.43	IC50	3752	nM	CHEMBL6170737
5.38	IC50	4200	nM	CHEMBL4455412
5.38	IC50	4169	nM	CHEMBL4455412
5.34	IC50	4600	nM	CHEMBL4573527
5.34	IC50	4571	nM	CHEMBL4573527
5.31	IC50	4900	nM	CHEMBL4577063
5.31	IC50	4898	nM	CHEMBL4577063
5.24	IC50	5800	nM	CHEMBL4450751
5.24	IC50	5754	nM	CHEMBL4450751
5.22	IC50	6026	nM	CHEMBL4572268
5.21	IC50	6100	nM	CHEMBL4572268
5.11	IC50	7811	nM	OLAPARIB
5.10	IC50	8000	nM	CHEMBL1688212
5.10	IC50	7943	nM	CHEMBL1688212
5.06	IC50	8700	nM	CHEMBL4565850
5.06	IC50	8710	nM	CHEMBL4565850
5.03	IC50	9400	nM	CHEMBL5406267

PubChem BioAssay actives

40 with measured affinity, of 101 total; 24 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
8-methyl-7-prop-1-ynyl-2-(pyrimidin-2-ylsulfanylmethyl)-3H-quinazolin-4-one	1868264: Inhibition of human full length GFP-tagged PARP11 in human HeLa cells incubated for 3 hrs by chemiluminescence based analysis	ic50	0.0140	uM
3-[4-(2-hydroxypropan-2-yl)phenyl]-6-methyl-2H-pyrrolo[1,2-a]pyrazin-1-one	1925212: Inhibition of N-terminal GST-tagged/C-terminal 6xHis-tagged human recombinant PARP11 (8 to 338 residues) expressed in Sf9 insect cells by chemiluminescence assay	ic50	0.0670	uM
4-[(8-methyl-4-oxo-7-prop-1-ynyl-3H-quinazolin-2-yl)methylsulfanyl]benzoic acid	1869178: Inhibition of PARP11 (unknown origin)	ic50	0.0990	uM
Talazoparib	2019997: Inhibition of human N-terminal FLAG-tagged/C-terminal His-tagged recombinant PARP11 (8 to 338 (end) residues) expressed in Sf9 cells	ic50	0.1400	uM
8-methyl-2-(pyrimidin-2-ylsulfanylmethyl)-3H-quinazolin-4-one	1853424: Inhibition of N-terminal His-tagged full length human PARP11 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	0.2000	uM
5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965929: Inhibition of N-terminal MBP tagged/C-terminal PARP11 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.2400	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965929: Inhibition of N-terminal MBP tagged/C-terminal PARP11 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.4677	uM
7,8-dimethyl-2-(pyrimidin-2-ylsulfanylmethyl)-3H-quinazolin-4-one	1869178: Inhibition of PARP11 (unknown origin)	ic50	0.5500	uM
5-phenyl-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	1.1749	uM
4-(4-carbamoylphenoxy)benzamide	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	2.0893	uM
5-methyl-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	2.1000	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	2012703: Inhibition of PARP11 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay	ic50	2.1660	uM
4-[[(2S)-1-[3-oxo-3-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propoxy]propan-2-yl]amino]-5-(trifluoromethyl)-1H-pyridazin-6-one	1965305: Inhibition of human recombinant N-terminal GST-tagged / C-terminal His-tagged PARP11 (8 to 338 end residues) expressed in baculovirus infected Sf9 cells expression system incubated for 1 hr by ELISA assay	ic50	2.2810	uM
(2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one	1683873: Inhibition of PARP-11 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay	ic50	2.7000	uM
5-bromo-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	2.8840	uM
6-(1H-indol-5-yl)-5-methyl-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	4.1687	uM
6-(3-methylphenyl)-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	4.5709	uM
6-(3-acetylphenyl)-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	4.8978	uM
6-(3-chlorophenyl)-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	5.7544	uM
6-(3-fluorophenyl)-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	6.0256	uM
Olaparib	2012703: Inhibition of PARP11 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay	ic50	7.8110	uM
3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	7.9433	uM
6-phenyl-3,4-dihydro-2H-isoquinolin-1-one	1515546: Inhibition of full length human His-SUMO-tagged PARP11 expressed in Escherichia coli BL21 assessed as reduction in MARylation of His6-tagged SRPK2 substrate after 60 mins in presence of NAD+ by chemifluorescence assay	ic50	8.7000	uM
[1,2,4]triazolo[3,4-b][1,3]benzothiazol-6-ol	1965929: Inhibition of N-terminal MBP tagged/C-terminal PARP11 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	9.4000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, increases methylation, affects cotreatment, decreases expression, affects expression	7
sodium arsenite	affects expression, affects methylation, increases expression	3
Nickel	increases expression	2
aristolochic acid I	decreases expression	1
methylmercuric chloride	decreases expression	1
triphenyl phosphate	affects expression	1
bisphenol A	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	increases expression	1
butyraldehyde	decreases expression	1
benzo(e)pyrene	decreases methylation	1
methacrylaldehyde	decreases expression, affects cotreatment	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, decreases expression	1
2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazophenyl)amide	affects cotreatment, increases expression	1
dorsomorphin	affects cotreatment, decreases expression	1
bisphenol S	decreases methylation	1
jinfukang	affects cotreatment, decreases expression	1
MT19c compound	increases expression	1
Acrolein	decreases expression, affects cotreatment	1
Air Pollutants	increases abundance, increases expression	1
Arsenic	affects methylation	1
Benzo(a)pyrene	increases methylation	1
Cisplatin	affects cotreatment, decreases expression	1
Lead	affects expression	1
Methapyrilene	decreases methylation	1
Methyl Methanesulfonate	increases expression	1
Ozone	affects cotreatment, decreases expression	1
Phthalic Acids	increases methylation	1
Silicon Dioxide	decreases expression	1
Tetrachlorodibenzodioxin	affects cotreatment, increases expression	1
Cyclosporine	increases expression	1

ChEMBL screening assays

28 unique, capped per target: 28 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2382490	Binding	Inhibition of PARP11 (unknown origin) at 10 uM relative to control	Fragment-based ligand design of novel potent inhibitors of tankyrases. — J Med Chem

Clinical trials (associated diseases)

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