PARP12

Summary

PARP12 (poly(ADP-ribose) polymerase family member 12, HGNC:21919) is a protein-coding gene on chromosome 7q34, encoding Protein mono-ADP-ribosyltransferase PARP12 (Q9H0J9). Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins.

Enables NAD+-protein mono-ADP-ribosyltransferase activity. Involved in protein auto-ADP-ribosylation. Predicted to be active in nucleus.

Source: NCBI Gene 64761 — RefSeq curated summary.

At a glance

• GWAS associations: 8
• Clinical variants (ClinVar): 113 total
• Druggable target: yes — 6 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_022750

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:21919
Approved symbol	PARP12
Name	poly(ADP-ribose) polymerase family member 12
Location	7q34
Locus type	gene with protein product
Status	Approved
Aliases	FLJ22693, PARP-12, ZC3H1, ARTD12
Ensembl gene	ENSG00000059378
Ensembl biotype	protein_coding
OMIM	612481
Entrez	64761

Gene structure

Transcript identifiers

Ensembl transcripts: 21 — 12 protein_coding, 6 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000263549, ENST00000466597, ENST00000467638, ENST00000470515, ENST00000473341, ENST00000484111, ENST00000488726, ENST00000489383, ENST00000489809, ENST00000491598, ENST00000493262, ENST00000496624, ENST00000851631, ENST00000851632, ENST00000851633, ENST00000851634, ENST00000851635, ENST00000851636, ENST00000949000, ENST00000949001, ENST00000949002

RefSeq mRNA: 1 — MANE Select: NM_022750 NM_022750

CCDS: CCDS5857

Canonical transcript exons

ENST00000263549 — 12 exons

Exon	Start	End
ENSE00000726694	140056856	140057153
ENSE00001156094	140062522	140062951
ENSE00001913686	140023749	140024885
ENSE00003467652	140046884	140047007
ENSE00003474942	140054662	140054763
ENSE00003475082	140057899	140058034
ENSE00003495060	140037715	140037856
ENSE00003522848	140034235	140034331
ENSE00003557309	140028613	140028688
ENSE00003633437	140027276	140027406
ENSE00003658972	140041644	140041839
ENSE00003677578	140026197	140026348

Expression profiles

Bgee: expression breadth ubiquitous, 253 present calls, max score 99.37.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 17.5819 / max 451.1032, expressed in 1738 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
86532	17.3261	1735
86530	0.1868	86
86528	0.0513	20
86529	0.0177	9

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	99.37	gold quality
oocyte	CL:0000023	98.50	gold quality
granulocyte	CL:0000094	97.34	gold quality
right lung	UBERON:0002167	95.96	gold quality
upper lobe of left lung	UBERON:0008952	95.87	gold quality
monocyte	CL:0000576	95.70	gold quality
mononuclear cell	CL:0000842	95.60	gold quality
small intestine Peyer’s patch	UBERON:0003454	95.37	gold quality
leukocyte	CL:0000738	95.34	gold quality
upper lobe of lung	UBERON:0008948	95.29	gold quality
spleen	UBERON:0002106	94.37	gold quality
ileal mucosa	UBERON:0000331	94.29	gold quality
mucosa of transverse colon	UBERON:0004991	94.22	gold quality
small intestine	UBERON:0002108	93.90	gold quality
rectum	UBERON:0001052	93.82	gold quality
tibial nerve	UBERON:0001323	93.81	gold quality
pancreatic ductal cell	CL:0002079	93.53	gold quality
right uterine tube	UBERON:0001302	93.31	gold quality
lymph node	UBERON:0000029	93.22	gold quality
metanephros cortex	UBERON:0010533	93.17	gold quality
body of pancreas	UBERON:0001150	93.09	gold quality
ectocervix	UBERON:0012249	92.97	gold quality
vermiform appendix	UBERON:0001154	92.88	gold quality
transverse colon	UBERON:0001157	92.83	gold quality
body of uterus	UBERON:0009853	92.78	gold quality
apex of heart	UBERON:0002098	92.44	gold quality
right coronary artery	UBERON:0001625	92.43	gold quality
duodenum	UBERON:0002114	92.39	gold quality
gall bladder	UBERON:0002110	92.25	gold quality
right ovary	UBERON:0002118	92.15	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	4.53

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): EZH2

miRNA regulators (miRDB)

62 targeting PARP12, 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-548C-3P	99.99	74.01	7587
HSA-MIR-10401-5P	99.99	65.79	948
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-548AA	99.96	70.64	3753
HSA-MIR-548AP-3P	99.96	70.64	3753
HSA-MIR-548T-3P	99.96	70.64	3753
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-548J-3P	99.94	72.61	4881
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-218-5P	99.93	72.22	2103
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-548E-5P	99.89	72.73	4486
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-548AZ-5P	99.83	69.94	3230
HSA-MIR-548T-5P	99.83	69.91	3220
HSA-MIR-1299	99.77	71.24	2389
HSA-MIR-12124	99.68	69.17	2700
HSA-MIR-587	99.64	70.86	2611
HSA-MIR-561-3P	99.64	70.90	3647

Literature-anchored findings (GeneRIF, showing 3)

• FLJ22693, TIPARP and ZAP proteins with TPH, WW and PARP-like domains constitute the TIPARP family. (PMID:12851707)
• PARP12 is a tumor suppressor that plays an important role in HCC metastasis through the regulation of FHL2 stability and TGF-beta1 expression. (PMID:30154409)
• PKD-dependent PARP12-catalyzed mono-ADP-ribosylation of Golgin-97 is required for E-cadherin transport from Golgi to plasma membrane. (PMID:34969853)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	parp12a	ENSDARG00000042496
mus_musculus	Parp12	ENSMUSG00000038507
rattus_norvegicus	Parp12	ENSRNOG00000008196

Paralogs (8): ZC3HAV1 (ENSG00000105939), PARP11 (ENSG00000111224), PARP9 (ENSG00000138496), ZC3HAV1L (ENSG00000146858), TIPARP (ENSG00000163659), PARP14 (ENSG00000173193), PARP15 (ENSG00000173200), PARP10 (ENSG00000178685)

Protein

Protein identifiers

Protein mono-ADP-ribosyltransferase PARP12 — Q9H0J9 (reviewed: Q9H0J9)

Alternative names: ADP-ribosyltransferase diphtheria toxin-like 12, Poly [ADP-ribose] polymerase 12, Zinc finger CCCH domain-containing protein 1

All UniProt accessions (6): Q9H0J9, A4D1T0, G5E9U9, H7C4L8, H7C4T3, H7C4Z9

UniProt curated annotations — full annotation on UniProt →

Function. Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins. Acts as an antiviral factor by cooperating with PARP11 to suppress Zika virus replication. Displays anti-alphavirus activity during IFN-gamma immune activation by directly ADP-ribosylating the alphaviral non-structural proteins nsP3 and nsP4. Acts as a component of the PRKD1-driven regulatory cascade that selectively controls a major branch of the basolateral transport pathway by catalyzing the MARylation of GOLGA1. Acts also as a key regulator of mitochondrial function, protein translation, and inflammation. Inhibits PINK1/Parkin-dependent mitophagy and promotes cartilage degeneration by inhibiting the ubiquitination and SUMOylation of MFN1/2 by upregulating ISG15 and ISGylation.

Subunit / interactions. Interacts with PARP11; this interaction plays a key role in zika virus suppression. Interacts with ISG15.

Subcellular location. Nucleus. Golgi apparatus. trans-Golgi network. Cytoplasm. Stress granule.

Post-translational modifications. Auto-mono-ADP-ribosylated. Phosphorylated by PRKD1.

Similarity. Belongs to the ARTD/PARP family.

RefSeq proteins (1): NP_073587* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000571	Znf_CCCH	Domain
IPR004170	WWE_dom	Domain
IPR012317	Poly(ADP-ribose)pol_cat_dom	Domain
IPR036388	WH-like_DNA-bd_sf	Homologous_superfamily
IPR037197	WWE_dom_sf	Homologous_superfamily
IPR051712	ARTD-AVP	Family
IPR056226	WH_PARP12	Domain
IPR057602	Zfn-CCCH_PARP12	Domain

Pfam: PF00644, PF02825, PF23466, PF24356, PF25261

Catalyzed reactions (Rhea), 2 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)

UniProt features (39 total): strand 10, helix 6, zinc finger region 5, modified residue 4, domain 3, sequence variant 3, mutagenesis site 2, turn 2, chain 1, compositionally biased region 1, sequence conflict 1, region of interest 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
8XPX	X-RAY DIFFRACTION	1.75
6V3W	X-RAY DIFFRACTION	2.04
2PQF	X-RAY DIFFRACTION	2.2

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9H0J9-F1	84.30	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 (4): 258, 474, 600, 611

Mutagenesis-validated functional residues (2):

Position	Phenotype
564	catalytically inactive mutant.
660	catalytically inactive mutant.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 312 (showing top): WALLACE_PROSTATE_CANCER_RACE_UP, GRAESSMANN_APOPTOSIS_BY_SERUM_DEPRIVATION_UP, GRAESSMANN_RESPONSE_TO_MC_AND_SERUM_DEPRIVATION_UP, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_UP, WIELAND_UP_BY_HBV_INFECTION, CAGCTG_AP4_Q5, PATIL_LIVER_CANCER, IRF7_01, GOCC_TRANS_GOLGI_NETWORK, ONKEN_UVEAL_MELANOMA_UP, GOBP_TRANSEPITHELIAL_TRANSPORT, DAUER_STAT3_TARGETS_DN, GOBP_POST_TRANSLATIONAL_PROTEIN_MODIFICATION, IRF_Q6, DODD_NASOPHARYNGEAL_CARCINOMA_UP

GO Biological Process (3): protein auto-ADP-ribosylation (GO:0070213), transepithelial transport (GO:0070633), cell-cell adhesion mediated by cadherin (GO:0044331)

GO Molecular Function (10): RNA binding (GO:0003723), NAD+ poly-ADP-ribosyltransferase activity (GO:0003950), zinc ion binding (GO:0008270), nucleotidyltransferase activity (GO:0016779), NAD+-protein-cysteine ADP-ribosyltransferase activity (GO:0140803), NAD+-protein-aspartate ADP-ribosyltransferase activity (GO:0140806), NAD+-protein mono-ADP-ribosyltransferase activity (GO:1990404), transferase activity (GO:0016740), glycosyltransferase activity (GO:0016757), metal ion binding (GO:0046872)

GO Cellular Component (5): nucleus (GO:0005634), trans-Golgi network (GO:0005802), cytoplasmic stress granule (GO:0010494), cytoplasm (GO:0005737), Golgi apparatus (GO:0005794)

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
pentosyltransferase activity	2
NAD+-protein mono-ADP-ribosyltransferase activity	2
intracellular membrane-bounded organelle	2
post-translational protein modification	1
transport	1
cell-cell adhesion	1
nucleic acid binding	1
transition metal ion binding	1
transferase activity, transferring phosphorus-containing groups	1
catalytic activity, acting on a protein	1
catalytic activity	1
transferase activity	1
cation binding	1
Golgi apparatus subcompartment	1
cytoplasmic ribonucleoprotein granule	1
intracellular anatomical structure	1
cellular anatomical structure	1
cytoplasm	1
endomembrane system	1

Protein interactions and networks

STRING

876 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PARP12	PARP1	P09874	886
PARP12	PARP16	Q8N5Y8	731
PARP12	PARP3	Q9Y6F1	683
PARP12	PARP6	Q2NL67	670
PARP12	PARP4	Q9UKK3	650
PARP12	PARP2	Q9UGN5	641
PARP12	PARP8	Q8N3A8	613
PARP12	PARG	Q86W56	587
PARP12	ZNFX1	Q9P2E3	580
PARP12	ADPRS	Q9NX46	561
PARP12	PARP15	Q460N3	558
PARP12	CMPK2	Q5EBM0	525
PARP12	TNKS	O95271	521
PARP12	MACROD1	Q9BQ69	512
PARP12	IFIH1	Q9BYX4	508

IntAct

14 interactions, top by confidence:

A	B	Type	Score
PARP12	GCLM	psi-mi:“MI:0914”(association)	0.530
PARP12	MLH1	psi-mi:“MI:0915”(physical association)	0.370
Xpo1	IFT56	psi-mi:“MI:0914”(association)	0.350
NUDCD1	TUBAL3	psi-mi:“MI:0914”(association)	0.350
PARP12	PDXK	psi-mi:“MI:0914”(association)	0.350
ENG	IGKV2-28	psi-mi:“MI:0914”(association)	0.350
CUL4B	GGTLC3	psi-mi:“MI:0914”(association)	0.350
CBX2	TRANK1	psi-mi:“MI:0914”(association)	0.350
PARP12	CASC3	psi-mi:“MI:0914”(association)	0.350
BCL6	CACNA1A	psi-mi:“MI:0914”(association)	0.350
ZC3H11A	ESYT2	psi-mi:“MI:2364”(proximity)	0.270
SUMO1	CHD2	psi-mi:“MI:0914”(association)	0.000

BioGRID (61): PARP12 (Affinity Capture-MS), PARP12 (Synthetic Lethality), PARP12 (Affinity Capture-MS), BHLHA15 (Affinity Capture-MS), RNF166 (Affinity Capture-MS), GCLM (Affinity Capture-MS), MKRN2 (Affinity Capture-MS), RNF114 (Affinity Capture-MS), PARP12 (Affinity Capture-RNA), PARP12 (Affinity Capture-MS), PARP12 (Affinity Capture-MS), PARP12 (Affinity Capture-MS), GNB2 (Affinity Capture-MS), PDXK (Affinity Capture-MS), PARP12 (Affinity Capture-MS)

ESM2 similar proteins: A4FVI0, A5PK19, E0CYC6, E9PYK3, F1QWK4, G5E8F4, O55239, P0C5J1, P40261, P85118, P98192, Q06AV1, Q09M05, Q14164, Q14CH1, Q5I0I5, Q5PPG7, Q5R699, Q5RFM7, Q5XG58, Q61211, Q6PZ05, Q7ZU92, Q8BML1, Q8BQJ6, Q8BZ20, Q8CHQ9, Q8IYR2, Q8N6R0, Q8N7N1, Q8WYN0, Q91W78, Q91YR5, Q96GJ1, Q96MI9, Q9CWQ2, Q9H0J9, Q9JIY6, Q9JIY7, Q9JIZ0

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

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	82
Likely benign	6
Benign	3

Top pathogenic / likely-pathogenic (0)

SpliceAI

2117 predictions. Top by Δscore:

Variant	Effect	Δscore
7:140026191:CCTTA:C	donor_loss	1.0000
7:140026194:TA:T	donor_loss	1.0000
7:140026195:A:AC	donor_gain	1.0000
7:140026195:AC:A	donor_gain	1.0000
7:140026196:C:CC	donor_gain	1.0000
7:140026196:C:CT	donor_loss	1.0000
7:140026196:CC:C	donor_gain	1.0000
7:140026201:G:A	donor_gain	1.0000
7:140026344:TTTGC:T	acceptor_gain	1.0000
7:140026345:TTGC:T	acceptor_gain	1.0000
7:140026346:TGC:T	acceptor_gain	1.0000
7:140026346:TGCC:T	acceptor_loss	1.0000
7:140026347:GC:G	acceptor_gain	1.0000
7:140026348:CC:C	acceptor_gain	1.0000
7:140026349:C:CC	acceptor_gain	1.0000
7:140026349:CTAGA:C	acceptor_loss	1.0000
7:140027275:CCA:C	donor_gain	1.0000
7:140027288:T:TA	donor_gain	1.0000
7:140027289:C:A	donor_gain	1.0000
7:140034330:GG:G	acceptor_gain	1.0000
7:140034332:C:CC	acceptor_gain	1.0000
7:140024882:CTCC:C	acceptor_gain	0.9900
7:140024884:CC:C	acceptor_gain	0.9900
7:140024885:CC:C	acceptor_gain	0.9900
7:140024885:CCT:C	acceptor_loss	0.9900
7:140024886:C:CC	acceptor_gain	0.9900
7:140026195:ACC:A	donor_gain	0.9900
7:140026196:CCC:C	donor_gain	0.9900
7:140026356:C:CT	acceptor_gain	0.9900
7:140027404:CTT:C	acceptor_gain	0.9900

AlphaMissense

4629 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
7:140024813:A:G	F618S	0.998
7:140026202:C:T	G592D	0.998
7:140034284:G:T	R458S	0.998
7:140041754:G:T	R358S	0.998
7:140046967:C:A	W301C	0.998
7:140046967:C:G	W301C	0.998
7:140046969:A:G	W301R	0.998
7:140046969:A:T	W301R	0.998
7:140046971:C:G	R300P	0.998
7:140024716:G:C	S650R	0.997
7:140024716:G:T	S650R	0.997
7:140024718:T:G	S650R	0.997
7:140024864:G:T	A601D	0.997
7:140026197:C:G	G594R	0.997
7:140026197:C:T	G594R	0.997
7:140026202:C:A	G592V	0.997
7:140026232:C:G	R582P	0.997
7:140027312:C:G	R531P	0.997
7:140041756:C:G	R357P	0.997
7:140054698:A:G	C276R	0.997
7:140024658:A:C	Y670D	0.996
7:140024674:A:C	F664L	0.996
7:140024674:A:T	F664L	0.996
7:140024676:A:G	F664L	0.996
7:140024885:C:T	G594E	0.996
7:140026197:C:A	G594W	0.996
7:140026287:G:C	H564D	0.996
7:140026288:G:C	F563L	0.996
7:140026288:G:T	F563L	0.996
7:140026289:A:G	F563S	0.996

dbSNP variants (sampled 300 via entrez): RS1000224259 (7:140027177 C>A,T), RS1000255674 (7:140045859 T>C), RS1000360009 (7:140060998 A>C), RS1000480471 (7:140040545 T>A), RS1000524017 (7:140063117 G>A), RS1000685817 (7:140057669 A>C), RS1000715417 (7:140051225 T>G), RS1000852550 (7:140040323 G>A), RS1000940050 (7:140063385 A>G), RS1000950293 (7:140035999 G>A), RS1000959501 (7:140024686 G>C,T), RS1000973906 (7:140038292 C>A,T), RS1000996762 (7:140030131 A>C,G), RS1001199508 (7:140051394 T>C), RS1001210194 (7:140029185 T>C)

Disease associations

OMIM: gene MIM:612481 | 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
GCST004785_34	Vitiligo	1.000000e-07
GCST005195_25	Coronary artery disease	7.000000e-09
GCST005196_153	Coronary artery disease	9.000000e-11
GCST010479_7	Coronary artery disease	1.000000e-08
GCST011362_3	Mental health related quality of life	4.000000e-07
GCST011365_71	Myocardial infarction	2.000000e-10
GCST90000025_313	Appendicular lean mass	5.000000e-27
GCST90020028_284	Hip circumference adjusted for BMI	3.000000e-09

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0011014	health-related quality of life measurement
EFO:0004980	appendicular lean mass
EFO:0008039	BMI-adjusted hip circumference

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2429709 (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: 34,261 (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
CHEMBL4112930	PAMIPARIB	3	2,114
CHEMBL506871	VELIPARIB	3	5,421
CHEMBL5095043	ATAMPARIB	1	246

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

ChEMBL bioactivities

24 potent at pChembl≥5 of 29 total, top 24 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.85	IC50	14.1	nM	CHEMBL5402698
7.60	IC50	25	nM	ATAMPARIB
7.58	IC50	26	nM	ATAMPARIB
7.10	IC50	79	nM	NIRAPARIB
6.80	IC50	160	nM	CHEMBL5404785
6.80	IC50	158.5	nM	CHEMBL5404785
6.65	IC50	223.9	nM	PJ34
6.64	IC50	230	nM	PJ34
6.44	IC50	360	nM	CHEMBL5639789
6.43	IC50	371	nM	CHEMBL5176874
6.34	IC50	453	nM	CHEMBL5395820
6.18	IC50	664	nM	CHEMBL5571636
6.16	IC50	690	nM	OLAPARIB
6.10	IC50	794.3	nM	NIRAPARIB
5.93	IC50	1163	nM	OLAPARIB
5.91	IC50	1244	nM	OLAPARIB
5.90	IC50	1253	nM	CHEMBL6170737
5.62	IC50	2400	nM	PAMIPARIB
5.58	IC50	2600	nM	CHEMBL5199558
5.36	IC50	4400	nM	CHEMBL5431108
5.18	IC50	6650	nM	RUCAPARIB
5.18	IC50	6607	nM	RUCAPARIB
5.09	IC50	8200	nM	CHEMBL4089522
5.00	IC50	1.005e+04	nM	OLAPARIB

PubChem BioAssay actives

21 with measured affinity, of 80 total; 15 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
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	2012704: Inhibition of PARP12 (unknown origin) using biotinylated NAD+ as substrate by luminescence assay	ic50	0.0141	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	2096821: Inhibition of PARP12 (unknown origin) by probe displacement assay	ic50	0.0250	uM
Niraparib	1428396: Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.0790	uM
5,8-dimethoxy-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965930: Inhibition of N-terminal MBP tagged/C-terminal PARP12 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	0.1585	uM
2-(dimethylamino)-N-(6-oxo-5H-phenanthridin-2-yl)acetamide	1428396: Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	0.2239	uM
4-[(2S)-2-[[3-oxo-3-[(10S)-5-(trifluoromethyl)-8-oxa-1,3,12-triazatricyclo[8.4.0.02,7]tetradeca-2(7),3,5-trien-12-yl]propoxy]methyl]azetidin-1-yl]-5-(trifluoromethyl)-1H-pyridazin-6-one	2142438: Inhibition of PARP12 (unknown origin)	ic50	0.3600	uM
4-[2-fluoro-5-[(4-oxo-3H-phthalazin-1-yl)methyl]benzoyl]-N-[4-[(4-methoxyphenyl)carbamoyl]phenyl]piperazine-1-carboxamide	1868364: Inhibition of PARP-12 (unknown origin)	ic50	0.3710	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	1965306: Inhibition of human recombinant N-terminal GST-tagged PARP12 (500 to 701 end residues) expressed in baculovirus infected Sf9 cells expression system incubated for 1 hr by ELISA assay	ic50	0.4530	uM
2-[(2S)-1-oxo-1-[4-[5-(trifluoromethyl)pyrimidin-2-yl]piperazin-1-yl]propan-2-yl]indazole-7-carboxamide	2096832: Inhibition of PARP12 (unknown origin) measured after 1 hr incubation by microplate reader assay	ic50	0.6640	uM
Olaparib	2019998: Inhibition of human N-terminal FLAG/His-tagged recombinant PARP12 (500 to 701(end) residues) expressed in Sf9 cells	ic50	0.6900	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	1683872: Inhibition of PARP-12 (unknown origin) pre-incubated for 30 mins before addition of activated DNA and NAD by chemiluminescent assay	ic50	2.4000	uM
3-[4-(2-hydroxypropan-2-yl)phenyl]-6-methyl-2H-pyrrolo[1,2-a]pyrazin-1-one	1925213: Inhibition of human PARP12 by chemiluminescence assay	ic50	2.6000	uM
6-methyl-[1,2,4]triazolo[3,4-b][1,3]benzothiazol-1-amine	1965930: Inhibition of N-terminal MBP tagged/C-terminal PARP12 (unknown origin) expressed in Escherichia coli in presence of NAD+ by proximity enhanced assay	ic50	4.4000	uM
Rucaparib	1428396: Inhibition of recombinant human His6-tagged PARP12 ADP-ribosyltransferase domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	6.6069	uM
3-[[(Z)-4-[4-(4-fluorophenyl)piperazin-1-yl]-4-oxobut-2-enoyl]amino]benzamide	1467142: Inhibition of His6-tagged PARP12 (unknown origin) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay	ic50	8.2000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
sodium arsenite	affects methylation, decreases expression, increases abundance	3
Acetaminophen	decreases expression, increases expression	3
Cyclosporine	decreases expression, increases expression	3
entinostat	increases expression, affects cotreatment	2
Arsenic	decreases expression, increases abundance, affects methylation	2
Benzo(a)pyrene	decreases expression, decreases methylation	2
Nickel	increases expression	2
SBI-797812	increases activity	1
potassium perchlorate	decreases expression	1
cobaltous chloride	decreases expression	1
ochratoxin A	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
perfluoro-n-nonanoic acid	increases expression	1
2-palmitoylglycerol	increases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	increases expression, affects cotreatment	1
ICG 001	increases expression	1
abrine	decreases expression	1
dorsomorphin	affects cotreatment, increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Temozolomide	increases expression	1
Sunitinib	increases expression	1
Ethanol	increases expression	1
Caffeine	affects phosphorylation	1
Succimer	affects cotreatment, increases expression	1
Doxorubicin	decreases expression	1
Estradiol	increases expression	1
Phthalic Acids	decreases methylation	1
Plant Extracts	affects cotreatment, increases expression	1
Quercetin	decreases expression	1

ChEMBL screening assays

36 unique, capped per target: 36 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2433126	Binding	Inhibition of human ARTD12 (489 to 684) using NAD+ as substrate at 1 uM by fluorescence assay	Discovery of tankyrase inhibiting flavones with increased potency and isoenzyme selectivity. — J Med Chem

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B1GV	Abcam A-549 PARP12 KO	Cancer cell line	Male
CVCL_TC13	HAP1 PARP12 (-) 1	Cancer cell line	Male
CVCL_XR35	HAP1 PARP12 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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