ATAD2

Summary

ATAD2 (ATPase family AAA domain containing 2, HGNC:30123) is a protein-coding gene on chromosome 8q24.13, encoding ATPase family AAA domain-containing protein 2 (Q6PL18). May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1.

A large family of ATPases has been described, whose key feature is that they share a conserved region of about 220 amino acids that contains an ATP-binding site. The proteins that belong to this family either contain one or two AAA (ATPases Associated with diverse cellular Activities) domains. AAA family proteins often perform chaperone-like functions that assist in the assembly, operation, or disassembly of protein complexes. The protein encoded by this gene contains two AAA domains, as well as a bromodomain.

Source: NCBI Gene 29028 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 184 total — 1 pathogenic
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_014109

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:30123
Approved symbol	ATAD2
Name	ATPase family AAA domain containing 2
Location	8q24.13
Locus type	gene with protein product
Status	Approved
Aliases	PRO2000, DKFZp667N1320, MGC5254, MGC29843, CT137, ANCCA
Ensembl gene	ENSG00000156802
Ensembl biotype	protein_coding
OMIM	611941
Entrez	29028

Gene structure

Transcript identifiers

Ensembl transcripts: 12 — 6 protein_coding, 3 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000287394, ENST00000517666, ENST00000519124, ENST00000521496, ENST00000521903, ENST00000530065, ENST00000534257, ENST00000550993, ENST00000915699, ENST00000915700, ENST00000915701, ENST00000962834

RefSeq mRNA: 1 — MANE Select: NM_014109 NM_014109

CCDS: CCDS6343

Canonical transcript exons

ENST00000287394 — 28 exons

Exon	Start	End
ENSE00002295382	123396187	123396447
ENSE00003465900	123371236	123371338
ENSE00003478796	123359221	123359336
ENSE00003479808	123369821	123370024
ENSE00003491560	123337625	123337821
ENSE00003494749	123361539	123361646
ENSE00003499891	123344884	123345069
ENSE00003504946	123336373	123336532
ENSE00003521496	123328190	123328579
ENSE00003541945	123347092	123347406
ENSE00003545241	123346086	123346272
ENSE00003551974	123334200	123334322
ENSE00003553123	123339311	123339446
ENSE00003561401	123322938	123323066
ENSE00003575493	123370903	123370990
ENSE00003577345	123369058	123369175
ENSE00003578782	123357562	123357736
ENSE00003586041	123380529	123380677
ENSE00003603575	123356389	123356477
ENSE00003603685	123372637	123372686
ENSE00003638100	123371670	123371835
ENSE00003643910	123319850	123321175
ENSE00003646054	123349285	123349444
ENSE00003658696	123348183	123348273
ENSE00003664008	123333878	123334021
ENSE00003664869	123359577	123359685
ENSE00003667314	123346618	123346750
ENSE00003677374	123325893	123326026

Expression profiles

Bgee: expression breadth ubiquitous, 224 present calls, max score 98.66.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 41.1554 / max 1010.6690, expressed in 1789 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
94722	37.1575	1763
94721	3.3586	990
94724	0.6393	342

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
secondary oocyte	CL:0000655	98.66	gold quality
ventricular zone	UBERON:0003053	95.89	gold quality
oocyte	CL:0000023	95.77	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	92.59	gold quality
ganglionic eminence	UBERON:0004023	91.36	gold quality
bone marrow	UBERON:0002371	88.20	gold quality
esophagus squamous epithelium	UBERON:0006920	87.79	gold quality
amniotic fluid	UBERON:0000173	87.43	gold quality
trabecular bone tissue	UBERON:0002483	87.42	gold quality
sperm	CL:0000019	87.30	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	87.30	gold quality
embryo	UBERON:0000922	86.96	gold quality
male germ cell	CL:0000015	84.74	gold quality
adrenal tissue	UBERON:0018303	84.59	gold quality
tendon of biceps brachii	UBERON:0008188	84.50	silver quality
bone marrow cell	CL:0002092	83.83	gold quality
testis	UBERON:0000473	83.62	gold quality
right testis	UBERON:0004534	83.09	gold quality
germinal epithelium of ovary	UBERON:0001304	82.49	gold quality
left testis	UBERON:0004533	81.96	gold quality
tonsil	UBERON:0002372	81.79	gold quality
tibia	UBERON:0000979	81.67	gold quality
epithelium of esophagus	UBERON:0001976	81.62	gold quality
mucosa of paranasal sinus	UBERON:0005030	81.41	silver quality
stromal cell of endometrium	CL:0002255	81.14	gold quality
tendon	UBERON:0000043	80.66	gold quality
gingival epithelium	UBERON:0001949	80.65	silver quality
lymph node	UBERON:0000029	80.08	gold quality
calcaneal tendon	UBERON:0003701	79.94	gold quality
rectum	UBERON:0001052	79.76	gold quality

Single-cell (SCXA)

Detected in 9 experiment(s), a significant marker in 8.

Experiment	Marker?	Max mean expression
E-MTAB-8559	yes	690.85
E-MTAB-11268	yes	483.27
E-GEOD-81383	yes	428.42
E-MTAB-6075	yes	353.21
E-MTAB-10290	yes	208.07
E-CURD-122	yes	24.13
E-CURD-46	yes	15.82
E-ANND-3	yes	6.49
E-MTAB-6678	no	3.54

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AR, E2F1, NCOA3

miRNA regulators (miRDB)

140 targeting ATAD2, 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-3163	100.00	77.23	8605
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-4476	100.00	68.18	2030
HSA-MIR-6876-5P	100.00	67.68	2126
HSA-MIR-8485	100.00	77.57	4731
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-3646	100.00	73.56	5283
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-371B-5P	99.99	75.34	4759
HSA-MIR-3662	99.99	73.82	5684
HSA-MIR-548AW	99.99	72.57	3559
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-373-5P	99.98	75.36	4753
HSA-MIR-616-5P	99.98	75.58	4775
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-302E	99.96	70.74	2669
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-570-3P	99.96	72.41	4910
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-559	99.95	72.28	3609

Literature-anchored findings (GeneRIF, showing 40)

• ANCCA associates directly with ERalpha and ACTR. It is selectively recruited to a subset of ERalpha target genes (cyclin D1, c-myc, and E2F1) and is required for their estrogen-induced expression and breast cancer cell proliferation. (PMID:17998543)
• ANCCA interacts with AR, required for IGF1R,IRS-2,SGK1, survivin expression and proliferation and survival of prostate cancer cells. ANCCA itself is highly induced by androgen. Its overexpression is found in prostate cancers with high Gleason scores. (PMID:19318566)
• Findings suggest that ANCCA plays an important role in prostate cancer by mediating specific AR functions in cancer cell survival and proliferation. (PMID:19318566)
• ATAD2 is a novel cofactor for MYC, overexpressed and amplified in aggressive tumors. (PMID:19843847)
• Genetic aberrations and dysregulation in expression of p160/SRC coactivators and the ANCCA in breast cancer, prostate cancer, and other nonhormone-responsive cancers, are reviewed. (PMID:20374707)
• Data report that ANCCA directly interacts with E2F1 to E2F3 in its complex with MLL and that its N terminus interacts with both the N and C termini of E2F1. (PMID:20855524)
• Data show that that ANCCA is crucial for proliferation and survival of triple-negative/basal-like cancer cells and that it controls the expression of B-Myb and histone methyltransferase EZH2. (PMID:20864510)
• Data conclude that AR and E2F1 cooperation results from a chromatin looping over the ATAD2 promoter region between the ARBS and E2F1 binding site in an androgen-dependent manner (PMID:22771493)
• However, only ATAD2, and not MYC, overexpression explained the behavior of proliferation-related genes and predicted a worse prognosis independently of disease stage in a large validation cohort (PMID:22914773)
• Data indicate high ATAD2 expression is a marker of aggressive endometrial cancers, and suggest specific inhibitors of ATAD2 may have therapeutic utility in these and other MYC-dependent cancers. (PMID:23393560)
• High ANCCA protein expression is associated with lymphatic metastasis in lung adenocarcinoma. (PMID:23775406)
• Study reveals ANCCA as a key mediator of kinesin family deregulation in breast cancer and the crucial role of multiple kinesins in growth and survival of the tumor cells. (PMID:24391143)
• miR-372 suppressed the expression of ATAD2, which was highly expressed in HCC and exerted a proto-oncogene effect in hepatic carcinogenesis. (PMID:24552534)
• High expression of ATAD2 is associated with ovarian carcinomas (PMID:24761900)
• Data highlight the implication of Yta7 not only in gene expression, as expected, but also in genome organization, as a possible histone chaperone acting at boundary sites and regulating transcription. [review] (PMID:25377252)
• ATAD2 protein expression may be a potential predictor of recurrence-free survival in hepatocellular carcinoma (HCC) patients after curative resection and ATAD2 may have prognostic value in patients with early stage HCC or normal serum alpha-fetoprotein level. (PMID:25687855)
• Cervical cancer tissues may have highly expressed ATAD2. Oncogene ATAD2 may play an important role in cervical cancer proliferation, invasion and migration. (PMID:25813398)
• We identified ANCCA protein expression as a novel independent poor prognostic indicator in endometrial carcinoma (PMID:25934333)
• Data indicate that gene expression alterations in endometrial carcinoma samples with high ATPase family, AAA domain containing 2 protein (ATAD2) expression showed upregulation of several cancer-related genes including B-MYB gene. (PMID:26308378)
• this work defines Atad2 as a facilitator of general chromatin-templated activities such as transcription. (PMID:26459632)
• Suppression of ATAD2 impaired the growth of HepG2 and Hep3B subcutaneous xenografts, by enhancing apoptosis and p-p53 and p-p38 levels. (PMID:26497681)
• ATAD2 protein overexpression was a poor independent prognostic factor for gastric cancer patients (PMID:26527032)
• Results showed that ATPase family AAA domain-containing 2 overexpression was associated with progression and prognosis of colorectal cancer. (PMID:26819280)
• ANCCA act as a potential biomarker for therapeutic strategy and prognostic prediction for squamous cell lung carcinoma. (PMID:27131099)
• esults suggest that silencing of ATAD2 inhibits migration and invasion of colorectal cancer cells by suppressing epithelial-mesenchymal transition and decreasing the activity of MMPs (PMID:27565322)
• a novel function of ATAD2 in cancer and for the first time identify a reader of newly synthesized histone di-acetylation-marks during replication. (PMID:27612420)
• Results show that ATAD2 expression is regulated by PCAT-14 which activates Hedgehog pathway in hepatocellular carcinoma cells, depending on miR-372. (PMID:28415780)
• BRDs are overexpressed in castration-resistant prostate cancer and that ATAD2 and BRD2 have prognostic value. (PMID:28591577)
• ATAD2 may play an important role in HCC tumorigenesis, and may be involved in malignant transformation of cells. ATAD2 expression can be a valuable marker for differentiating the nature of lesions in liver biopsy tissues during clinical practice. (PMID:28763839)
• the simulations indicate that disorder and electrostatic steering function jointly to recruit ATAD2A to the histone core and that these fuzzy interactions may promote cooperativity between nearby epigenetic marks. (PMID:28798233)
• The ATAD2 as a potential therapeutic target for angiogenesis in colorectal cancer. (PMID:29958090)
• Molecular dynamics simulations indicate that the formation of the disulfide bridge in the ATPase family, AAA domain-containing protein 2 (ATAD2) bromodomain does not alter the structure of the folded state or flexibility of the acetyllysine binding pocket. (PMID:30520161)
• Elevated PLK4 expression was observed in high grade glioblastoma (GBM) patients and was associated with poor prognosis. PLK4 expression was markedly elevated by the exogenous overexpression of ATAD2 in GBM cells. Results suggested that the ATAD2dependent transcriptional regulation of PLK4 promoted cell proliferation and tumorigenesis. (PMID:30816483)
• Overexpression of miR-186 attenuates retinoblastoma via the inactivation of the Hedgehog signaling pathway by downregulating ATAD2. (PMID:30993715)
• correlation between ATAD2 expression and glycometabolism in cancers (PMID:31186081)
• Kinesin family member 15 promotes cancer stem cell phenotype and malignancy via reactive oxygen species imbalance in hepatocellular carcinoma. (PMID:31733289)
• ATAD2 predicts poor outcomes in patients with ovarian cancer and is a marker of proliferation. (PMID:31746426)
• Data reported for the first time that the expression of ANCCA was highly induced by DNAdamaging chemotherapy agents such as carboplatin, doxorubicin and mitomycin C, as well as ionizing radiation. Its knockdown sensitizes triplenegative breast cancer cells to carboplatin. (PMID:31789405)
• HIF1alpha-dependent upregulation of ATAD2 promotes proliferation and migration of stomach cancer cells in response to hypoxia. (PMID:31959473)
• Mutual Balance of Histone Deacetylases 1 and 2 and the Acetyl Reader ATAD2 Regulates the Level of Acetylation of Histone H4 on Nascent Chromatin of Human Cells. (PMID:32015101)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
danio_rerio	atad2	ENSDARG00000076590
mus_musculus	Atad2	ENSMUSG00000022360
caenorhabditis_elegans		WBGENE00008682

Paralogs (1): ATAD2B (ENSG00000119778)

Protein

Protein identifiers

ATPase family AAA domain-containing protein 2 — Q6PL18 (reviewed: Q6PL18)

Alternative names: AAA nuclear coregulator cancer-associated protein

All UniProt accessions (4): Q6PL18, A0A0B4J211, E5RHW7, E5RIP2

UniProt curated annotations — full annotation on UniProt →

Function. May be a transcriptional coactivator of the nuclear receptor ESR1 required to induce the expression of a subset of estradiol target genes, such as CCND1, MYC and E2F1. May play a role in the recruitment or occupancy of CREBBP at some ESR1 target gene promoters. May be required for histone hyperacetylation. Involved in the estrogen-induced cell proliferation and cell cycle progression of breast cancer cells.

Subunit / interactions. Interacts with ESR1 and NCOA3 and these interactions are enhanced by estradiol. Interacts with acetylated lysine residues on histone H1.4, H2A, H2B and H3 (in vitro).

Subcellular location. Nucleus.

Tissue specificity. Highly expressed in estrogen receptor positive breast tumors and in osteosarcoma tumors.

Induction. Up-regulated in breast, uterus, colon, ovary, and stomach tumors. Induced in breast cancer cells overexpressing NCOA3 or treated with estrogen. Down-regulated in 5-fluorouracil-resistant derivatives of the colon cancer cell line HCT 116.

Miscellaneous. Dubious isoform. 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 AAA ATPase family.

Isoforms (2)

UniProt ID	Names	Canonical?
Q6PL18-1	1	yes
Q6PL18-2	2

RefSeq proteins (1): NP_054828* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001487	Bromodomain	Domain
IPR003593	AAA+_ATPase	Domain
IPR003959	ATPase_AAA_core	Domain
IPR003960	ATPase_AAA_CS	Conserved_site
IPR027417	P-loop_NTPase	Homologous_superfamily
IPR036427	Bromodomain-like_sf	Homologous_superfamily
IPR041569	AAA_lid_3	Domain
IPR045199	ATAD2-like	Family

Pfam: PF00004, PF00439, PF17862

Catalyzed reactions (Rhea), 1 shown:

• ATP + H2O = ADP + phosphate + H(+) (RHEA:13065)

UniProt features (107 total): helix 35, modified residue 20, strand 14, turn 11, compositionally biased region 7, cross-link 5, region of interest 4, splice variant 3, mutagenesis site 2, coiled-coil region 2, chain 1, domain 1, binding site 1, sequence variant 1

Structure

Experimental structures (PDB)

120 structures, top 30 by resolution.

PDB	Method	Resolution (Å)
5R4V	X-RAY DIFFRACTION	1.29
7Z9H	X-RAY DIFFRACTION	1.34
7Z9N	X-RAY DIFFRACTION	1.34
7PPX	X-RAY DIFFRACTION	1.35
8RU5	X-RAY DIFFRACTION	1.36
5R4X	X-RAY DIFFRACTION	1.4
5QXN	X-RAY DIFFRACTION	1.41
5QXP	X-RAY DIFFRACTION	1.41
7QYK	X-RAY DIFFRACTION	1.43
7R0Y	X-RAY DIFFRACTION	1.43
5R4F	X-RAY DIFFRACTION	1.44
7QYL	X-RAY DIFFRACTION	1.44
7QZM	X-RAY DIFFRACTION	1.45
5QXJ	X-RAY DIFFRACTION	1.46
5R4Z	X-RAY DIFFRACTION	1.46
5QXO	X-RAY DIFFRACTION	1.47
5R4W	X-RAY DIFFRACTION	1.47
7QUK	X-RAY DIFFRACTION	1.47
7Z9O	X-RAY DIFFRACTION	1.47
7R00	X-RAY DIFFRACTION	1.48
7QX1	X-RAY DIFFRACTION	1.49
5EPB	X-RAY DIFFRACTION	1.5
5F36	X-RAY DIFFRACTION	1.5
5QXM	X-RAY DIFFRACTION	1.5
7QUM	X-RAY DIFFRACTION	1.5
7QWO	X-RAY DIFFRACTION	1.5
7Z9I	X-RAY DIFFRACTION	1.5
7Z9S	X-RAY DIFFRACTION	1.5
7QXT	X-RAY DIFFRACTION	1.51
7R05	X-RAY DIFFRACTION	1.53

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q6PL18-F1	61.63	0.12

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 (1): 467–474

Post-translational modifications (25): 60, 61, 165, 170, 327, 337, 342, 410, 746, 751, 1139, 1149, 1152, 1176, 1200, 1233, 1235, 1243, 1302, 1323 …

Mutagenesis-validated functional residues (2):

Position	Phenotype
473	reduces the ability to mediate estradiol-dependent induction of ccnd1 and e2f1; when associated with q-532.
532	reduces the ability to mediate estradiol-dependent induction of ccnd1 and e2f1; when associated with t-473.

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-8866910	TFAP2 (AP-2) family regulates transcription of growth factors and their receptors
R-HSA-212436	Generic Transcription Pathway
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)
R-HSA-8864260	Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors

MSigDB gene sets: 320 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_DN, GSE45365_CTRL_VS_MCMV_INFECTION_NK_CELL_DN, E2F_Q4, WU_APOPTOSIS_BY_CDKN1A_VIA_TP53, E2F_Q4_01, RODRIGUES_THYROID_CARCINOMA_ANAPLASTIC_UP, KANG_DOXORUBICIN_RESISTANCE_UP, RODRIGUES_THYROID_CARCINOMA_POORLY_DIFFERENTIATED_UP, E2F4DP1_01, FISCHER_G1_S_CELL_CYCLE, TGACCTY_ERR1_Q2, PATIL_LIVER_CANCER, WEI_MYCN_TARGETS_WITH_E_BOX, CEBP_Q2, E2F1DP1_01

GO Biological Process (4): nucleosome assembly (GO:0006334), nucleosome disassembly (GO:0006337), transcription initiation-coupled chromatin remodeling (GO:0045815), positive regulation of DNA-templated transcription (GO:0045893)

GO Molecular Function (7): chromatin binding (GO:0003682), ATP binding (GO:0005524), ATP hydrolysis activity (GO:0016887), histone binding (GO:0042393), nucleotide binding (GO:0000166), protein binding (GO:0005515), hydrolase activity (GO:0016787)

GO Cellular Component (3): nucleus (GO:0005634), nucleoplasm (GO:0005654), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-4 pathways:

Category	Pathways
Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors	1
RNA Polymerase II Transcription	1
Gene expression (Transcription)	1
Generic Transcription Pathway	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
nucleosome organization	2
binding	2
chromatin organization	1
protein-DNA complex assembly	1
protein-DNA complex disassembly	1
transcription initiation at RNA polymerase II promoter	1
positive regulation of gene expression, epigenetic	1
DNA-templated transcription	1
regulation of DNA-templated transcription	1
positive regulation of RNA biosynthetic process	1
adenyl ribonucleotide binding	1
purine ribonucleoside triphosphate binding	1
ribonucleoside triphosphate phosphatase activity	1
ATP-dependent activity	1
protein binding	1
nucleoside phosphate binding	1
heterocyclic compound binding	1
catalytic activity	1
intracellular membrane-bounded organelle	1
nuclear lumen	1
cellular anatomical structure	1
extracellular vesicle	1

Protein interactions and networks

STRING

2986 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
ATAD2	ESR1	P03372	699
ATAD2	BRD4	O60885	682
ATAD2	NCOA3	Q9Y6Q9	672
ATAD2	E2F1	Q01094	608
ATAD2	AR	P10275	585
ATAD2	TOP2A	P11388	584
ATAD2	NTAQ1	Q96HA8	564
ATAD2	AURKA	O14965	561
ATAD2	H4C16	P02304	554
ATAD2	H4C7	Q99525	554
ATAD2	CDC6	Q99741	547
ATAD2	MYC	P01106	546
ATAD2	TPX2	Q9ULW0	546
ATAD2	CDCA7	Q9BWT1	529
ATAD2	H3-3A	P06351	519

IntAct

53 interactions, top by confidence:

A	B	Type	Score
ATAD2	ESR1	psi-mi:“MI:0915”(physical association)	0.740
ATAD2	ESR1	psi-mi:“MI:0407”(direct interaction)	0.740
ESR1	ATAD2	psi-mi:“MI:0915”(physical association)	0.740
CFTR	ESYT2	psi-mi:“MI:2364”(proximity)	0.710
CSNK2B	NMT2	psi-mi:“MI:0914”(association)	0.660
ASF1B	HAT1	psi-mi:“MI:0914”(association)	0.640
CYCS	FAAP100	psi-mi:“MI:0914”(association)	0.530
DAXX	TNRC18	psi-mi:“MI:0914”(association)	0.530
HDGFL2	CDC7	psi-mi:“MI:0914”(association)	0.530
TTC23L	EFCAB7	psi-mi:“MI:0914”(association)	0.530
ATAD2	NCOA3	psi-mi:“MI:0915”(physical association)	0.520
DDX21	MED19	psi-mi:“MI:2364”(proximity)	0.480
H3C1	SMCHD1	psi-mi:“MI:2364”(proximity)	0.410
ATAD2	SPTBN2	psi-mi:“MI:0915”(physical association)	0.400
ATAD2	BAG4	psi-mi:“MI:0915”(physical association)	0.370
BCAR3	ATAD2	psi-mi:“MI:0915”(physical association)	0.370
ATAD2	CASP8	psi-mi:“MI:0915”(physical association)	0.370
Naa50	WDR46	psi-mi:“MI:0914”(association)	0.350
Mecom	ESYT2	psi-mi:“MI:0914”(association)	0.350
ESR1	ESYT2	psi-mi:“MI:0914”(association)	0.350
CSNK2A1	RPS3A	psi-mi:“MI:0914”(association)	0.350
CSNK2B	OSBPL8	psi-mi:“MI:0914”(association)	0.350
H2BC21	SMCHD1	psi-mi:“MI:0914”(association)	0.350
HMGN5	SMCHD1	psi-mi:“MI:0914”(association)	0.350
NUMA1	SHANK3	psi-mi:“MI:0914”(association)	0.350

BioGRID (80): ATAD2 (Affinity Capture-RNA), ATAD2 (Co-fractionation), ATAD2 (Affinity Capture-MS), ATAD2 (Two-hybrid), ATAD2 (Two-hybrid), ATAD2 (Two-hybrid), ATAD2 (Two-hybrid), ATAD2 (Proximity Label-MS), ATAD2 (Proximity Label-MS), SPTBN2 (Affinity Capture-MS), ATAD2 (Affinity Capture-MS), ATAD2 (Affinity Capture-RNA), ATAD2 (Affinity Capture-MS), ATAD2 (Affinity Capture-MS), ATAD2 (Affinity Capture-MS)

ESM2 similar proteins: A0A0G2JZ79, A1ZA92, A6QQR4, A7E2Z2, A8JQ65, A8WRG3, B3NYS4, B4K6T8, B4R0A5, B6VQ60, F4JZ68, O75164, O94640, P06700, P33294, P42124, P50526, P70351, Q04688, Q08BS4, Q14149, Q15910, Q21921, Q28D84, Q28Z18, Q2NKX8, Q4R381, Q4V863, Q5RD88, Q5RDS6, Q5RDX4, Q60L58, Q61188, Q61IS6, Q640I9, Q6DTM3, Q6PL18, Q757M7, Q8CDM1, Q8K3E5

Diamond homologs: A0A0R4IXF6, A0A7U2QYM2, A2AHJ4, A2AUY4, A2BIL7, B2RRD7, B7ZS37, D4A7T3, E9Q2Z1, F1QW93, F1R5H6, F7DRV9, G5E8P1, O15164, O60885, O74350, O88379, O88665, O95696, P13709, P21675, P25440, P35817, P51123, P53236, P54816, P55201, P87152, Q02206, Q03330, Q07442, Q08D75, Q09948, Q12830, Q15059, Q1LUC3, Q23590, Q32S26, Q338B9, Q4R8Y1

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 67 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

GO biological processes:

GO term	Partners	Fold	FDR
nucleosome assembly	7	16.1×	1e-04
negative regulation of canonical NF-kappaB signal transduction	5	14.1×	6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	141
Likely benign	8
Benign	1

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
57126	GRCh38/hg38 8q24.13(chr8:122751607-123361569)x3	Pathogenic

SpliceAI

3826 predictions. Top by Δscore:

Variant	Effect	Δscore
8:123322932:GTTTA:G	donor_loss	1.0000
8:123322933:TTTAC:T	donor_loss	1.0000
8:123322934:TTAC:T	donor_loss	1.0000
8:123322935:TA:T	donor_loss	1.0000
8:123322936:A:AT	donor_loss	1.0000
8:123322937:C:G	donor_loss	1.0000
8:123323062:AGATT:A	acceptor_gain	1.0000
8:123323063:GATT:G	acceptor_gain	1.0000
8:123323064:ATT:A	acceptor_gain	1.0000
8:123323065:TT:T	acceptor_gain	1.0000
8:123323066:TCTAA:T	acceptor_loss	1.0000
8:123323067:C:CC	acceptor_gain	1.0000
8:123323067:CTAAA:C	acceptor_loss	1.0000
8:123325888:CATA:C	donor_gain	1.0000
8:123325889:ATAC:A	donor_loss	1.0000
8:123325890:TA:T	donor_loss	1.0000
8:123325891:A:AC	donor_gain	1.0000
8:123325892:C:CA	donor_gain	1.0000
8:123325892:CT:C	donor_gain	1.0000
8:123325892:CTT:C	donor_gain	1.0000
8:123326022:CATTT:C	acceptor_gain	1.0000
8:123326023:ATTT:A	acceptor_gain	1.0000
8:123326024:TTT:T	acceptor_gain	1.0000
8:123326025:TT:T	acceptor_gain	1.0000
8:123326026:TCTA:T	acceptor_loss	1.0000
8:123326027:C:CC	acceptor_gain	1.0000
8:123326027:C:CG	acceptor_loss	1.0000
8:123326028:T:A	acceptor_loss	1.0000
8:123326032:A:AC	acceptor_gain	1.0000
8:123328185:CGTA:C	donor_loss	1.0000

AlphaMissense

9187 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
8:123334310:C:A	R1075M	1.000
8:123334310:C:G	R1075T	1.000
8:123336397:A:G	Y1063H	1.000
8:123336405:G:T	A1060D	1.000
8:123337650:A:G	F1009S	1.000
8:123337710:A:G	L989P	1.000
8:123349322:A:G	F590S	1.000
8:123349326:G:T	R589S	1.000
8:123349334:C:A	R586M	1.000
8:123349334:C:G	R586T	1.000
8:123349366:G:C	N575K	1.000
8:123349366:G:T	N575K	1.000
8:123349373:G:T	A573D	1.000
8:123349376:C:T	G572D	1.000
8:123349377:C:G	G572R	1.000
8:123349382:A:T	V570D	1.000
8:123349413:C:G	D560H	1.000
8:123349418:A:G	L558P	1.000
8:123349424:A:G	L556P	1.000
8:123349427:A:G	L555P	1.000
8:123356443:T:A	D531V	1.000
8:123356443:T:G	D531A	1.000
8:123356444:C:G	D531H	1.000
8:123357581:A:G	L513P	1.000
8:123357599:C:T	G507E	1.000
8:123357600:C:G	G507R	1.000
8:123357600:C:T	G507R	1.000
8:123357604:C:A	W505C	1.000
8:123357604:C:G	W505C	1.000
8:123357606:A:G	W505R	1.000

dbSNP variants (sampled 300 via entrez): RS1000001617 (8:123341104 A>C), RS1000010368 (8:123383599 C>G), RS1000016239 (8:123417955 A>T), RS1000043399 (8:123333052 A>G), RS1000076686 (8:123324380 T>C), RS1000081233 (8:123390281 A>G), RS1000102423 (8:123409832 A>C), RS1000140646 (8:123392654 A>C), RS1000171649 (8:123380916 G>A), RS1000222681 (8:123322435 G>C), RS1000275544 (8:123392867 T>A,G), RS1000298097 (8:123372841 A>C), RS1000307073 (8:123365765 A>G), RS1000307476 (8:123410066 T>C), RS1000318141 (8:123351115 T>A,C)

Disease associations

OMIM: gene MIM:611941 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2150837 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 379,231 (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
CHEMBL190	THEOPHYLLINE ANHYDROUS	4	168,475
CHEMBL52609	DOXRIBTIMINE	2	210,756

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — 3.6.1.3 ATPases

Most potent curated ligand interactions (7 total), top 7:

Ligand	Action	Affinity	Parameter
AZ13824374	Inhibition	8.2	pIC50
GSK8814	Inhibition	7.3	pIC50
BAY-850	Binding	6.94	pKd
compound 23 [PMID: 31398032]	Inhibition	6.5	pIC50
compound 57 [PMID: 26155854]	Inhibition	5.9	pIC50
compound 60 [PMID: 26155854]	Inhibition	5.9	pIC50
compound 33 [PMID: 26230603]	Inhibition	5.3	pIC50

Binding affinities (BindingDB)

17 measured of 18 human assays (18 total across all organisms); most potent 17 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
CHEMBL5087319	IC50	16 nM
CHEMBL5093862	IC50	20 nM
CHEMBL5090369	IC50	20 nM
CHEMBL5086059	IC50	40 nM
CHEMBL5086260	IC50	79 nM
CHEMBL5074983	IC50	200 nM
CHEMBL5084768	IC50	251 nM
CHEMBL5083025	IC50	398 nM
CHEMBL5093167	IC50	398 nM
CHEMBL5092181	IC50	398 nM
CHEMBL5083653	IC50	1580 nM
CHEMBL5090538	IC50	3160 nM
CHEMBL5087156	IC50	5010 nM
CHEMBL5087174	IC50	12600 nM
CHEMBL5090410	IC50	20000 nM
CHEMBL5083337	IC50	25100 nM
CHEMBL5084439	IC50	31600 nM

ChEMBL bioactivities

252 potent at pChembl≥5 of 367 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.90	Kd	1.259	nM	CHEMBL5079885
8.89	Kd	1.3	nM	CHEMBL4206758
8.20	IC50	6.31	nM	CHEMBL5079885
8.15	IC50	7	nM	CHEMBL5079885
8.10	Kd	7.943	nM	CHEMBL3590405
8.10	Kd	8	nM	CHEMBL4206758
8.00	Kd	10	nM	CHEMBL4449894
7.85	IC50	14	nM	CHEMBL5087319
7.80	IC50	15.85	nM	CHEMBL5087319
7.70	Ki	19.95	nM	CHEMBL3590408
7.70	Ki	20	nM	CHEMBL3590408
7.70	IC50	19.95	nM	CHEMBL5093862
7.70	IC50	19.95	nM	CHEMBL5090369
7.70	IC50	20	nM	CHEMBL5093862
7.66	IC50	22	nM	CHEMBL5090369
7.66	IC50	22	nM	CHEMBL5397368
7.66	IC50	22	nM	CHEMBL4536031
7.60	IC50	25.12	nM	CHEMBL4576280
7.52	IC50	30	nM	CHEMBL4529901
7.50	IC50	31.62	nM	CHEMBL3590383
7.50	IC50	31.62	nM	CHEMBL5077167
7.40	IC50	39.81	nM	CHEMBL3590391
7.40	IC50	39.81	nM	CHEMBL3590405
7.40	IC50	39.81	nM	CHEMBL4244134
7.40	IC50	39.81	nM	CHEMBL5086059
7.39	IC50	41	nM	CHEMBL5086059
7.30	IC50	50.12	nM	CHEMBL3590407
7.30	Kd	50	nM	CHEMBL3590391
7.30	Kd	50.12	nM	CHEMBL3590391
7.30	IC50	50.12	nM	CHEMBL4206758
7.30	IC50	50.12	nM	CHEMBL5079885
7.22	Kd	60	nM	CHEMBL3590405
7.20	IC50	63.1	nM	CHEMBL3590405
7.20	IC50	63.1	nM	CHEMBL3590406
7.20	Kd	63.1	nM	CHEMBL3590405
7.20	Kd	63.1	nM	CHEMBL3590408
7.20	IC50	63.1	nM	CHEMBL4449894
7.11	IC50	78	nM	CHEMBL5086260
7.10	IC50	79.43	nM	CHEMBL3590407
7.10	Kd	79.43	nM	CHEMBL3590383
7.10	IC50	79.43	nM	CHEMBL5086260
7.10	IC50	79.43	nM	CHEMBL5079885
7.05	Kd	90	nM	CHEMBL3590383
7.05	Kd	90	nM	CHEMBL3590405
7.00	IC50	100	nM	CHEMBL3590406
7.00	IC50	100	nM	CHEMBL3590381
7.00	IC50	100	nM	CHEMBL3590385
7.00	IC50	100	nM	CHEMBL3590408
7.00	IC50	100	nM	CHEMBL4242484
7.00	IC50	100	nM	CHEMBL4589592

PubChem BioAssay actives

250 with measured affinity, of 612 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
8-[[(3R,4R,5S)-3-[(4,4-difluorocyclohexyl)methoxy]-5-methoxypiperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1376127: Binding affinity to partial length human ATAD2A (Q981 to R1108) expressed in bacterial expression system by Bromoscan method	kd	0.0013	uM
(1R,9S,12R)-13-[8-[[1-(2-fluoro-2-methylpropyl)piperidin-4-yl]amino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1823008: Binding affinity to ATAD2 bromodomain (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) by BROMOscan method	kd	0.0013	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-quinolin-2-one	1234389: Binding affinity to ATAD2 in human HUT78 cells incubated for 45 mins by mass spectrometry based bromosphere chemoproteomic assay	kd	0.0079	uM
N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[(4S)-4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl]acetamide	1561905: Binding affinity to human partial length ATAD2A (Q981 to R1108 residues) expressed in bacterial expression system by BROMOscan assay	kd	0.0100	uM
(1R,9S,12R)-13-[3-methyl-8-(3-pyrrolidin-1-ylpropylamino)-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822949: Inhibition of GST-ATAD2 BD (951 to 1132 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0140	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]-1-methylpiperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1234380: Binding affinity to ATAD2 (unknown origin) by BROMOscan panel based assay	ki	0.0199	uM
(1R,9S,12R)-13-[8-[3-(4,4-difluoropiperidin-1-yl)propylamino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0199	uM
(1R,9S,12R)-13-[8-[[1-(2,2-difluoropropyl)piperidin-4-yl]amino]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0199	uM
N-[(2R)-1-[(4-aminocyclohexyl)amino]-3-(4-cyanophenyl)propan-2-yl]-2-chloro-4-methoxy-5-[5-[[[(1R)-1-(4-methylphenyl)ethyl]amino]methyl]furan-2-yl]benzamide	2034414: Inhibition of N-terminal Hexahistidine-GST-tagged human ATAD2 bromodomain expressed in Escherichia coli BL21 (DE3) Rosetta cells incubated for 1 hr by FRET analysis	ic50	0.0220	uM
2-chloro-N-[(2R)-1-(methylamino)-3-(4-nitrophenyl)-1-oxopropan-2-yl]-5-[5-[[[(1R)-1-(4-methylphenyl)ethyl]amino]methyl]furan-2-yl]benzamide	2034414: Inhibition of N-terminal Hexahistidine-GST-tagged human ATAD2 bromodomain expressed in Escherichia coli BL21 (DE3) Rosetta cells incubated for 1 hr by FRET analysis	ic50	0.0220	uM
N-[4-bromo-3-[(3S,4S)-3,4-dimethylpyrrolidin-1-yl]sulfonylphenyl]-2-(4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl)acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.0251	uM
[1-methyl-6-(4-methylpiperazin-1-yl)pyrazolo[3,4-d]pyrimidin-4-yl]-phenylmethanone	1516801: Displacement of biotinylated H4 peptide from His6/FLAG-tagged TEV fused ATAD2 bromodomain (950 to 1148 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells after 30 mins by TR-FRET assay	ic50	0.0300	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.0316	uM
(1R,9S)-13-[3-methyl-8-[(1-methylpiperidin-4-yl)amino]-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0316	uM
5-(5-amino-3-pyridinyl)-8-[[(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino]-3-methyl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.0398	uM
8-[[(3R,4R)-3-[(4,4-difluorocyclohexyl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-quinolin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.0398	uM
(1R,9S)-13-[3-methyl-8-(3-pyrrolidin-1-ylpropylamino)-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl]-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0398	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-ethyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.0501	uM
8-[[(3R,4R)-3-[[(2R,6S)-2,6-dimethyl-1,1-dioxothian-4-yl]methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.0631	uM
2-methyl-4-[(1R,9S,12R)-12-methyl-10-oxo-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-triene-13-carbonyl]-6-(trifluoromethoxy)-9H-pyrido[3,4-b]indol-1-one	1822949: Inhibition of GST-ATAD2 BD (951 to 1132 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.0780	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-pyridin-3-yl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.1000	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-5-(5-methoxy-3-pyridinyl)-3-methyl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.1000	uM
8-[[(1S,2R,3R,5R)-2-[2-(4,4-difluorocyclohexyl)ethyl]-8-azabicyclo[3.2.1]octan-3-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.1000	uM
N-[4-bromo-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-[(4R)-4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl]acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.1000	uM
8-[[(3R,4R,5S)-3-[(1,1-dioxothian-4-yl)methoxy]-5-methoxypiperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.1259	uM
8-[[(3R,4R)-3-(cyclohexylmethoxy)piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1234389: Binding affinity to ATAD2 in human HUT78 cells incubated for 45 mins by mass spectrometry based bromosphere chemoproteomic assay	kd	0.1585	uM
3-methyl-8-[[(3R,4R)-3-(oxan-4-ylmethoxy)piperidin-4-yl]amino]-5-pyridin-3-yl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.1995	uM
8-[[(3S,4R,5R)-3-methoxy-5-(oxan-4-ylmethoxy)piperidin-4-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.1995	uM
2-methyl-4-[(1R,9S,12R)-12-methyl-10-oxo-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-triene-13-carbonyl]-9H-pyrido[3,4-b]indol-1-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.1995	uM
N-[(2S)-1-[(4-aminocyclohexyl)amino]-3-(4-cyanophenyl)propan-2-yl]-2-chloro-4-methoxy-5-[5-[[[(1R)-1-(4-methylphenyl)ethyl]amino]methyl]furan-2-yl]benzamide	2192498: Inhibitory activity against ATAD2 (unknown origin) at bromodomain incubated for 180 min by Tr-FRET assay	ic50	0.2420	uM
3-methyl-5-(5-methyl-3-pyridinyl)-8-[[(3R,4R)-3-(oxan-4-ylmethoxy)piperidin-4-yl]amino]-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.2512	uM
5-(5-methoxy-3-pyridinyl)-3-methyl-8-[[(3R,4R)-3-(oxan-4-ylmethoxy)piperidin-4-yl]amino]-1H-1,7-naphthyridin-2-one	1234373: Displacement of histone H4 peptide from FLAG-6His-Tev-ATAD2 (981 to 1121) (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by TR-FRET analysis relative to control	ic50	0.2512	uM
8-[[(1S,2R,3R,5R)-2-[2-(1,1-dioxothian-4-yl)ethyl]-8-azabicyclo[3.2.1]octan-3-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-quinolin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.2512	uM
8-[[(1S,2R,3R,5R)-2-[2-(1,1-dioxothian-4-yl)ethyl]-8-azabicyclo[3.2.1]octan-3-yl]amino]-3-methyl-5-(5-methyl-3-pyridinyl)-1H-1,7-naphthyridin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.2512	uM
3-methyl-5-(5-methyl-3-pyridinyl)-8-[[(1S,2R,3R,5R)-2-[2-(oxan-4-yl)ethyl]-8-azabicyclo[3.2.1]octan-3-yl]amino]-1H-1,7-naphthyridin-2-one	1400529: Inhibition of N-terminal FLAG-6His-tagged TEV-fused ATAD2 (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) after 30 mins in presence of biotinylated triacetylated histone H4 peptide by alexa fluor 488-dye based TR-FRET assay	ic50	0.2512	uM
N-[4-chloro-3-[(3S,4S)-3,4-dimethylpyrrolidin-1-yl]sulfonylphenyl]-2-(2,5-dioxoimidazolidin-1-yl)acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.2512	uM
N-(4-bromo-3-pyrrolidin-1-ylsulfonylphenyl)-2-[(4S)-4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl]acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.2512	uM
(1R,9S)-13-(8-amino-3-methyl-[1,2,4]triazolo[4,3-b]pyridazine-6-carbonyl)-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.2512	uM
N-(4-bromo-3-piperidin-1-ylsulfonylphenyl)-2-(4-cyclopropyl-4-methyl-2,5-dioxoimidazolidin-1-yl)acetamide	1516806: Displacement of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGAKRHRKV-biotin) from His6/FLAG-tagged TEV fused ATAD2 bromodomain (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells after 30 mins by TR-FRET assay	ic50	0.3162	uM
(1R,9S)-13-[3-methyl-8-[(1-methylpiperidin-4-yl)amino]-[1,2,4]triazolo[4,3-a]pyridine-6-carbonyl]-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-trien-10-one	1822949: Inhibition of GST-ATAD2 BD (951 to 1132 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.3700	uM
2-methyl-4-[(1R,9S)-10-oxo-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-triene-13-carbonyl]-9H-pyrido[3,4-b]indol-1-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.3981	uM
2-methyl-4-[(1R,9S,12R)-10-oxo-12-propan-2-yl-11,13-diazatricyclo[7.3.1.02,7]trideca-2,4,6-triene-13-carbonyl]-9H-pyrido[3,4-b]indol-1-one	1822946: Inhibition of GST-ATAD2 BD (981 to 1108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) and biotinylated tetra-acetylated histone H4 peptides as substrate incubated for 30 mins by TR-FRET assay	ic50	0.3981	uM
N-[4-chloro-3-(3-cyclopropylpyrrolidin-1-yl)sulfonylphenyl]-2-(2,5-dioxoimidazolidin-1-yl)acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.5012	uM
8-[[(3R,4R)-3-[(1,1-dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.5012	uM
N-[4-chloro-3-(3-ethylpyrrolidin-1-yl)sulfonylphenyl]-2-(2,5-dioxoimidazolidin-1-yl)acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.6310	uM
N-[4-bromo-3-(3-methylpiperidin-1-yl)sulfonylphenyl]-2-(2,5-dioxoimidazolidin-1-yl)acetamide	1516834: Displacement of Alexa Fluor 488 labelled ligand from ATAD2 bromodomain (981 to 1121 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells after 30 mins by TR-FRET assay	ic50	0.6310	uM
8-[[1-(3-aminopropyl)piperidin-4-yl]amino]-5-[5-(hydroxymethyl)-3-pyridinyl]-3-methyl-1H-1,7-naphthyridin-2-one	1766142: Inhibition of ATAD2 (unknown origin) by TR-FRET assay	ic50	0.6310	uM
5-(5-amino-3-pyridinyl)-3-methyl-8-(piperidin-4-ylamino)-1H-1,7-naphthyridin-2-one	1231074: Displacement of histone H4 peptide from FLAG-6His-Tev-ATAD2 (981 to 1121) (unknown origin) expressed in Escherichia coli BL21 (DE3) after 30 mins by TR-FRET analysis	ic50	0.7943	uM
3-methyl-8-[[(3R,4R)-3-(oxan-4-ylmethoxy)piperidin-4-yl]amino]-5-pyrimidin-5-yl-1H-1,7-naphthyridin-2-one	1234377: Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay	ic50	0.7943	uM
N-[4-chloro-3-[(3S)-3-methylpyrrolidin-1-yl]sulfonylphenyl]-2-(2,5-dioxoimidazolidin-1-yl)acetamide	1561897: Displacement of Alexa Fluor 488-labeled ligand from FLAG-6His-Tev-fused ATAD2 (981 to 1121 residue) (unknown origin) measured after 30 mins by TR-FRET assay	ic50	0.7943	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, increases expression, increases abundance, affects expression, affects cotreatment (+1 more)	5
Estradiol	affects cotreatment, increases expression	5
Benzo(a)pyrene	decreases expression	4
Tetrachlorodibenzodioxin	affects expression, decreases expression	4
Cisplatin	affects cotreatment, decreases expression, increases expression	3
7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide	decreases expression, increases expression	3
Cyclosporine	decreases expression	3
trichostatin A	affects cotreatment, decreases expression	2
sodium arsenite	decreases expression, increases expression	2
Dasatinib	affects cotreatment, decreases expression	2
Resveratrol	affects cotreatment, increases expression	2
Progesterone	affects cotreatment, increases expression	2
Tretinoin	decreases expression	2
afuresertib	decreases expression	1
FR900359	affects phosphorylation	1
TAK-243	decreases sumoylation	1
ginger extract	affects cotreatment, affects expression, increases abundance	1
dicrotophos	decreases expression	1
chloroacetaldehyde	affects expression	1
methylmercuric chloride	increases expression	1
triphenyl phosphate	affects expression	1
pirinixic acid	affects binding, decreases expression, increases activity	1
deoxynivalenol	increases expression	1
beta-lapachone	decreases expression	1
arsenite	affects binding, decreases reaction	1
methylparaben	increases expression	1
cobaltous chloride	decreases expression	1
perfluorooctanoic acid	decreases expression	1
zinc chromate	decreases expression, increases abundance	1
2,3-bis(3’-hydroxybenzyl)butyrolactone	increases expression, affects cotreatment	1

ChEMBL screening assays

112 unique, capped per target: 112 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2156122	Binding	Binding affinity to ATAD2 by isothermal titration calorimetric analysis	Discovery and characterization of small molecule inhibitors of the BET family bromodomains. — J Med Chem

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B0ZT	Abcam MCF-7 ATAD2 KO	Cancer cell line	Female
CVCL_B1K8	Abcam HeLa ATAD2 KO	Cancer cell line	Female
CVCL_SD79	HAP1 ATAD2 (-) 1	Cancer cell line	Male
CVCL_SD80	HAP1 ATAD2 (-) 2	Cancer cell line	Male

Clinical trials (associated diseases)

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