BRD7

Summary

BRD7 (bromodomain containing 7, HGNC:14310) is a protein-coding gene on chromosome 16q12.1, encoding Bromodomain-containing protein 7 (Q9NPI1). Acts both as coactivator and as corepressor. It is a selective cancer dependency (DepMap: 17.2% of cell lines).

This gene encodes a protein which is a member of the bromodomain-containing protein family. The product of this gene has been identified as a component of one form of the SWI/SNF chromatin remodeling complex, and as a protein which interacts with p53 and is required for p53-dependent oncogene-induced senescence which prevents tumor growth. Pseudogenes have been described on chromosomes 2, 3, 6, 13 and 14. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 29117 — RefSeq curated summary.

At a glance

• GWAS associations: 4
• Clinical variants (ClinVar): 116 total — 1 likely-pathogenic
• Druggable target: yes — 1 molecules with ChEMBL bioactivity
• Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 2 cancer types
• Cancer dependency (DepMap): dependent in 17.2% of screened cell lines
• MANE Select transcript: NM_013263

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:14310
Approved symbol	BRD7
Name	bromodomain containing 7
Location	16q12.1
Locus type	gene with protein product
Status	Approved
Aliases	CELTIX1, BP75, SMARCI1
Ensembl gene	ENSG00000166164
Ensembl biotype	protein_coding
OMIM	618489
Entrez	29117

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 6 protein_coding, 2 protein_coding_CDS_not_defined, 1 retained_intron

ENST00000394688, ENST00000394689, ENST00000401491, ENST00000475877, ENST00000562383, ENST00000567826, ENST00000569774, ENST00000710356, ENST00000710357

RefSeq mRNA: 2 — MANE Select: NM_013263 NM_001173984, NM_013263

CCDS: CCDS10742, CCDS54007

Canonical transcript exons

ENST00000394688 — 17 exons

Exon	Start	End
ENSE00001100339	50323587	50323698
ENSE00001100349	50319887	50320030
ENSE00001100356	50320248	50320391
ENSE00001100368	50321982	50322038
ENSE00001141719	50320663	50320774
ENSE00001141735	50325748	50325883
ENSE00001141741	50326284	50326391
ENSE00001141743	50328669	50328744
ENSE00001141746	50333574	50333697
ENSE00001519214	50368726	50368988
ENSE00002657824	50315957	50319266
ENSE00003545279	50339976	50340086
ENSE00003577749	50334711	50334895
ENSE00003592018	50350023	50350167
ENSE00003607847	50354793	50354922
ENSE00003665579	50354425	50354482
ENSE00004011632	50368090	50368298

Expression profiles

Bgee: expression breadth ubiquitous, 217 present calls, max score 97.63.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 48.5049 / max 652.5918, expressed in 1823 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
157307	44.7214	1823
157308	2.9991	1303
157306	0.7843	452

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
sural nerve	UBERON:0015488	97.63	gold quality
ventricular zone	UBERON:0003053	97.15	gold quality
ganglionic eminence	UBERON:0004023	96.49	gold quality
islet of Langerhans	UBERON:0000006	96.13	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	95.76	gold quality
calcaneal tendon	UBERON:0003701	95.75	gold quality
cortical plate	UBERON:0005343	95.74	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	95.49	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	95.08	gold quality
right testis	UBERON:0004534	95.08	gold quality
popliteal artery	UBERON:0002250	95.06	gold quality
tibial artery	UBERON:0007610	95.05	gold quality
left testis	UBERON:0004533	94.96	gold quality
ascending aorta	UBERON:0001496	94.83	gold quality
thoracic aorta	UBERON:0001515	94.82	gold quality
aorta	UBERON:0000947	94.67	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	94.48	gold quality
muscle layer of sigmoid colon	UBERON:0035805	94.47	gold quality
granulocyte	CL:0000094	94.44	gold quality
descending thoracic aorta	UBERON:0002345	94.44	gold quality
lower esophagus	UBERON:0013473	94.37	gold quality
lower esophagus muscularis layer	UBERON:0035833	94.36	gold quality
smooth muscle tissue	UBERON:0001135	94.35	gold quality
ectocervix	UBERON:0012249	94.34	gold quality
right coronary artery	UBERON:0001625	94.32	gold quality
body of pancreas	UBERON:0001150	94.29	gold quality
skin of abdomen	UBERON:0001416	94.28	gold quality
lower esophagus mucosa	UBERON:0035834	94.26	gold quality
mucosa of stomach	UBERON:0001199	94.24	gold quality
leukocyte	CL:0000738	94.17	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-GEOD-134144	yes	28.04
E-CURD-112	yes	14.15
E-ANND-3	yes	9.01

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

3 targets.

Target	Regulation
BRD2	Activation
BRD3	Activation
E2F3	Repression

Upstream regulators (CollecTRI, top): AR, E2F6, MAX, MYC, SP1

miRNA regulators (miRDB)

11 targeting BRD7, 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-5011-5P	100.00	83.46	5820
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-493-5P	99.96	72.47	2382
HSA-MIR-548E-5P	99.89	72.73	4486
HSA-MIR-556-3P	99.74	68.75	1203
HSA-MIR-889-3P	99.40	69.76	2103
HSA-MIR-4263	99.18	69.25	2236
HSA-MIR-548L	99.06	70.90	2560

Functional genomics

DepMap (CRISPR cell-line fitness): dependent in 17.2% of screened cell lines.

Literature-anchored findings (GeneRIF, showing 40)

• Regulation of transcription by E1B-AP5 is mediated by complex formation with this protein. (PMID:12489984)
• BRD7 could up-regulate the expression levels of BRD2 and BRD3 genes in mRNA level to some extent. (PMID:12600283)
• Expression levels of NAG-7, and BRD7 did not alter in gastric and colorectal cancers. NAG-7 and BRD7 genes may not play role in gastric and colorectal carcinogenesis. (PMID:12918109)
• BRD7 inhibits G1-S progression by transcriptionally regulating some important molecules involved in ras/MEK/ERK and Rb/E2F pathways. (PMID:15137061)
• Taken together, the present work shed light on the fact that a novel bromodomain gene, BRD7, is of importance in transcriptional regulation and cellular events including cell cycle. (PMID:16265664)
• the nuclear localization of BRD7 is critical for the expression of cell cycle related molecules and cell biological function. (PMID:16475162)
• The results showed that BRD7 could interact with BRD2 and the region from amino acid 430 to 798 of BRD2 was critical for the interaction of BRD2 with BRD7. BRD2 mainly localizes in nucleus and BRD2 has distinct roles in initiating apoptosis. (PMID:16786191)
• BRD7 promoter demethylation is a prerequisite for high level induction of BRD7 gene expression in human nasopharyngeal carcinoma cells (PMID:18778484)
• BRD7 is a novel PBAF-specific SWI/SNF subunit that is required for target gene activation and repression in embryonic stem cells (PMID:18809673)
• c-Myc negatively regulates and Sp1 slightly positively regulate BRD7 promoter activity. (PMID:19111069)
• TRIM24 regulates AR-mediated transcription in collaboration with TIP60 and BRD7. (PMID:19909775)
• BRD7 suppresses tumorigenicity by serving as a p53 cofactor required for the efficient induction of p53-dependent oncogene-induced senescence. (PMID:20228809)
• All-trans retinoic acid enhances brd7 gene expression as HL-60 cells differentiate. (PMID:20561408)
• as unique regulators of replicative senescence in human cells, both BRD7 and BAF180 regulate p53 transcriptional activity toward a subset of its target genes required for replicative and oncogenic stress senescence induction (PMID:20660729)
• The region from aa219 to aa450 is primarily defined as an atypical nuclear export signal in BRD7. (PMID:21873788)
• Data indicate that BRD7 may be related to the occurrence, development, and metastasis of lung cancers. (PMID:22008115)
• miR-200c inhibits the expression of BRD7. MiR-200c regulated the translocation of beta-catenin from the cytoplasm to the nucleus via inhibition of BRD7, resulting in increased expression of its transcriptional target genes, cyclinD1 and c-myc. (PMID:22015043)
• No evidence for breast cancer susceptibility is associated with variants of BRD7. (PMID:22864638)
• Data show a substantial proportion of germ-line mutations in triple-negative breast cancer (TNBC), with a preponderance of BRCA1 mutations over mutations in BRCA2 or PALB2, but no evidence to implicate BRD7 mutations in the etiology of TNBC. (PMID:23110154)
• These results suggested that BRD7 acts as a tumor suppressor in epithelial ovarian cancers (PMID:24198243)
• Disturbing miR-182 and -381 inhibits BRD7 transcription and glioma growth by directly targeting LRRC4. (PMID:24404152)
• BRD7-mediated translocation of a subfraction (but not all) of the p85 protein to the nucleus could enhance PI3K signaling. (PMID:24657164)
• lower BRD7 expression is an indicator for poor prognosis in patients with osteosarcoma. (PMID:24840027)
• BRD7 promoter hypermethylation is an indicator of well differentiated oral squamous cell carcinomas. (PMID:25743841)
• Data indicate that bromodomain-containing protein 7 (BRD7) was a direct target of microRNA-410 (miR-410). (PMID:26149213)
• constructed a regulating network of BRD7 downstream genes, and this network suggests multiple feedback regulations of the pathways. Furthermore, we validated BIRC2, BIRC3, TXN2, and NOTCH1 genes as direct, functional BRD7 targets (PMID:26407966)
• Propose that the balance between BRD7 function and Ras/Raf/MEK/ERK activity is important for determining the outcomes of HCV infection and HCC development. (PMID:26620707)
• our data indicated that BRD7 may serve as a tumor suppressor in hepatocellular carcinoma (PMID:26919247)
• the expression of miR-141 in BRD7-overexpressing NPC cells could partially reverse the tumor suppressive effect of BRD7 on cell proliferation and tumor growth in vitro and in vivo. (PMID:27010857)
• Results demonstrate a novel function of BRD7 in TGF-beta signaling. BRD7 interacts with the Smad tumor suppressor complex, and enhances both DNA-binding ability and transcriptional activity of Smads. BRD7 functions in growth inhibition and tumor suppression partly as a transcriptional co-activator of Smads. (PMID:27270427)
• the transcriptional signature of low BRD7 expressing cells is associated with increased angiogenesis. (PMID:28951988)
• c-Myc transactivates miR-141 expression and that BRD7, a direct target of c-Myc, serves as a cofactor of c-Myc and forms a negative feedback loop with c-Myc in miR-141 transcription in NPC. (PMID:29559001)
• BRD7 was positively correlated with BAK levels in breast cancer tissues, and the survival rate of patients with low BAK and BRD7 expression was significantly lower than that of patients with high BAK and BRD7 expression. In addition, BRD7 activated BAK promoter activity and induced BAK expression in an indirect manner. (PMID:30592293)
• PARP1 induces the degradation of BRD7. (PMID:30940648)
• Expression and subcellular localization of the bromodomain-containing protein 7 is a prognostic biomarker in breast cancer. (PMID:31929348)
• Bromodomain-containing protein 7 regulates matrix metabolism and apoptosis in human nucleus pulposus cells through the BRD7-PI3K-YAP1 signaling axis. (PMID:34038745)
• BRD7 restrains TNF-alpha-induced proliferation and migration of airway smooth muscle cells by inhibiting notch signaling. (PMID:35943053)
• LncRNA LENGA acts as a tumor suppressor in gastric cancer through BRD7/TP53 signaling. (PMID:36477655)
• Characterization of the Functional Interplay between the BRD7 and BRD9 Homologues in mSWI/SNF Complexes. (PMID:36484504)
• BRD7 inhibits enhancer activity and expression of BIRC2 to suppress tumor growth and metastasis in nasopharyngeal carcinoma. (PMID:36788209)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	brd7	ENSDARG00000008380
mus_musculus	Brd7	ENSMUSG00000031660
rattus_norvegicus	Brd7	ENSRNOG00000014419
drosophila_melanogaster	Brd7-9	FBGN0031947
caenorhabditis_elegans	swsn-9	WBGENE00007256

Paralogs (2): BRD9 (ENSG00000028310), YBEY (ENSG00000182362)

Protein

Protein identifiers

Bromodomain-containing protein 7 — Q9NPI1 (reviewed: Q9NPI1)

Alternative names: 75 kDa bromodomain protein, Protein CELTIX-1

All UniProt accessions (5): A0AA34QVS2, A0AA34QW01, Q9NPI1, I3L0Y7, I3L4V5

UniProt curated annotations — full annotation on UniProt →

Function. Acts both as coactivator and as corepressor. May play a role in chromatin remodeling. Activator of the Wnt signaling pathway in a DVL1-dependent manner by negatively regulating the GSK3B phosphotransferase activity. Induces dephosphorylation of GSK3B at ‘Tyr-216’. Down-regulates TRIM24-mediated activation of transcriptional activation by AR. Transcriptional corepressor that down-regulates the expression of target genes. Binds to target promoters, leading to increased histone H3 acetylation at ‘Lys-9’ (H3K9ac). Binds to the ESR1 promoter. Recruits BRCA1 and POU2F1 to the ESR1 promoter. Coactivator for TP53-mediated activation of transcription of a set of target genes. Required for TP53-mediated cell-cycle arrest in response to oncogene activation. Promotes acetylation of TP53 at ‘Lys-382’, and thereby promotes efficient recruitment of TP53 to target promoters. Inhibits cell cycle progression from G1 to S phase.

Subunit / interactions. Interacts with TRIM24, PTPN13 and DVL1. Identified in a complex with SMARCA4/BRG1, SMARCC1/BAF155, SMARCE1/BAF57, DPF2/BAF45D and ARID2, subunits of the SWI/SNF-B (PBAF) chromatin remodeling complex. Interacts with IRF2 and HNRPUL1. Interacts (via N-terminus) with TP53. Interacts (via C-terminus) with EP300. Interacts with BRCA1. Interacts (via bromo domain) with histone H3 (via N-terminus) acetylated at ‘Lys-14’ (H3K14ac). Has low affinity for histone H3 acetylated at ‘Lys-9’ (H3K9ac). Has the highest affinity for histone H3 that is acetylated both at ‘Lys-9’ (H3K9ac) and at ‘Lys-14’ (H3K14ac). Has very low affinity for non-acetylated histone H3. Interacts (via bromo domain) with histone H4 (via N-terminus) acetylated at ‘Lys-8’ (H3K8ac) (in vitro).

Subcellular location. Nucleus. Chromosome Nucleus.

Isoforms (2)

UniProt ID	Names	Canonical?
Q9NPI1-1	1	yes
Q9NPI1-2	2

RefSeq proteins (2): NP_001167455, NP_037395* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001487	Bromodomain	Domain
IPR021900	DUF3512	Family
IPR036427	Bromodomain-like_sf	Homologous_superfamily
IPR051831	Bromodomain_contain_prot	Family

Pfam: PF00439, PF12024

UniProt features (51 total): cross-link 12, helix 11, modified residue 7, compositionally biased region 5, sequence conflict 5, strand 3, region of interest 2, chain 1, domain 1, splice variant 1, turn 1, coiled-coil region 1, short sequence motif 1

Structure

Experimental structures (PDB)

11 structures.

PDB	Method	Resolution (Å)
5MQ1	X-RAY DIFFRACTION	1.5
6V0Q	X-RAY DIFFRACTION	1.69
6PPA	X-RAY DIFFRACTION	1.77
6V16	X-RAY DIFFRACTION	1.9
6V1H	X-RAY DIFFRACTION	1.93
6V1F	X-RAY DIFFRACTION	2
6V17	X-RAY DIFFRACTION	2.05
6V1E	X-RAY DIFFRACTION	2.3
7VDV	ELECTRON MICROSCOPY	3.4
7Y8R	ELECTRON MICROSCOPY	4.4
2I7K	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NPI1-F1	64.87	0.23

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 (19): 279, 289, 328, 380, 482, 514, 621, 21, 52, 127, 186, 197, 201, 212, 241, 305, 307, 344, 389

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-6804758	Regulation of TP53 Activity through Acetylation
R-HSA-9933939	Formation of the polybromo-BAF (pBAF) complex
R-HSA-212436	Generic Transcription Pathway
R-HSA-3700989	Transcriptional Regulation by TP53
R-HSA-5633007	Regulation of TP53 Activity
R-HSA-73857	RNA Polymerase II Transcription
R-HSA-74160	Gene expression (Transcription)

MSigDB gene sets: 210 (showing top): GOBP_REGULATION_OF_DOUBLE_STRAND_BREAK_REPAIR, GOBP_REGULATION_OF_CELL_ACTIVATION, GOBP_CHROMOSOME_ORGANIZATION, GOBP_POSITIVE_REGULATION_OF_HEMOPOIESIS, GOBP_CELL_CYCLE_PHASE_TRANSITION, GOBP_REGULATION_OF_DNA_REPAIR, GOBP_POSITIVE_REGULATION_OF_CELL_ADHESION, GOBP_CELL_CELL_ADHESION, GOBP_REGULATION_OF_LEUKOCYTE_DIFFERENTIATION, GOBP_NUCLEOTIDE_EXCISION_REPAIR, GOBP_REGULATION_OF_MYOBLAST_DIFFERENTIATION, GOBP_REGULATION_OF_HEMOPOIESIS, GOBP_MUSCLE_STRUCTURE_DEVELOPMENT, GOBP_NEGATIVE_REGULATION_OF_CELL_CYCLE_PROCESS, GOBP_REGULATION_OF_CHROMOSOME_SEGREGATION

GO Biological Process (16): chromatin remodeling (GO:0006338), regulation of transcription by RNA polymerase II (GO:0006357), regulation of mitotic cell cycle (GO:0007346), Wnt signaling pathway (GO:0016055), regulation of mitotic metaphase/anaphase transition (GO:0030071), positive regulation of T cell differentiation (GO:0045582), positive regulation of cell differentiation (GO:0045597), positive regulation of myoblast differentiation (GO:0045663), transcription initiation-coupled chromatin remodeling (GO:0045815), negative regulation of DNA-templated transcription (GO:0045892), regulation of G0 to G1 transition (GO:0070316), regulation of G1/S transition of mitotic cell cycle (GO:2000045), negative regulation of G1/S transition of mitotic cell cycle (GO:2000134), positive regulation of double-strand break repair (GO:2000781), regulation of nucleotide-excision repair (GO:2000819), positive regulation of DNA-templated transcription (GO:0045893)

GO Molecular Function (7): transcription cis-regulatory region binding (GO:0000976), p53 binding (GO:0002039), transcription coactivator activity (GO:0003713), transcription corepressor activity (GO:0003714), histone binding (GO:0042393), histone H3K14ac reader activity (GO:0140015), protein binding (GO:0005515)

GO Cellular Component (9): kinetochore (GO:0000776), chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytosol (GO:0005829), nuclear matrix (GO:0016363), RSC-type complex (GO:0016586), chromosome (GO:0005694)

Reactome top-level categories

Rollup of top-6 pathways:

Category	Pathways
Regulation of TP53 Activity	1
SWI/SNF chromatin remodelers	1
RNA Polymerase II Transcription	1
Generic Transcription Pathway	1
Transcriptional Regulation by TP53	1
Gene expression (Transcription)	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	5
regulation of DNA-templated transcription	3
regulation of mitotic cell cycle phase transition	2
DNA-templated transcription	2
G1/S transition of mitotic cell cycle	2
protein binding	2
transcription coregulator activity	2
intracellular membraneless organelle	2
nuclear lumen	2
chromatin organization	1
transcription by RNA polymerase II	1
mitotic cell cycle	1
regulation of cell cycle	1
cell surface receptor signaling pathway	1
metaphase/anaphase transition of mitotic cell cycle	1
regulation of metaphase/anaphase transition of cell cycle	1
T cell differentiation	1
regulation of T cell differentiation	1
positive regulation of lymphocyte differentiation	1
positive regulation of T cell activation	1
cell differentiation	1
regulation of cell differentiation	1
positive regulation of cellular process	1
positive regulation of developmental process	1
myoblast differentiation	1
positive regulation of cell differentiation	1
regulation of myoblast differentiation	1
transcription initiation at RNA polymerase II promoter	1
positive regulation of gene expression, epigenetic	1
negative regulation of RNA biosynthetic process	1
regulation of cell cycle process	1
G0 to G1 transition	1
regulation of cell cycle G1/S phase transition	1
negative regulation of mitotic cell cycle phase transition	1
negative regulation of cell cycle G1/S phase transition	1
regulation of G1/S transition of mitotic cell cycle	1
double-strand break repair	1
positive regulation of DNA repair	1
regulation of double-strand break repair	1
regulation of DNA repair	1

Protein interactions and networks

STRING

2132 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
BRD7	ARID2	Q68CP9	997
BRD7	PHF10	Q8WUB8	996
BRD7	PBRM1	Q86U86	992
BRD7	SMARCA4	P51532	986
BRD7	ARID1A	O14497	962
BRD7	ACTL6A	O96019	944
BRD7	TP53	P04637	938
BRD7	ARID1B	Q8NFD5	936
BRD7	SMARCB1	Q12824	932
BRD7	SMARCE1	Q969G3	907
BRD7	SMARCC1	Q92922	873
BRD7	DPF2	Q92785	855
BRD7	SMARCC2	Q8TAQ2	817
BRD7	DPF1	Q92782	800
BRD7	SMARCA2	P51531	791

IntAct

190 interactions, top by confidence:

A	B	Type	Score
SMARCB1	ARID1A	psi-mi:“MI:0914”(association)	0.860
SMARCE1	ARID1A	psi-mi:“MI:0914”(association)	0.840
NUP50	KPNA4	psi-mi:“MI:0914”(association)	0.830
SMARCC1	ARID1A	psi-mi:“MI:0914”(association)	0.790
SMARCC2	ARID1A	psi-mi:“MI:0914”(association)	0.790
SMARCD1	ARID1A	psi-mi:“MI:0914”(association)	0.790
TP53	BRD7	psi-mi:“MI:0915”(physical association)	0.730
BRD7	TP53	psi-mi:“MI:0915”(physical association)	0.730
TP53	BRD7	psi-mi:“MI:0403”(colocalization)	0.730
SMARCE1	SMARCA2	psi-mi:“MI:0914”(association)	0.730

BioGRID (740): BRD7 (Affinity Capture-MS), BRD7 (Affinity Capture-MS), BRD7 (Affinity Capture-MS), BRD7 (Affinity Capture-MS), TP53 (Affinity Capture-Western), TP53 (Reconstituted Complex), BRD7 (Co-localization), EP300 (Affinity Capture-Western), ARID2 (Co-fractionation), BRD7 (Co-fractionation), BRD7 (Co-fractionation), PBRM1 (Co-fractionation), BRD7 (Two-hybrid), BRD7 (Affinity Capture-MS), BRD7 (Affinity Capture-MS)

ESM2 similar proteins: A0JMK9, A0JMT0, A2BIL7, A8DZJ1, D4AEC2, F4IDY7, O60268, O88379, P13864, P61406, Q03111, Q12830, Q24K09, Q3T8J9, Q4R707, Q4V7A6, Q535K8, Q5R8B0, Q5RAK6, Q5S003, Q63ZP1, Q640I9, Q6DD45, Q6P1G2, Q6ZRS2, Q7TNN8, Q80Y56, Q86US8, Q86W92, Q8BMD7, Q8BRB7, Q8BZ21, Q8C1B1, Q8R0A7, Q8WML3, Q8WUB8, Q92539, Q92794, Q96KC8, Q98TA5

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

4 interactions.

A	Effect	B	Mechanism
BRD7	“up-regulates quantity by expression”	BRD2	“transcriptional regulation”
BRD7	“up-regulates quantity by expression”	BRD3	“transcriptional regulation”
BRD7	“form complex”	“SWI/SNF ACTL6B varian”	binding
ATM	“down-regulates activity”	BRD7	phosphorylation

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 177 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.

Reactome pathways:

Pathway	Partners	Fold	FDR
Formation of the canonical BAF (cBAF) complex	12	60.4×	6e-18
Formation of the polybromo-BAF (pBAF) complex	12	60.4×	6e-18
Formation of the embryonic stem cell BAF (esBAF) complex	12	57.2×	1e-17
Formation of neuronal progenitor and neuronal BAF (npBAF and nBAF)	15	54.4×	4e-21
Formation of the non-canonical BAF (ncBAF) complex	9	48.0×	3e-12
Regulation of endogenous retroelements	12	35.1×	2e-14
Regulation of MITF-M-dependent genes involved in pigmentation	16	33.7×	1e-18
RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known	11	26.2×	1e-11

GO biological processes:

GO term	Partners	Fold	FDR
regulation of G0 to G1 transition	15	61.3×	2e-21
regulation of nucleotide-excision repair	15	54.7×	6e-21
nucleosome disassembly	11	53.5×	2e-15
regulation of mitotic metaphase/anaphase transition	15	45.1×	1e-19
NLS-bearing protein import into nucleus	9	43.8×	2e-11
positive regulation of double-strand break repair	15	31.3×	8e-17
positive regulation of T cell differentiation	11	30.4×	4e-12
regulation of G1/S transition of mitotic cell cycle	15	27.9×	5e-16

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 2 cancer types — HCC, MEL.

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	1
Uncertain significance	79
Likely benign	4
Benign	0

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
208203	NM_013263.5(BRD7):c.1834C>T (p.Arg612Ter)	Likely pathogenic

SpliceAI

3410 predictions. Top by Δscore:

Variant	Effect	Δscore
16:50313955:CA:C	acceptor_loss	1.0000
16:50313956:A:AG	acceptor_gain	1.0000
16:50313957:G:GT	acceptor_gain	1.0000
16:50313957:GC:G	acceptor_gain	1.0000
16:50313957:GCT:G	acceptor_gain	1.0000
16:50313957:GCTC:G	acceptor_gain	1.0000
16:50313957:GCTCC:G	acceptor_gain	1.0000
16:50314060:CAG:C	donor_loss	1.0000
16:50314061:AG:A	donor_loss	1.0000
16:50314062:G:GT	donor_loss	1.0000
16:50314063:GTA:G	donor_loss	1.0000
16:50314286:CCGCA:C	acceptor_loss	1.0000
16:50314288:GCAGG:G	acceptor_loss	1.0000
16:50314290:A:AG	acceptor_gain	1.0000
16:50314291:G:A	acceptor_loss	1.0000
16:50314291:G:GG	acceptor_gain	1.0000
16:50314291:GGA:G	acceptor_gain	1.0000
16:50314353:G:GG	donor_gain	1.0000
16:50314403:GTCG:G	donor_gain	1.0000
16:50314406:GG:G	donor_loss	1.0000
16:50314407:G:GA	donor_loss	1.0000
16:50314407:G:GG	donor_gain	1.0000
16:50314408:TGAG:T	donor_loss	1.0000
16:50315354:TTCA:T	acceptor_loss	1.0000
16:50315357:A:AC	acceptor_loss	1.0000
16:50315357:A:AG	acceptor_gain	1.0000
16:50315357:AG:A	acceptor_gain	1.0000
16:50315358:G:GG	acceptor_gain	1.0000
16:50315358:GG:G	acceptor_gain	1.0000
16:50315358:GGT:G	acceptor_gain	1.0000

AlphaMissense

4352 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
16:50334879:A:G	L240P	1.000
16:50339995:C:T	G228E	1.000
16:50339996:C:G	G228R	1.000
16:50339996:C:T	G228R	1.000
16:50340007:A:G	L224P	1.000
16:50340016:G:T	A221E	1.000
16:50340017:C:G	A221P	1.000
16:50340029:A:C	Y217D	1.000
16:50340029:A:G	Y217H	1.000
16:50340034:G:A	T215I	1.000
16:50340045:A:C	N211K	1.000
16:50340045:A:T	N211K	1.000
16:50340047:T:C	N211D	1.000
16:50340050:A:C	Y210D	1.000
16:50340058:G:T	A207D	1.000
16:50340066:A:C	C204W	1.000
16:50340067:C:T	C204Y	1.000
16:50340068:A:G	C204R	1.000
16:50350112:A:G	Y168H	1.000
16:50350120:G:T	A165D	1.000
16:50350135:A:T	V160E	1.000
16:50350146:A:C	F156L	1.000
16:50350146:A:T	F156L	1.000
16:50350147:A:G	F156S	1.000
16:50350148:A:G	F156L	1.000
16:50350164:T:A	K150N	1.000
16:50350164:T:G	K150N	1.000
16:50350165:T:A	K150I	1.000
16:50354431:A:G	L147S	1.000
16:50354443:A:G	L143P	1.000

dbSNP variants (sampled 300 via entrez): RS1000015838 (16:50330309 G>A), RS1000031011 (16:50336663 G>A), RS1000118189 (16:50330323 T>C), RS1000145907 (16:50364375 C>T), RS1000149866 (16:50368898 G>A,C,T), RS1000152663 (16:50330051 A>T), RS1000183954 (16:50316571 C>T), RS1000232181 (16:50336591 AAAC>A), RS1000292453 (16:50323686 A>G,T), RS1000295133 (16:50362312 C>A,T), RS1000325801 (16:50362614 C>T), RS1000340364 (16:50317054 G>A), RS1000350988 (16:50358312 C>G,T), RS1000378136 (16:50316783 C>CTTTT), RS1000379099 (16:50368488 G>A)

Disease associations

OMIM: gene MIM:618489 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): granular cell cancer (MONDO:0003252)

Orphanet (0):

HPO phenotypes

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

GWAS associations

4 associations (top):

Study	Trait	p-value
GCST002207_11	Liver enzyme levels (alanine transaminase)	4.000000e-06
GCST006408_14	Allergic sensitization	4.000000e-07
GCST007343_3	Epilepsy	4.000000e-08
GCST007932_79	Medication use (thyroid preparations)	5.000000e-10

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0005298	allergic sensitization measurement
EFO:0009933	Thyroid preparation use measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (5): CHEMBL3085622 (SINGLE PROTEIN), CHEMBL5291686 (PROTEIN-PROTEIN INTERACTION), CHEMBL5291696 (PROTEIN-PROTEIN INTERACTION), CHEMBL5291945 (SELECTIVITY GROUP), CHEMBL5291966 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 79,020 (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
CHEMBL535	SUNITINIB	4	79,020

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: enzyme — Bromodomain kinase (BRDK) family

Most potent curated ligand interactions (3 total), top 3:

Ligand	Action	Affinity	Parameter
BI-9564	Inhibition	6.62	pKd
TP-472	Inhibition	6.47	pIC50
LP99	Inhibition	6.0	pKd

ChEMBL bioactivities

93 potent at pChembl≥5 of 103 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.52	Kd	0.3	nM	CHEMBL3823478
9.50	Kd	0.3162	nM	CHEMBL3823478
9.12	Kd	0.76	nM	CHEMBL4872300
8.35	EC50	4.5	nM	CHEMBL5182441
7.60	Ki	25.12	nM	CHEMBL4648548
7.46	EC50	34.5	nM	CHEMBL5182441
7.39	IC50	41	nM	CHEMBL3823599
7.38	IC50	42	nM	CHEMBL3824146
7.15	IC50	71	nM	CHEMBL3823478
7.14	Kd	73	nM	CHEMBL3823101
7.10	Kd	79.43	nM	CHEMBL3823101
7.09	IC50	82	nM	CHEMBL4102050
7.00	IC50	100	nM	CHEMBL4643109
7.00	Kd	100	nM	CHEMBL4635496
6.97	IC50	108	nM	CHEMBL3824146
6.96	Kd	110	nM	CHEMBL5268484
6.93	IC50	117	nM	CHEMBL3823478
6.92	Kd	121	nM	CHEMBL3823478
6.90	Kd	125	nM	CHEMBL5083849
6.85	IC50	140	nM	CHEMBL3752151
6.83	Kd	148	nM	CHEMBL3769507
6.77	Ki	170	nM	CHEMBL5413197
6.73	IC50	188	nM	CHEMBL3824312
6.70	Kd	200	nM	CHEMBL5270178
6.64	IC50	230	nM	CHEMBL3822990
6.64	Kd	230	nM	CHEMBL5080049
6.62	Kd	239	nM	CHEMBL3823101
6.62	IC50	240	nM	CHEMBL3823697
6.54	Kd	290	nM	CHEMBL5413197
6.52	Ki	300	nM	CHEMBL3823478
6.51	Ki	310	nM	CHEMBL5434122
6.50	Kd	316.2	nM	CHEMBL4065619
6.47	Kd	340	nM	CHEMBL4065619
6.47	Kd	340	nM	CHEMBL5282240
6.47	Kd	340	nM	CHEMBL5412877
6.43	Kd	368	nM	CHEMBL3740819
6.41	Kd	392	nM	CHEMBL3133807
6.41	Kd	390	nM	CHEMBL3769507
6.40	Kd	398.1	nM	CHEMBL3769507
6.38	Kd	418	nM	CHEMBL3823101
6.37	Kd	430	nM	CHEMBL5439294
6.30	Ki	501.2	nM	CHEMBL4639574
6.28	Kd	520	nM	CHEMBL5289762
6.25	Kd	556	nM	CHEMBL4065619
6.19	IC50	644	nM	CHEMBL3823697
6.10	EC50	800	nM	CHEMBL3823101
6.09	Kd	812.8	nM	CHEMBL3356143
6.07	Ki	860	nM	CHEMBL5407972
6.07	IC50	850	nM	CHEMBL5413197
6.04	Kd	909	nM	CHEMBL3753082

PubChem BioAssay actives

86 with measured affinity, of 311 total; 47 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-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one	1309649: Binding affinity to human BRD7 by BROMOScan analysis	kd	0.0003	uM
5-[4-(2-aminoethyl)anilino]-4-chloro-2-methylpyridazin-3-one	1769027: Binding affinity to BRD7 (unknown origin) by BROMOscan method	kd	0.0008	uM
(2S,4R)-N-[[2-[5-[4-[[2,6-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl]piperazin-1-yl]pentoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-1-[(2S)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide	1960450: PROTAC activity at VHL/BRD7 in human Ri-1 cells assessed as degradation of BRD7 protein incubated for 8 hrs by Western blot analysis	ec50	0.0045	uM
2,4-dimethyl-5-[[2-(4-methylpiperazin-1-yl)phenyl]methylamino]pyridazin-3-one	1655019: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	ki	0.0251	uM
5-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-1,3,4-trimethylpyridin-2-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	0.0410	uM
4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methylisoquinolin-1-one	2191068: Inhibition of BRD7 (unknown origin) using histone H3 K9/14/18/23Ac (1-28) peptide as substrate incubated for 60 mins by alpha-screen assay	ic50	0.0420	uM
4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one	1309649: Binding affinity to human BRD7 by BROMOScan analysis	kd	0.0730	uM
4-cyano-N-(1,3-dimethyl-2-oxoquinolin-6-yl)benzenesulfonamide	1483628: Inhibition of human BRD7 expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay	ic50	0.0820	uM
6-[(E)-but-2-enyl]-4-[2,5-dimethoxy-4-(morpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one	1655010: Binding affinity to BRD7 (unknown origin)	kd	0.1000	uM
2-[[2,5-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl-methylamino]-N-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide	1655010: Binding affinity to BRD7 (unknown origin)	ic50	0.1000	uM
6-[(E)-but-2-enyl]-4-[2,5-dimethoxy-4-(morpholine-4-carbonyl)phenyl]-2-methyl-1H-pyrrolo[2,3-c]pyridin-7-one	1958292: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	kd	0.1100	uM
N-[2-[8-(hydroxyamino)-8-oxooctoxy]-5-morpholin-4-ylsulfonylphenyl]-3-methyl-4-oxo-5,6,7,8-tetrahydro-2H-cyclohepta[c]pyrrole-1-carboxamide	1832803: Binding affinity to human BRD7 assessed as dissociation constant by isothermal titration calorimetry assay	kd	0.1250	uM
4-cyano-N-(1,3-dimethyl-2-oxoquinolin-6-yl)-2-methoxybenzenesulfonamide	1475717: Inhibition of human BRD7 (125 to 254 residues) expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay	ic50	0.1400	uM
N’-(1,1-dioxothian-4-yl)-5-ethyl-4-oxo-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide	1561117: Binding affinity to recombinant human His-tagged BRD7 (129 to 250 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry	kd	0.1480	uM
7-(6-methoxy-2-methyl-3-pyridinyl)-1,4-dimethylquinolin-2-one	1976153: Displacement of FAM-labeled BI-FAMb from N-terminal His TEV-tagged human recombinant BRD7 bromodomain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	ki	0.1700	uM
8-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-6-methylpyrido[4,3-d]pyrimidin-5-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	0.1880	uM
6-[(E)-but-2-enyl]-4-[4-(morpholine-4-carbonyl)phenyl]-1H-pyrrolo[2,3-c]pyridin-7-one	1958292: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	kd	0.2000	uM
5-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-1,3-dimethylpyridin-2-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	0.2300	uM
N-[5-[3-[(E)-3-(hydroxyamino)-3-oxoprop-1-enyl]pyrrol-1-yl]sulfonyl-2-methoxyphenyl]-3-methyl-4-oxo-5,6,7,8-tetrahydro-2H-cyclohepta[c]pyrrole-1-carboxamide	1832803: Binding affinity to human BRD7 assessed as dissociation constant by isothermal titration calorimetry assay	kd	0.2300	uM
5-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-1,3,6-trimethylpyridin-2-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	0.2400	uM
4-(2,6-dimethoxy-3-pyridinyl)-2-methylisoquinolin-1-one	1976153: Displacement of FAM-labeled BI-FAMb from N-terminal His TEV-tagged human recombinant BRD7 bromodomain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	ki	0.3100	uM
3-(6-acetylpyrrolo[1,2-a]pyrimidin-8-yl)-N-cyclopropyl-4-methylbenzamide	1655010: Binding affinity to BRD7 (unknown origin)	kd	0.3162	uM
6-[(E)-but-2-enyl]-4-[4-(2-hydroxypropan-2-yl)-2-methoxyphenyl]-1H-pyrrolo[2,3-c]pyridin-7-one	1958292: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	kd	0.3400	uM
7-(2,6-dimethoxy-3-pyridinyl)-1,4-dimethylquinolin-2-one	1976149: Binding affinity to human partial length BRD7 bromodomain (125 to 254 residues) expressed in mammalian expression system by BROMOscan KdELECT analysis	kd	0.3400	uM
ethyl N-[6-[3-(methanesulfonamido)-4-methylphenyl]-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate	1561117: Binding affinity to recombinant human His-tagged BRD7 (129 to 250 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry	kd	0.3920	uM
1-(5-amino-2-chlorophenyl)-3-methyl-5,6,7,8-tetrahydro-2H-cyclohepta[c]pyrrol-4-one	1995395: Binding affinity to BRD7 (unknown origin) assessed as dissociation constant by site-directed competition binding assay	kd	0.4300	uM
4-butyl-2-methyl-5-[[2-(4-methylpiperazin-1-yl)phenyl]methylamino]pyridazin-3-one	1655019: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	ki	0.5012	uM
6-[(E)-but-2-enyl]-4-[4-(2-hydroxypropan-2-yl)-2,5-dimethoxyphenyl]-2-methyl-1H-pyrrolo[2,3-c]pyridin-7-one	1958292: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	kd	0.5200	uM
4-(3,5-dimethylphenyl)-2-methylisoquinolin-1-one	1976153: Displacement of FAM-labeled BI-FAMb from N-terminal His TEV-tagged human recombinant BRD7 bromodomain expressed in Escherichia coli BL21(DE3) by competitive fluorescence polarization assay	ki	0.8600	uM
N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxoquinolin-7-yl)-6-oxopiperidin-3-yl]-2-methylpropane-1-sulfonamide	1309643: Inhibition of human BRD7 by VP-ITC method	kd	0.9090	uM
1-(5-amino-2-chlorophenyl)-3-propyl-5,6,7,8-tetrahydro-2H-cyclohepta[c]pyrrol-4-one	1995395: Binding affinity to BRD7 (unknown origin) assessed as dissociation constant by site-directed competition binding assay	kd	1.1000	uM
4-[(2-amino-4-hydroxy-3,5-dimethylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide	1054709: Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay	ki	1.4300	uM
4-[(2-amino-3-chloro-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide	1054709: Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay	ki	1.4300	uM
4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,6-naphthyridin-1-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	1.5650	uM
5-[8-[5-acetyl-1-(oxan-4-yl)-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]isoquinolin-3-yl]-N-methylpyridine-2-carboxamide	1372252: Binding affinity to human partial length BRD7 (L125 to R254 residues) expressed in mammalian expression system by BROMOscan assay	kd	1.8000	uM
8-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-6-methyl-1,6-naphthyridin-5-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	2.4750	uM
4-[(2-amino-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide	1054709: Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay	ki	2.7200	uM
5-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-1,3,4-trimethylpyridin-2-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	2.9760	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	1234398: Binding affinity to BRD7 in human HUT78 cells incubated for 45 mins by mass spectrometry based bromosphere chemoproteomic assay	kd	3.1623	uM
5-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-1,3,6-trimethylpyridin-2-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	3.2830	uM
4-[(4-hydroxy-3,5-dimethylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamide	1054709: Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay	ki	3.5400	uM
5-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-7-methyl-1,7-naphthyridin-8-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	3.7250	uM
(1Z)-1-(3-ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one	1561117: Binding affinity to recombinant human His-tagged BRD7 (129 to 250 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry	kd	4.2000	uM
4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methylisoquinolin-1-one	1309635: Inhibition of human N-terminal GST-tagged BRD7 expressed in Escherichia coli using tetra-acetylated histone H4 measured after 60 mins by AlphaScreen assay	ic50	4.3070	uM
4-acetyl-N-[(2,8-dihydroxynaphthalen-1-yl)methyl]-3-ethyl-5-methylpyrrolidine-2-carboxamide	2027182: Binding affinity to BRD7 (unknown origin) assessed as dissociation constant	kd	4.5000	uM
5-[7-(difluoromethyl)-6-(1-methylpyrazol-4-yl)-3,4-dihydro-2H-quinolin-1-yl]-N-methyl-7-propan-2-yl-1H-pyrrolo[2,3-c]pyridine-3-carboxamide	1477696: Binding affinity to human BRD7 (L125 to R254) expressed in mammalian cells by BromoScan assay	kd	5.1000	uM
4-acetyl-3-ethyl-N-[5-[(E)-3-(hydroxyamino)-3-oxoprop-1-enyl]-2-methoxyphenyl]-5-methyl-1H-pyrrole-2-carboxamide	1832803: Binding affinity to human BRD7 assessed as dissociation constant by isothermal titration calorimetry assay	kd	8.5000	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	affects cotreatment, increases expression, decreases expression	2
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
TAK-243	decreases sumoylation	1
methylmercuric chloride	decreases expression	1
lasiocarpine	decreases expression, increases metabolic processing	1
triphenyl phosphate	affects expression	1
pirinixic acid	affects binding, increases activity, increases expression	1
beta-methylcholine	affects expression	1
di-n-butylphosphoric acid	affects expression	1
pentabromodiphenyl ether	decreases expression	1
CGP 52608	affects binding, increases reaction	1
2,2’,4,4’-tetrabromodiphenyl ether	decreases expression	1
bisphenol S	decreases methylation	1
Acetaminophen	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Benzo(a)pyrene	affects methylation	1
Caffeine	decreases phosphorylation	1
Dexamethasone	affects cotreatment, increases expression	1
Doxorubicin	increases expression	1
Indomethacin	affects cotreatment, increases expression	1
Lead	increases expression	1
Methyl Methanesulfonate	increases expression	1
Ozone	affects expression, increases abundance	1
Quercetin	decreases expression	1
1-Methyl-3-isobutylxanthine	affects cotreatment, increases expression	1
Monocrotaline	decreases expression, increases metabolic processing	1
Antirheumatic Agents	increases expression	1
Copper Sulfate	decreases expression	1

ChEMBL screening assays

152 unique, capped per target: 146 binding, 3 admet, 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL3089618	Binding	Displacement of fluorescein-labeled MS226 from recombinant human BRD7 after 1 hr by fluorescence anisotropy assay	Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. — J Med Chem
CHEMBL4358807	ADMET	Binding affinity to recombinant human His-tagged BRD7 (129 to 250 residues) expressed in Escherichia coli BL21 DE3 assessed as change in melting temperature at 100 uM by SYPRO orange dye based differential scanning fluorimetry	Structural Basis of Inhibitor Selectivity in the BRD7/9 Subfamily of Bromodomains. — J Med Chem
CHEMBL5210054	Functional	Affinity Phenotypic Cellular interaction (CellTiter-Glo assay (Promega, EOL-1 cell proliferation)) EUB0000004c BRD7	Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3

Cellosaurus cell lines

22 cell lines: 22 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_4972	MHCC97-H	Cancer cell line	Male
CVCL_6832	HCCLM3	Cancer cell line	Male
CVCL_7680	HCCLM6	Cancer cell line	Male
CVCL_A5CU	HCCLM9	Cancer cell line	Male
CVCL_A9LY	MHCC97H-GFP-LC3	Cancer cell line	Male
CVCL_B8C6	Abcam HCT 116 BRD7 KO	Cancer cell line	Male
CVCL_B8T5	Abcam MCF-7 BRD7 KO	Cancer cell line	Female
CVCL_B9EC	Abcam A-549 BRD7 KO	Cancer cell line	Male
CVCL_D6B7	HyCyte HCCLM3 KO-hHSPA4	Cancer cell line	Male
CVCL_D6B8	HyCyte HCCLM3 KO-hUSP22	Cancer cell line	Male

Clinical trials (associated diseases)

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