PBRM1

Summary

PBRM1 (polybromo 1, HGNC:30064) is a protein-coding gene on chromosome 3p21.1, encoding Protein polybromo-1 (Q86U86). Involved in transcriptional activation and repression of select genes by chromatin remodeling (alteration of DNA-nucleosome topology). In precision oncology, PBRM1 Mutation confers sensitivity to Sunitinib + Everolimus in Renal Cell Carcinoma (CIViC Level B); 1 further curated variant–drug associations are listed below.

This locus encodes a subunit of ATP-dependent chromatin-remodeling complexes. The encoded protein has been identified as in integral component of complexes necessary for ligand-dependent transcriptional activation by nuclear hormone receptors. Mutations at this locus have been associated with primary clear cell renal cell carcinoma.

Source: NCBI Gene 55193 — RefSeq curated summary.

At a glance

• GWAS associations: 70
• Clinical variants (ClinVar): 146 total — 1 pathogenic
• Phenotypes (HPO): 2
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 2 curated variant–drug associations
• Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 15 cancer types
• MANE Select transcript: NM_001405607

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:30064
Approved symbol	PBRM1
Name	polybromo 1
Location	3p21.1
Locus type	gene with protein product
Status	Approved
Aliases	BAF180, PB1, SMARCH1
Ensembl gene	ENSG00000163939
Ensembl biotype	protein_coding
OMIM	606083
Entrez	55193

Gene structure

Transcript identifiers

Ensembl transcripts: 33 — 30 protein_coding, 2 retained_intron, 1 nonsense_mediated_decay

ENST00000296302, ENST00000337303, ENST00000356770, ENST00000394830, ENST00000409057, ENST00000409114, ENST00000409767, ENST00000410007, ENST00000412587, ENST00000420148, ENST00000423351, ENST00000424867, ENST00000431678, ENST00000439181, ENST00000446103, ENST00000449505, ENST00000450271, ENST00000458294, ENST00000462207, ENST00000480064, ENST00000707071, ENST00000875042, ENST00000875043, ENST00000923715, ENST00000923716, ENST00000923717, ENST00000923718, ENST00000923719, ENST00000923720, ENST00000923721, ENST00000966403, ENST00000966404, ENST00000966405

RefSeq mRNA: 131 — MANE Select: NM_001405607 NM_001350074, NM_001350075, NM_001350076, NM_001350077, NM_001350078, NM_001350079, NM_001366070, NM_001366071, NM_001366072, NM_001366073, NM_001366074, NM_001366075, NM_001366076, NM_001394867, NM_001394868, NM_001394869, NM_001394870, NM_001394871, NM_001394872, NM_001394873, NM_001394874, NM_001394875, NM_001394876, NM_001394877, NM_001394878, NM_001394879, NM_001400470, NM_001400471, NM_001400472, NM_001400473, NM_001400474, NM_001400475, NM_001400479, NM_001400481, NM_001400484, NM_001400487, NM_001400490, NM_001400496, NM_001400500, NM_001400501, NM_001400504, NM_001405552, NM_001405553, NM_001405554, NM_001405555, NM_001405556, NM_001405557, NM_001405558, NM_001405559, NM_001405560, NM_001405561, NM_001405563, NM_001405564, NM_001405565, NM_001405566, NM_001405567, NM_001405568, NM_001405569, NM_001405570, NM_001405571, NM_001405572, NM_001405573, NM_001405574, NM_001405575, NM_001405576, NM_001405577, NM_001405578, NM_001405579, NM_001405580, NM_001405581, NM_001405582, NM_001405583, NM_001405584, NM_001405585, NM_001405586, NM_001405587, NM_001405588, NM_001405589, NM_001405590, NM_001405591, NM_001405592, NM_001405593, NM_001405594, NM_001405595, NM_001405596, NM_001405597, NM_001405598, NM_001405599, NM_001405600, NM_001405601, NM_001405602, NM_001405603, NM_001405604, NM_001405605, NM_001405606, NM_001405607, NM_001405608, NM_001405609, NM_001405610, NM_001405611, NM_001405612, NM_001405613, NM_001405617, NM_001405618, NM_001405619, NM_001405620, NM_001405621, NM_001405622, NM_001405623, NM_001405624, NM_001405625, NM_001405626, NM_001405627, NM_001405628, NM_001405629, NM_001405630, NM_001405631, NM_001405632, NM_001405633, NM_001405634, NM_001405635, NM_001405636, NM_001405637, NM_001405638, NM_001405639, NM_001405640, NM_001405641, NM_001405642, NM_001405643, NM_018313, NM_181042

CCDS: CCDS2859, CCDS2860, CCDS43099, CCDS87087, CCDS93285, CCDS93286

Canonical transcript exons

ENST00000707071 — 32 exons

Exon	Start	End
ENSE00001178725	52658199	52658315
ENSE00001290630	52615351	52615456
ENSE00001302735	52634602	52634815
ENSE00001306341	52627273	52627370
ENSE00001311253	52617262	52617538
ENSE00001321987	52609313	52609955
ENSE00001324274	52628894	52629035
ENSE00001325694	52641954	52642045
ENSE00001338851	52558249	52558413
ENSE00001342942	52643248	52643343
ENSE00001342943	52644704	52644789
ENSE00001342944	52648344	52648442
ENSE00001342945	52651742	52651810
ENSE00001342949	52662133	52662276
ENSE00001606104	52678500	52678597
ENSE00001784711	52668498	52668645
ENSE00001899954	52679574	52679726
ENSE00003461027	52587353	52587510
ENSE00003468419	52579054	52579199
ENSE00003551711	52550747	52550817
ENSE00003565445	52564050	52564233
ENSE00003572789	52589070	52589255
ENSE00003596302	52550421	52550637
ENSE00003598212	52561767	52561968
ENSE00003598635	52576541	52576698
ENSE00003603129	52586425	52586688
ENSE00003604738	52563283	52563493
ENSE00003644261	52545367	52548235
ENSE00003669656	52554724	52554879
ENSE00003680361	52603521	52603732
ENSE00003998141	52624897	52624941
ENSE00003998142	52685749	52685913

Expression profiles

Bgee: expression breadth ubiquitous, 289 present calls, max score 96.35.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 21.5095 / max 265.8441, expressed in 1814 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
42462	14.1883	1792
42461	3.5340	1355
42459	2.7175	1346
42460	1.0152	602
42451	0.0392	6
42453	0.0153	5

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
cortical plate	UBERON:0005343	96.35	gold quality
ganglionic eminence	UBERON:0004023	95.78	gold quality
amniotic fluid	UBERON:0000173	95.45	gold quality
sural nerve	UBERON:0015488	95.43	gold quality
penis	UBERON:0000989	94.72	gold quality
saphenous vein	UBERON:0007318	93.98	gold quality
calcaneal tendon	UBERON:0003701	93.58	gold quality
mucosa of paranasal sinus	UBERON:0005030	93.57	gold quality
thymus	UBERON:0002370	93.02	gold quality
epithelium of nasopharynx	UBERON:0001951	92.89	gold quality
nasopharynx	UBERON:0001728	92.87	gold quality
adrenal tissue	UBERON:0018303	92.76	gold quality
germinal epithelium of ovary	UBERON:0001304	92.75	gold quality
ventricular zone	UBERON:0003053	92.63	gold quality
synovial joint	UBERON:0002217	92.54	gold quality
urethra	UBERON:0000057	92.47	gold quality
embryo	UBERON:0000922	92.28	gold quality
tonsil	UBERON:0002372	92.14	gold quality
trabecular bone tissue	UBERON:0002483	92.06	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	91.99	gold quality
cerebellar vermis	UBERON:0004720	91.97	gold quality
corpus callosum	UBERON:0002336	91.81	gold quality
heart right ventricle	UBERON:0002080	91.74	gold quality
medial globus pallidus	UBERON:0002477	91.74	gold quality
tendon	UBERON:0000043	91.68	gold quality
superficial temporal artery	UBERON:0001614	91.66	gold quality
bone marrow cell	CL:0002092	91.53	gold quality
colonic epithelium	UBERON:0000397	91.45	gold quality
bone marrow	UBERON:0002371	91.13	gold quality
nasal cavity epithelium	UBERON:0005384	91.10	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	11.25

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

9 targets.

Target	Regulation
CDKN1A	Activation
CRABP2	Activation
CREBBP
CSF2
IL10
RARB	Activation
S100A13	Activation
SMARCA2
SMARCA4

Literature-anchored findings (GeneRIF, showing 40)

• cDNA cloning; the hPB1 gene is located on chromosome 3p21, where the tumor suppressor genes for breast, lung and kidney cancers have been mapped (PMID:12487023)
• We conclude that abnormalities of BAF180 are not frequently involved in the pathogenesis of lung cancer. (PMID:15735765)
• Results indicate that single bromodomains bind specific acetyl-lysine sites within the histone 3 tail with sub-micromolar affinity. (PMID:17320048)
• studies on how Pb1, and the broader class of bromodomain proteins, directs multisubunit chromatin remodeling complexes to specific acetyl-nucleosome sites (PMID:18191465)
• BAF180 suppresses tumorigenesis, at least in part, through its ability to regulate p21. (PMID:18339845)
• Bromodomain 2 of Polybromo protein preferentially recognizes acetylated lysine 14 of histone H3 (H3K14ac), a post-translational mark known for gene transcriptional activation. (PMID:20368734)
• 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)
• identification of the SWI/SNF chromatin remodelling complex gene PBRM1 (ref. 4) as a second major ccRCC cancer gene, with truncating mutations in 41% (92/227) of cases (PMID:21248752)
• PBRM1 was found to be mutated in 88 of 257 cases of clear cell renal cell carcinoma. (PMID:21604427)
• The role of syncytin-1 and Pb1 in cell-cell fusion was studied using lentiviral vectors that express short hairpin RNAs for stable knockdown of both genes. (PMID:22573740)
• Functional inactivation of PBRM1 in the context of VHL loss-of-function may represent a key event in the development of an aggressive tumor behavior. (PMID:22949125)
• The median overall survival in the UTSW cohort was significantly shorter for patients with BAP1-mutant tumours (4.6 years; 95% CI 2.1-7.2), than for patients with PBRM1-mutant tumours (10.6 years; 9.8-11.5). (PMID:23333114)
• PBRM1, KDM6A, SETD2 and BAP1 were unmethylated in all tumor and normal specimens. (PMID:23644518)
• the evidence that implicated PBRM1 and BAP1 as renal cancer driver genes, provide an update on the function of the gene products, and speculate on how mutations in these genes may be exploited therapeutically. (PMID:23867514)
• Mutation frequencies among CT images of clear cell RCCs were as follows: PBRM1, 28.8% (67 of 233). (PMID:24029645)
• PBRM1-negative expression is a markedly poor prognosis event in clear cell renal cell carcinoma. (PMID:24053427)
• PBRM1 (33%) mutations were identified in ccRCCs. (PMID:24166983)
• Frequent inactivating mutations in multiple chromatin-remodeling genes (including BAP1, ARID1A and PBRM1), and mutation in one of these genes occurred in almost half of the carcinomas sequenced. (PMID:24185509)
• Data demonstrate a function for BAF180 in promoting genome stability that is distinct from its well-characterized role in transcriptional regulation. (PMID:24613357)
• Of the 23 epithelioid sarcoma cases, 19 showed a loss of PBRM1, and 18 a loss of INI1. In 17 cases, loss of both proteins was observed. The pattern of PBRM1 expression was similar to that of INI1: not correlated with changes in cellular morphology. (PMID:25200863)
• Data suggest biallelic inactivation of PBRM1 or BAP1 is less common in non-ccRCC when compared with ccRCC tumors. Findings suggest loss of PBRM1 or BAP1 are key events in ccRCC, whereas other pathways may support tumorigenesis in non-ccRCC subtypes. (PMID:25465300)
• We report, for the first time, co-inactivation and frequent mutations of SMARCB1, SMARCA2 and PBRM1 in MRTs. (PMID:25496315)
• The subsequent validation study on 68 LCBs identified recurrent mutations in TERT promoter, chromatin regulators (BAP1, PBRM1 and ARID2), a synapse organization gene (PCLO), IDH genes and KRAS. (PMID:25636086)
• It evaluates the PB1 domain proteins as a family in the context of multiple phenotypic readouts in EC function as well as evaluate them as drug targets against disease. (PMID:25686626)
• We show for the first time that an inherited mutation in PBRM1 predisposes to RCC. (PMID:25911086)
• PBRM1 could block the G2/M transition by repressing cyclin B1. The data indicated that PBRM1 functions as a tumor suppressor in bladder cancer by repressing cyclin B1 expression. (PMID:25978027)
• Decreased expression of PBRM1 predicts unfavorable clinical outcome in patients with ccRCC. (PMID:26003625)
• The expression of BAF180 promotes UV-induced PCNA ubiquitination during S phase. (PMID:26117423)
• our data describe a close interrelation between p53 and PBRM1 in renal cell carcinomas (PMID:26178300)
• PBRM1 expression identified 4 clinical subgroups of patients with clear cell renal cell carcinoma who had divergent clinical outcomes. (PMID:26300218)
• Use bioinformatic tools to predict the molecular effects of all mutations lying in PBRM1 genes. (PMID:26452128)
• PBRM1 might involve in the development and progression of breast cancer as a tumor suppressor, and thereby may be a valuable prognostic marker for breast cancer patients. (PMID:26464681)
• Functionally, suppression of PBRM1 expression promoted cell proliferation and cell cycle progression (PMID:26634388)
• PBRM1 gene deletion is associated with chordoma. (PMID:27072194)
• PBRM1 re-expression led to upregulation of genes involved in cellular adhesion, carbohydrate metabolism, apoptotic process and response to hypoxia, and a downregulation of genes involved in different stages of cell division. (PMID:27100670)
• Synthetic lethality screening identifies TIP60-dependent radiation sensitivity in the absence of BAF180. (PMID:27461052)
• our integrative analysis suggested that methylation and miRNA alterations were likely the downstream events associated with PBRM1 truncation mutations. In summary, this study provided some important insights into the understanding of tumorigenesis driven by PBRM1 truncated mutations in Clear cell renal cell carcinoma (ccRCC). The approach may be applied to many driver genes in various cancers. (PMID:27556922)
• BAP1 and PBRM1 loss is seen frequently in intrahepatic cholangiocarcinoma (PMID:27864835)
• PBRM1 mutation is associated with small Cell Lung Cancer. (PMID:28007623)
• conclude that four of the BDs act together to target PBRM1 to sites on chromatin; when a single BD is mutated, PBRM1 no longer controls gene expression properly, leading to increased cell proliferation (PMID:28053089)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	pbrm1	ENSDARG00000003877
danio_rerio	pbrm1l	ENSDARG00000077038
mus_musculus	Pbrm1	ENSMUSG00000042323
rattus_norvegicus	Pbrm1	ENSRNOG00000028227
drosophila_melanogaster	polybromo	FBGN0039227
caenorhabditis_elegans	pbrm-1	WBGENE00007042

Protein

Protein identifiers

Protein polybromo-1 — Q86U86 (reviewed: Q86U86)

Alternative names: BRG1-associated factor 180, Polybromo-1D

All UniProt accessions (10): A0A9L9PXL4, C9J053, C9J409, C9J9L6, C9JCJ2, C9JPI5, C9JQF1, Q86U86, E7EVG2, H0Y5B5

UniProt curated annotations — full annotation on UniProt →

Function. Involved in transcriptional activation and repression of select genes by chromatin remodeling (alteration of DNA-nucleosome topology). Required for the stability of the SWI/SNF chromatin remodeling complex SWI/SNF-B (PBAF). Acts as a negative regulator of cell proliferation.

Subunit / interactions. Component of the SWI/SNF-B (PBAF) chromatin remodeling complex, at least composed of SMARCA4/BRG1, SMARCB1/BAF47/SNF5, ACTL6A/BAF53A or ACTL6B/BAF53B, SMARCE1/BAF57, SMARCD1/BAF60A, SMARCD2/BAF60B, perhaps SMARCD3/BAF60C, SMARCC1/BAF155, SMARCC2/BAF170, PBRM1/BAF180, ARID2/BAF200 and actin. Interacts with PHF10/BAF45A. Interacts with acetylated ‘Lys-14’ of histone H3 (H3K14ac), and may also interact with other acetylated or methylated Lys residues on histone H3.

Subcellular location. Nucleus.

Tissue specificity. Widely expressed.

Disease relevance. Renal cell carcinoma (RCC) [MIM:144700] Renal cell carcinoma is a heterogeneous group of sporadic or hereditary carcinoma derived from cells of the proximal renal tubular epithelium. It is subclassified into clear cell renal carcinoma (non-papillary carcinoma), papillary renal cell carcinoma, chromophobe renal cell carcinoma, collecting duct carcinoma with medullary carcinoma of the kidney, and unclassified renal cell carcinoma. Clear cell renal cell carcinoma is the most common subtype. The disease is caused by variants affecting the gene represented in this entry.

Isoforms (9)

UniProt ID	Names	Canonical?
Q86U86-1	1	yes
Q86U86-2	2
Q86U86-3	3
Q86U86-4	4
Q86U86-5	5
Q86U86-6	6
Q86U86-7	7
Q86U86-8	8
Q86U86-9	9

RefSeq proteins (131): NP_001337003, NP_001337004, NP_001337005, NP_001337006, NP_001337007, NP_001337008, NP_001352999, NP_001353000, NP_001353001, NP_001353002, NP_001353003, NP_001353004, NP_001353005, NP_001381796, NP_001381797, NP_001381798, NP_001381799, NP_001381800, NP_001381801, NP_001381802, NP_001381803, NP_001381804, NP_001381805, NP_001381806, NP_001381807, NP_001381808, NP_001387399, NP_001387400, NP_001387401, NP_001387402, NP_001387403, NP_001387404, NP_001387408, NP_001387410, NP_001387413, NP_001387416, NP_001387419, NP_001387425, NP_001387429, NP_001387430, NP_001387433, NP_001392481, NP_001392482, NP_001392483, NP_001392484, NP_001392485, NP_001392486, NP_001392487, NP_001392488, NP_001392489, NP_001392490, NP_001392492, NP_001392493, NP_001392494, NP_001392495, NP_001392496, NP_001392497, NP_001392498, NP_001392499, NP_001392500, NP_001392501, NP_001392502, NP_001392503, NP_001392504, NP_001392505, NP_001392506, NP_001392507, NP_001392508, NP_001392509, NP_001392510, NP_001392511, NP_001392512, NP_001392513, NP_001392514, NP_001392515, NP_001392516, NP_001392517, NP_001392518, NP_001392519, NP_001392520, NP_001392521, NP_001392522, NP_001392523, NP_001392524, NP_001392525, NP_001392526, NP_001392527, NP_001392528, NP_001392529, NP_001392530, NP_001392531, NP_001392532, NP_001392533, NP_001392534, NP_001392535, NP_001392536, NP_001392537, NP_001392538, NP_001392539, NP_001392540, NP_001392541, NP_001392542, NP_001392546, NP_001392547, NP_001392548, NP_001392549, NP_001392550, NP_001392551, NP_001392552, NP_001392553, NP_001392554, NP_001392555, NP_001392556, NP_001392557, NP_001392558, NP_001392559, NP_001392560, NP_001392561, NP_001392562, NP_001392563, NP_001392564, NP_001392565, NP_001392566, NP_001392567, NP_001392568, NP_001392569, NP_001392570, NP_001392571, NP_001392572, NP_060783, NP_851385 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR001025	BAH_dom	Domain
IPR001487	Bromodomain	Domain
IPR009071	HMG_box_dom	Domain
IPR018359	Bromodomain_CS	Conserved_site
IPR036427	Bromodomain-like_sf	Homologous_superfamily
IPR036910	HMG_box_dom_sf	Homologous_superfamily
IPR037382	Rsc/polybromo	Family
IPR037968	PBRM1_BD5	Domain
IPR043151	BAH_sf	Homologous_superfamily

Pfam: PF00439, PF00505, PF01426

UniProt features (199 total): helix 48, sequence variant 38, modified residue 23, cross-link 19, strand 18, sequence conflict 17, domain 8, region of interest 8, turn 7, splice variant 7, compositionally biased region 4, chain 1, DNA-binding region 1

Structure

Experimental structures (PDB)

30 structures.

PDB	Method	Resolution (Å)
6ZNV	X-RAY DIFFRACTION	1.14
5FH7	X-RAY DIFFRACTION	1.47
3LJW	X-RAY DIFFRACTION	1.5
5FH8	X-RAY DIFFRACTION	1.55
3HMF	X-RAY DIFFRACTION	1.63
3IU5	X-RAY DIFFRACTION	1.63
3MB4	X-RAY DIFFRACTION	1.66
6ZS3	X-RAY DIFFRACTION	1.67
5HRV	X-RAY DIFFRACTION	1.7
5HRX	X-RAY DIFFRACTION	1.73
3G0J	X-RAY DIFFRACTION	1.78
4Q0N	X-RAY DIFFRACTION	1.78
8FTA	X-RAY DIFFRACTION	1.78
3IU6	X-RAY DIFFRACTION	1.79
5HRW	X-RAY DIFFRACTION	1.8
4Q0O	X-RAY DIFFRACTION	1.83
6OXB	X-RAY DIFFRACTION	1.86
5E7D	X-RAY DIFFRACTION	1.87
4Y03	X-RAY DIFFRACTION	1.94
6ZS4	X-RAY DIFFRACTION	2
5II1	X-RAY DIFFRACTION	2.02
6ZN6	X-RAY DIFFRACTION	2.02
5II2	X-RAY DIFFRACTION	2.1
3TLP	X-RAY DIFFRACTION	2.13
3K2J	X-RAY DIFFRACTION	2.2
5FH6	X-RAY DIFFRACTION	2.3
5IID	X-RAY DIFFRACTION	2.4
7VDV	ELECTRON MICROSCOPY	3.4
7Y8R	ELECTRON MICROSCOPY	4.4
2KTB	SOLUTION NMR

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q86U86-F1	74.32	0.41

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 (42): 10, 39, 131, 134, 178, 316, 319, 353, 355, 371, 375, 414, 498, 509, 636, 648, 689, 948, 987, 1119 …

Function

Pathways and Gene Ontology

Reactome pathways

3 pathways

ID	Pathway
R-HSA-3214858	RMTs methylate histone arginines
R-HSA-8939243	RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known
R-HSA-9933939	Formation of the polybromo-BAF (pBAF) complex

MSigDB gene sets: 253 (showing top): GOBP_REGULATION_OF_DOUBLE_STRAND_BREAK_REPAIR, GOBP_REGULATION_OF_CELL_ACTIVATION, E2F_Q4, GOBP_CHROMOSOME_ORGANIZATION, HORIUCHI_WTAP_TARGETS_DN, GOBP_POSITIVE_REGULATION_OF_HEMOPOIESIS, E2F4DP1_01, PAL_PRMT5_TARGETS_UP, GCANCTGNY_MYOD_Q6, GOBP_CELL_CYCLE_PHASE_TRANSITION, GRAESSMANN_APOPTOSIS_BY_DOXORUBICIN_DN, AP2_Q3, AATGGAG_MIR136, USF_C, GOBP_REGULATION_OF_DNA_REPAIR

GO Biological Process (15): mitotic cell cycle (GO:0000278), chromatin remodeling (GO:0006338), regulation of transcription by RNA polymerase II (GO:0006357), transcription elongation by RNA polymerase II (GO:0006368), negative regulation of cell population proliferation (GO:0008285), 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), regulation of G0 to G1 transition (GO:0070316), regulation of G1/S transition of mitotic cell cycle (GO:2000045), positive regulation of double-strand break repair (GO:2000781), regulation of nucleotide-excision repair (GO:2000819), chromatin organization (GO:0006325), positive regulation of dendritic spine development (GO:0060999)

GO Molecular Function (3): DNA binding (GO:0003677), chromatin binding (GO:0003682), protein binding (GO:0005515)

GO Cellular Component (9): nuclear chromosome (GO:0000228), kinetochore (GO:0000776), chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), nuclear matrix (GO:0016363), SWI/SNF complex (GO:0016514), RSC-type complex (GO:0016586), chromosome (GO:0005694)

Reactome top-level categories

Rollup of top-3 pathways:

Category	Pathways
Chromatin modifying enzymes	1
Transcriptional regulation by RUNX1	1
SWI/SNF chromatin remodelers	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
nuclear lumen	3
cellular anatomical structure	3
transcription by RNA polymerase II	2
regulation of mitotic cell cycle phase transition	2
positive regulation of developmental process	2
binding	2
chromosome	2
intracellular membraneless organelle	2
SWI/SNF superfamily-type complex	2
cell cycle	1
mitotic nuclear division	1
chromatin organization	1
regulation of DNA-templated transcription	1
DNA-templated transcription elongation	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	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
myoblast differentiation	1
positive regulation of cell differentiation	1
regulation of myoblast differentiation	1
regulation of cell cycle process	1
G0 to G1 transition	1
G1/S transition of mitotic cell cycle	1
regulation of cell cycle G1/S phase transition	1
double-strand break repair	1
positive regulation of DNA repair	1
regulation of double-strand break repair	1
regulation of DNA repair	1
nucleotide-excision repair	1
cellular component organization	1
dendritic spine development	1

Protein interactions and networks

STRING

2972 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
PBRM1	ARID2	Q68CP9	999
PBRM1	ARID1A	O14497	997
PBRM1	SMARCB1	Q12824	996
PBRM1	PHF10	Q8WUB8	995
PBRM1	ARID1B	Q8NFD5	993
PBRM1	SMARCA4	P51532	992
PBRM1	BRD7	Q9NPI1	992
PBRM1	SMARCC2	Q8TAQ2	977
PBRM1	SMARCC1	Q92922	967
PBRM1	SMARCA2	P51531	966
PBRM1	ACTL6A	O96019	958
PBRM1	DPF2	Q92785	906
PBRM1	SMARCE1	Q969G3	905
PBRM1	SMARCD3	Q6STE5	900
PBRM1	H3-3A	P06351	899
PBRM1	H3C1	P02295	899

IntAct

200 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
PBRM1	SMARCA4	psi-mi:“MI:0915”(physical association)	0.800
PBRM1	SMARCA4	psi-mi:“MI:0914”(association)	0.800
SMARCC1	ARID1A	psi-mi:“MI:0914”(association)	0.790
SMARCD1	ARID1A	psi-mi:“MI:0914”(association)	0.790
SMARCC2	ARID1A	psi-mi:“MI:0914”(association)	0.790
ARID2	SMARCA4	psi-mi:“MI:0915”(physical association)	0.770
ARID2	SMARCA4	psi-mi:“MI:0914”(association)	0.770
SMARCE1	SMARCA2	psi-mi:“MI:0914”(association)	0.730
SMARCA4	ACTL6A	psi-mi:“MI:0914”(association)	0.670
ACTL6A	SMARCA4	psi-mi:“MI:0915”(physical association)	0.670
SMARCD3	ARID1A	psi-mi:“MI:0914”(association)	0.640
BCL7C	ARID1A	psi-mi:“MI:0914”(association)	0.640
BCL7A	ARID1A	psi-mi:“MI:0914”(association)	0.640
KPNA1	TCERG1	psi-mi:“MI:0914”(association)	0.640

BioGRID (368): PBRM1 (Two-hybrid), PBRM1 (Affinity Capture-MS), PBRM1 (Affinity Capture-MS), PBRM1 (Affinity Capture-MS), PBRM1 (Affinity Capture-MS), PBRM1 (Affinity Capture-MS), PBRM1 (Affinity Capture-MS), ARID2 (Co-fractionation), COPS3 (Co-fractionation), PBRM1 (Co-fractionation), PBRM1 (Co-fractionation), PBRM1 (Affinity Capture-RNA), PBRM1 (Affinity Capture-MS), PBRM1 (Proximity Label-MS), PBRM1 (Affinity Capture-MS)

ESM2 similar proteins: A2A4P0, F1M386, F1MSG6, F1P065, F1PBJ0, G5EDB9, G5EGS5, O35889, O43295, O60264, P26675, P28370, P35817, P36582, P36583, P41877, P55196, P70600, Q06488, Q12929, Q14289, Q14562, Q15057, Q15326, Q18685, Q24368, Q24564, Q5FVC7, Q5R4H4, Q5ZK62, Q63648, Q6IVG4, Q6PGB8, Q6ZQK5, Q7PS12, Q7Z6B7, Q812A2, Q86U86, Q8BSQ9, Q8CHG7

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

6 interactions.

A	Effect	B	Mechanism
PBRM1	“up-regulates quantity by expression”	CRABP2	“transcriptional regulation”
PBRM1	“up-regulates quantity by expression”	RARB	“transcriptional regulation”
PBRM1	“up-regulates quantity by expression”	S100A13	“transcriptional regulation”
PBRM1	“up-regulates quantity by expression”	CDKN1A	“transcriptional regulation”
PBRM1	“form complex”	“SWI/SNF ACTL6B varian”	binding
TRIM32	“down-regulates quantity by destabilization”	PBRM1	ubiquitination

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 203 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 polybromo-BAF (pBAF) complex	13	56.1×	5e-19
Formation of the canonical BAF (cBAF) complex	12	51.8×	5e-17
Formation of the embryonic stem cell BAF (esBAF) complex	12	49.1×	1e-16
Formation of neuronal progenitor and neuronal BAF (npBAF and nBAF)	15	46.6×	5e-20
Formation of the non-canonical BAF (ncBAF) complex	9	41.1×	1e-11
Regulation of endogenous retroelements	12	30.1×	2e-13
Regulation of MITF-M-dependent genes involved in pigmentation	16	28.9×	1e-17
RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known	11	22.5×	7e-11

GO biological processes:

GO term	Partners	Fold	FDR
regulation of G0 to G1 transition	16	58.3×	3e-23
regulation of nucleotide-excision repair	16	52.0×	2e-22
nucleosome disassembly	11	47.7×	1e-14
regulation of mitotic metaphase/anaphase transition	16	42.9×	1e-20
NLS-bearing protein import into nucleus	8	34.7×	3e-09
positive regulation of T cell differentiation	13	32.0×	1e-14
positive regulation of double-strand break repair	16	29.7×	1e-17
positive regulation of myoblast differentiation	15	29.7×	2e-16

Disease & clinical

Cancer significance

From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 15 cancer types — CCRCC, CEAD, CHOL, COADREAD, ESCA, GBC, LUAD, MEL, NSCLC, PLMESO, PRCC, RCC…(+3 more).

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	1
Likely pathogenic	0
Uncertain significance	6
Likely benign	6
Benign	51

Top pathogenic / likely-pathogenic (1)

Variant ID	HGVS	Classification
218955	NM_001405607.1(PBRM1):c.4043_4050del (p.Asp1348fs)	Pathogenic

SpliceAI

4795 predictions. Top by Δscore:

Variant	Effect	Δscore
3:52548231:TCGAG:T	acceptor_gain	1.0000
3:52548232:CGAG:C	acceptor_gain	1.0000
3:52548232:CGAGC:C	acceptor_gain	1.0000
3:52548233:GAG:G	acceptor_gain	1.0000
3:52548234:AG:A	acceptor_gain	1.0000
3:52548236:C:CC	acceptor_gain	1.0000
3:52548236:CTGA:C	acceptor_loss	1.0000
3:52548242:A:AC	acceptor_gain	1.0000
3:52548242:A:C	acceptor_gain	1.0000
3:52548243:T:C	acceptor_gain	1.0000
3:52548243:T:TC	acceptor_gain	1.0000
3:52548248:G:C	acceptor_gain	1.0000
3:52548248:G:GC	acceptor_gain	1.0000
3:52550415:TCTTA:T	donor_loss	1.0000
3:52550416:CTTA:C	donor_loss	1.0000
3:52550417:TTACC:T	donor_loss	1.0000
3:52550418:TACC:T	donor_loss	1.0000
3:52550419:A:AC	donor_gain	1.0000
3:52550419:ACCT:A	donor_loss	1.0000
3:52550419:ACCTG:A	donor_gain	1.0000
3:52550420:C:CC	donor_gain	1.0000
3:52550420:C:CT	donor_loss	1.0000
3:52550420:CCTG:C	donor_gain	1.0000
3:52550420:CCTGC:C	donor_gain	1.0000
3:52550635:CACCT:C	acceptor_loss	1.0000
3:52550637:CCTGA:C	acceptor_loss	1.0000
3:52550639:T:G	acceptor_loss	1.0000
3:52550814:ACACC:A	acceptor_loss	1.0000
3:52550815:CAC:C	acceptor_gain	1.0000
3:52550816:ACCTA:A	acceptor_loss	1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000000822 (3:52672116 G>A,C), RS1000024069 (3:52678427 T>C), RS1000026976 (3:52636047 A>G), RS1000060010 (3:52584044 A>G), RS1000095963 (3:52584394 C>T), RS1000115053 (3:52672454 G>T), RS1000122526 (3:52600793 C>G), RS1000157169 (3:52635938 A>G), RS1000167231 (3:52545045 C>T), RS1000172490 (3:52684145 G>A), RS1000221826 (3:52653308 G>A), RS1000253484 (3:52665678 G>C), RS1000258196 (3:52629699 A>G), RS1000272206 (3:52635547 C>T), RS1000310470 (3:52616037 C>T)

Disease associations

OMIM: gene MIM:606083 | disease phenotypes: MIM:144700

GenCC curated gene-disease

Mondo (3): PBRM1-related BAFopathy (MONDO:0700122), clear cell renal carcinoma (MONDO:0005005), nonpapillary renal cell carcinoma (MONDO:0007763)

Orphanet (2): Clear cell renal carcinoma (Orphanet:319276), Hereditary clear cell renal cell carcinoma (Orphanet:422526)

HPO phenotypes

2 total (2 of 2 shown, HPO-id order):

HPO	Term
HP:0003745	Sporadic
HP:0005584	Renal cell carcinoma

GWAS associations

70 associations (top):

Study	Trait	p-value
GCST000570_1	Major mood disorders	2.000000e-09
GCST001241_15	Bipolar disorder	2.000000e-06
GCST001715_7	Bipolar disorder with mood-incongruent psychosis	2.000000e-06
GCST002149_14	Schizophrenia	1.000000e-08
GCST002539_48	Schizophrenia	4.000000e-11
GCST002782_195	Waist-to-hip ratio adjusted for body mass index	4.000000e-09
GCST002782_196	Waist-to-hip ratio adjusted for body mass index	3.000000e-11
GCST002782_197	Waist-to-hip ratio adjusted for body mass index	1.000000e-08
GCST002782_198	Waist-to-hip ratio adjusted for body mass index	7.000000e-11
GCST004505_90	Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)	2.000000e-07
GCST004505_91	Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)	9.000000e-06
GCST004521_123	Autism spectrum disorder or schizophrenia	3.000000e-12
GCST004521_201	Autism spectrum disorder or schizophrenia	4.000000e-08
GCST004521_259	Autism spectrum disorder or schizophrenia	6.000000e-09
GCST004562_175	Waist circumference adjusted for body mass index	4.000000e-11
GCST004562_197	Waist circumference adjusted for body mass index	2.000000e-11
GCST004562_88	Waist circumference adjusted for body mass index	6.000000e-10
GCST004563_161	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	1.000000e-10
GCST004563_225	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	5.000000e-10
GCST004563_65	Waist circumference adjusted for BMI (joint analysis main effects and physical activity interaction)	4.000000e-09
GCST004564_42	Waist circumference adjusted for BMI in active individuals	5.000000e-10
GCST004564_43	Waist circumference adjusted for BMI in active individuals	3.000000e-09
GCST004564_44	Waist circumference adjusted for BMI in active individuals	1.000000e-08
GCST004567_62	Waist-to-hip ratio adjusted for BMI (joint analysis for main effect and physical activity interaction)	1.000000e-06
GCST004567_63	Waist-to-hip ratio adjusted for BMI (joint analysis for main effect and physical activity interaction)	6.000000e-07
GCST004567_71	Waist-to-hip ratio adjusted for BMI (joint analysis for main effect and physical activity interaction)	2.000000e-08
GCST004576_68	Waist-to-hip ratio adjusted for body mass index	6.000000e-08
GCST004576_69	Waist-to-hip ratio adjusted for body mass index	2.000000e-09
GCST004576_71	Waist-to-hip ratio adjusted for body mass index	5.000000e-08
GCST004578_17	Waist-to-hip ratio adjusted for BMI in active individuals	5.000000e-06

EFO canonical traits (12, from GWAS)

EFO ID	Trait name
EFO:0007788	BMI-adjusted waist-hip ratio
EFO:0004318	smoking behavior
EFO:0007789	BMI-adjusted waist circumference
EFO:0008002	physical activity measurement
EFO:0004337	intelligence
EFO:0004341	body fat distribution
EFO:0007876	insomnia measurement
EFO:0004509	hemoglobin measurement
EFO:0004346	neuroimaging measurement
EFO:0004587	lymphocyte count
EFO:0009188	Red cell distribution width
EFO:0004532	serum gamma-glutamyl transferase measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1795184 (SINGLE PROTEIN), CHEMBL5291979 (PROTEIN-PROTEIN INTERACTION)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 25,061 (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
CHEMBL1232461	MOLIBRESIB	2	1,538
CHEMBL151	LUTEOLIN	2	23,523

Clinical evidence (CIViC)

Drug × variant × indication: 2 predictive associations from 2 curated evidence items; also 2 prognostic.

Variant	Therapy	Indication	Effect	Level	CIViC
PBRM1 Mutation	Sunitinib + Everolimus	Renal Cell Carcinoma	Sensitivity/Response	CIViC B	EID5996
PBRM1 Mutation	CTLA-4 Inhibitor + Anti-PD-L1 Monoclonal Antibody	Clear Cell Renal Cell Carcinoma	Sensitivity/Response	CIViC B	EID7247

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

GtoPdb / IUPHAR curated pharmacology

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

Target class: other protein — Non-enzymatic BRD containing proteins

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

Ligand	Action	Affinity	Parameter
GNE-064	Inhibition	7.74	pIC50
PFI-3	Binding	7.32	pKd
GNE-235	Binding	4.82	pKd

Binding affinities (BindingDB)

31 measured of 31 human assays (31 total across all organisms); most potent 31 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[6-amino-5-[1-(1-phenylethyl)pyrazol-4-yl]pyridazin-3-yl]phenol	IC50	5.7 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(2-phenylpropoxy)pyridazin-3-yl]phenol	IC50	7.2 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-cyclohexylpyridazin-3-yl)phenol	IC50	8.8 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(1-methylpyrazol-4-yl)pyridazin-3-yl]phenol	IC50	10 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[(1S)-1-phenylethoxy]pyridazin-3-yl]phenol	IC50	14.9 nM	US-10308614: Therapeutic compounds and uses thereof
1-[4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-2-methylpiperazin-1-yl]-2,2-dimethylpropan-1-one	IC50	18.4 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(2-phenylethoxy)pyridazin-3-yl]phenol	IC50	19 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[4-[(dimethylamino)methyl]piperidin-1-yl]pyridazin-3-yl]phenol	IC50	22.5 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-cyclopentylpyridazin-3-yl)phenol	IC50	25 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(3-phenoxyazetidin-1-yl)pyridazin-3-yl]phenol	IC50	35.6 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(3-methyl-4-methylsulfonylpiperazin-1-yl)pyridazin-3-yl]phenol	IC50	35.8 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[4-(1-phenylethyl)piperazin-1-yl]pyridazin-3-yl]phenol	IC50	36.1 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-phenylpyridazin-3-yl)phenol	IC50	37.3 nM	US-10308614: Therapeutic compounds and uses thereof
1-[4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-2-methylpiperazin-1-yl]ethanone	IC50	39 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(1-benzylpiperidin-4-yl)pyridazin-3-yl]phenol	IC50	39.3 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-piperidin-1-ylpyridazin-3-yl)phenol	IC50	45.9 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(3-benzyl-4-methylsulfonylpiperazin-1-yl)pyridazin-3-yl]phenol	IC50	46.8 nM	US-10308614: Therapeutic compounds and uses thereof
2-[5-[(3aR,6aS)-2-benzyl-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]-6-aminopyridazin-3-yl]phenol	IC50	47.6 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[4-[(dimethylamino)methyl]phenyl]pyridazin-3-yl]phenol	IC50	49.3 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(1-benzylpyrrolidin-3-yl)oxypyridazin-3-yl]phenol	IC50	59.7 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[4-(pyridin-3-ylmethyl)piperazin-1-yl]pyridazin-3-yl]phenol	IC50	60.7 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(2,6-dimethylmorpholin-4-yl)pyridazin-3-yl]phenol	IC50	69.6 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-morpholin-4-ylpyridazin-3-yl)phenol	IC50	71.5 nM	US-10308614: Therapeutic compounds and uses thereof
1-[4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazin-1-yl]ethanone	IC50	71.7 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(8-benzyl-3,8-diazabicyclo[3.2.1]octan-3-yl)pyridazin-3-yl]phenol	IC50	79 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-(1-phenylpropan-2-yloxy)pyridazin-3-yl]phenol	IC50	92.5 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[1-(oxan-4-yl)ethoxy]pyridazin-3-yl]phenol	IC50	197 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[2-(dimethylamino)ethoxy]pyridazin-3-yl]phenol	IC50	276 nM	US-10308614: Therapeutic compounds and uses thereof
2-(6-amino-5-phenylpyridazin-3-yl)-6-fluorophenol	IC50	320 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-amino-5-[1-(benzenesulfonyl)pyrrolidin-3-yl]pyridazin-3-yl]phenol	IC50	466 nM	US-10308614: Therapeutic compounds and uses thereof
2-[6-(methylamino)pyridazin-3-yl]phenol	IC50	1040 nM	US-10308614: Therapeutic compounds and uses thereof

ChEMBL bioactivities

140 potent at pChembl≥5 of 178 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.30	Kd	5	nM	CHEMBL5428009
8.22	Kd	6	nM	CHEMBL5415064
8.22	Kd	6	nM	CHEMBL5409404
8.05	IC50	8.9	nM	CHEMBL5177096
8.05	Kd	9	nM	CHEMBL5412292
8.05	Kd	9	nM	CHEMBL5406315
8.00	Kd	10	nM	CHEMBL5424811
7.89	Kd	13	nM	CHEMBL4780617
7.82	Kd	15	nM	CHEMBL5401472
7.82	Kd	15	nM	CHEMBL5431862
7.81	EC50	15.6	nM	CHEMBL5278697
7.75	Kd	18	nM	CHEMBL5207330
7.72	Kd	19	nM	CHEMBL5409404
7.66	Kd	22	nM	CHEMBL5401472
7.62	Kd	24	nM	CHEMBL5406315
7.60	Kd	25	nM	CHEMBL3752911
7.58	Kd	26	nM	CHEMBL4746865
7.55	Kd	28	nM	CHEMBL3819245
7.54	Kd	29	nM	CHEMBL5398829
7.52	Kd	30	nM	CHEMBL5401472
7.50	EC50	32	nM	CHEMBL5278697
7.44	Kd	36	nM	CHEMBL5431862
7.40	Kd	40	nM	CHEMBL5428009
7.40	Kd	40	nM	CHEMBL5177096
7.40	Kd	40	nM	CHEMBL5411199
7.40	Kd	40	nM	CHEMBL5424811
7.37	Kd	43	nM	CHEMBL3899245
7.32	Kd	48	nM	CHEMBL3752911
7.30	Kd	50	nM	CHEMBL5401472
7.28	Kd	53	nM	CHEMBL5425250
7.21	Kd	62	nM	CHEMBL5401472
7.19	Kd	64	nM	CHEMBL4793170
7.16	Kd	69	nM	CHEMBL5177096
7.16	Kd	70	nM	CHEMBL5411199
7.15	Kd	71	nM	MOLIBRESIB
7.05	Kd	90	nM	CHEMBL5398829
7.00	Kd	100	nM	CHEMBL5424811
6.91	Kd	124	nM	CHEMBL3822689
6.90	Kd	127	nM	CHEMBL3823524
6.86	Kd	137	nM	CHEMBL3823132
6.85	Kd	142	nM	CHEMBL3824067
6.85	Kd	140	nM	CHEMBL5426305
6.84	Kd	145	nM	CHEMBL5415064
6.82	Kd	152	nM	CHEMBL3819245
6.80	IC50	160	nM	CHEMBL5180611
6.77	Kd	170	nM	CHEMBL3823055
6.77	Kd	170	nM	CHEMBL5183240
6.75	IC50	180	nM	MOLIBRESIB
6.70	IC50	200	nM	CHEMBL3823055
6.70	IC50	200	nM	CHEMBL5195502

PubChem BioAssay actives

134 with measured affinity, of 699 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
2-[6-amino-5-[(2S)-2-methylpiperidin-1-yl]pyridazin-3-yl]phenol	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0050	uM
2-(6-amino-5-pyrrolidin-1-ylpyridazin-3-yl)phenol	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0060	uM
2-[6-amino-5-[(2R)-2-propan-2-ylpyrrolidin-1-yl]pyridazin-3-yl]phenol	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0060	uM
2-(6-amino-5-phenylpyridazin-3-yl)phenol	1886337: Inhibition of PBRM1 bromodomain 5 (unknown origin) by TR-FRET assay	ic50	0.0089	uM
2-[6-amino-5-[(2S)-2-ethylpyrrolidin-1-yl]pyridazin-3-yl]phenol	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0090	uM
tert-butyl (3S)-4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-3-methylpiperazine-1-carboxylate	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0090	uM
2-(6-amino-5-piperidin-1-ylpyridazin-3-yl)phenol	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0100	uM
tert-butyl 4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazine-1-carboxylate	1683130: Binding affinity to polybromo-1 (5) (unknown origin) by ITC analysis	kd	0.0130	uM
2-[6-amino-5-[(2S)-2-methylpyrrolidin-1-yl]pyridazin-3-yl]phenol	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0150	uM
2-[6-amino-5-[(2R)-2-cyclopropylpyrrolidin-1-yl]pyridazin-3-yl]phenol	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0150	uM
(2R,4S)-N-[[2-[2-[4-[[4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperazin-1-yl]methyl]phenoxy]ethoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-1-[(2R)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide	1928112: PROTAC activity at PBRM1/VHL in human NCI-H1568 cells assessed as degradation protein measured after 18 hrs	ec50	0.0156	uM
1-[(2R)-4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-2-methylpiperazin-1-yl]ethanone	1886342: Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assay	kd	0.0180	uM
(E)-1-(2-hydroxyphenyl)-3-[(1R,4R)-5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one	1886342: Binding affinity to human PBRM1 bromodomain 5 (S645 to D766 residues) expressed in bacterial expression system by bromoscan assay	kd	0.0250	uM
2-(6-amino-5-piperazin-1-ylpyridazin-3-yl)phenol	1683130: Binding affinity to polybromo-1 (5) (unknown origin) by ITC analysis	kd	0.0260	uM
(E)-3-[4-(cyclopropylamino)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-1-(2-hydroxyphenyl)prop-2-en-1-one	1308370: Binding affinity to human PB1 isoform 5 expressed in BL21 (DE3)-R3-BirA cells by isothermal titration calorimetry	kd	0.0280	uM
1-[(3S)-4-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]-3-methylpiperazin-1-yl]ethanone	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0290	uM
2-[6-amino-5-[(2R)-2-methylpiperidin-1-yl]pyridazin-3-yl]phenol	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0400	uM
(E)-1-(2-hydroxyphenyl)-3-(5-pyridin-2-yl-2,5-diazabicyclo[2.2.1]heptan-2-yl)prop-2-en-1-one	1323617: Binding affinity to N-terminal his6-tagged human PB1 bromodomain 5 expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 at 15 uM by ITC method	kd	0.0430	uM
2-[6-amino-5-[(2R)-2-methylpyrrolidin-1-yl]pyridazin-3-yl]phenol	2014568: Binding affinity to PBRM1 bromodomain 5 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.0530	uM
1-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperidin-4-ol	1683130: Binding affinity to polybromo-1 (5) (unknown origin) by ITC analysis	kd	0.0640	uM
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide	2179201: Binding affinity against PBRM1 (unknown origin) assessed as apparent dissociation constant incubated for 1 hr by colloidal coomassie staining based LC-MS/MS analysis	kd	0.0710	uM
(3E)-6-chloro-3-[(4-methylpiperazin-1-yl)methylidene]-1,2-dihydropyrrolo[1,2-a]quinazolin-5-one	1310276: Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry	kd	0.1240	uM
(3E)-6-chloro-3-(piperidin-1-ylmethylidene)-1,2-dihydropyrrolo[1,2-a]quinazolin-5-one	1310276: Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry	kd	0.1270	uM
(3E)-6-chloro-3-(dimethylaminomethylidene)-1,2-dihydropyrrolo[1,2-a]quinazolin-5-one	1310276: Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry	kd	0.1370	uM
6-(furan-2-yl)-4-[(2S)-2-methylpiperidin-1-yl]pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.1400	uM
(3E)-6-chloro-3-[(4-ethylpiperazin-1-yl)methylidene]-1,2-dihydropyrrolo[1,2-a]quinazolin-5-one	1310276: Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry	kd	0.1420	uM
5-bromo-2-(3-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.1600	uM
(3E)-6-chloro-3-(2-ethylbutylidene)-1,2-dihydropyrrolo[1,2-a]quinazolin-5-one	1310276: Binding affinity to His6-tagged human recombinant PB1 bromodomain isoform 5 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by VP-ITC microcalorimetry	kd	0.1700	uM
4-phenyl-5H-pyridazino[4,3-b]indol-3-amine	1886343: Binding affinity to human PBRM1 bromodomain 2 (S178 to E291 residues) expressed in bacterial expression system by bromoscan assay	kd	0.1700	uM
5-chloro-2-(2-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.2000	uM
5-chloro-2-(2,3-dimethylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.2200	uM
(3R)-1-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperidin-3-ol	1683130: Binding affinity to polybromo-1 (5) (unknown origin) by ITC analysis	kd	0.2380	uM
5-chloro-2-(3-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.2600	uM
6-(furan-2-yl)-4-[(2S)-2-methylpyrrolidin-1-yl]pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.2800	uM
5-chloro-2-(2,6-dimethylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.2900	uM
5-bromo-2-(2-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.2900	uM
(3S,4R)-1-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperidine-3,4-diol	1683133: Binding affinity to polybromo-1 (2) (unknown origin) by ITC analysis	kd	0.4200	uM
5-chloro-2-(2,5-dimethylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.4300	uM
4-[(2S)-2-ethylpyrrolidin-1-yl]-6-(furan-2-yl)pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.4400	uM
4-[(2R)-2-cyclopropylpyrrolidin-1-yl]-6-(furan-2-yl)pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.5600	uM
6-(furan-2-yl)-4-[(2R)-2-propan-2-ylpyrrolidin-1-yl]pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.6000	uM
4-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acid	1165986: Inhibition of human PBRM1 bromodomain 1 by BROMOscan assay	ic50	0.6310	uM
4-[(2S)-2-methylpyrrolidin-1-yl]-6-thiophen-2-ylpyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.8000	uM
6-(furan-2-yl)-4-[(2R)-2-methylpiperidin-1-yl]pyridazin-3-amine	2014569: Binding affinity to PBRM1 bromodomain 2 (unknown origin) assessed as dissociation constant by BROMOscan LeadHunter assay	kd	0.8000	uM
5-chloro-2-(2,4-dimethylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.8600	uM
5-chloro-2-(4-methylphenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	0.8700	uM
(3S,4S)-1-[3-amino-6-(2-hydroxyphenyl)pyridazin-4-yl]piperidine-3,4-diol	1683133: Binding affinity to polybromo-1 (2) (unknown origin) by ITC analysis	kd	0.8920	uM
2-[6-amino-5-[(3R)-3-phenoxypiperidin-1-yl]pyridazin-3-yl]phenol	1683132: Binding affinity to polybromo-1 (3) (unknown origin) by ITC analysis	kd	0.9110	uM
5-chloro-2-(2-chloro-6-fluorophenyl)-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	1.0000	uM
5-chloro-2-phenyl-2,3-dihydro-1H-quinazolin-4-one	1857772: Inhibition of biotinylated histone H3K14 (1 to 20 residues) peptide binding to His6-tagged recombinant human PBRM1 BD2 transfected in Escherichia coli BL21 (DE3) incubated for 30 mins by Alphascreen assay	ic50	1.1000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects expression, decreases expression, decreases methylation	4
methylmercuric chloride	decreases expression, increases expression	2
sodium arsenite	affects cotreatment, decreases expression, increases expression	2
Cyclosporine	increases expression	2
aristolochic acid I	decreases expression	1
FR900359	affects phosphorylation	1
TAK-243	decreases sumoylation	1
triphenyl phosphate	affects expression	1
trichostatin A	decreases expression	1
riddelliine	decreases expression, increases metabolic processing	1
beta-lapachone	decreases expression	1
potassium chromate(VI)	affects cotreatment, decreases expression	1
coumarin	decreases phosphorylation	1
epigallocatechin gallate	affects cotreatment, decreases expression	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression	1
LDN 193189	affects cotreatment, increases expression	1
Resveratrol	affects cotreatment, increases expression	1
Sunitinib	increases expression	1
Arsenic Trioxide	decreases expression	1
Fulvestrant	decreases methylation	1
Acetaminophen	increases expression	1
Air Pollutants	affects expression, increases abundance	1
Atrazine	decreases expression	1
Vehicle Emissions	increases abundance, increases expression	1
Caffeine	increases phosphorylation	1
Doxorubicin	affects expression	1
Methotrexate	increases expression	1
Ozone	affects expression, increases abundance	1
Plant Extracts	affects cotreatment, increases expression	1
Quercetin	increases expression	1

ChEMBL screening assays

193 unique, capped per target: 193 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1832846	Binding	Binding affinity to PB1 assessed as change in melting temperature at 100 uM by differential scanning fluorimetry	3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands. — J Med Chem

Cellosaurus cell lines

33 cell lines: 17 cancer cell line, 13 telomerase immortalized cell line, 3 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_5884	KTCTL-1M	Cancer cell line	Male
CVCL_A656	MZ-CRC-1	Cancer cell line	Female
CVCL_B8M6	Abcam HCT 116 PBRM1 KO	Cancer cell line	Male
CVCL_B9A1	Abcam MCF-7 PBRM1 KO	Cancer cell line	Female
CVCL_B9PD	Abcam A-549 PBRM1 KO	Cancer cell line	Male
CVCL_E0JR	Ubigene HeLa PBRM1 KO	Cancer cell line	Female
CVCL_E3VB	1BR3-hTERT PBRM1 KO 3	Telomerase immortalized cell line	Male
CVCL_E3VC	1BR3-hTERT PBRM1 KO 4	Telomerase immortalized cell line	Male
CVCL_E3VD	1BR3-hTERT PBRM1 KO 5	Telomerase immortalized cell line	Male
CVCL_E3VE	1BR3-hTERT PBRM1 KO 6	Telomerase immortalized cell line	Male

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT01521715	PHASE4	COMPLETED	First Line Pazopanib in Poor Risk Patients With Metastatic Renal Cell Carcinoma
NCT02570789	PHASE4	TERMINATED	Evaluation of Predictive Markers for Toxicity and Efficacy in Patients With mccRCC Treated by Anti-VEGF Therapy
NCT00414765	PHASE4	COMPLETED	Aldesleukin in Participants With Metastatic Renal Cell Carcinoma or Metastatic Melanoma
NCT00777504	PHASE4	UNKNOWN	Study to the Optimal Duration of Therapy With Oral Angiogenesis Inhibitors
NCT00930345	PHASE4	TERMINATED	Biological, Pathological and Imagery Markers in the First-line Treatment of Metastatic Clear-cell Renal Cell Carcinoma
NCT01206764	PHASE4	COMPLETED	A Trial of Everolimis in Patients With Advanced Renal Cell Carcinoma.
NCT01266837	PHASE4	COMPLETED	Open Label, Single Arm Trial to Characterize Patients With Metastatic RCC Treated With Everolimus After Failure of the First VEGF-targeted Therapy (MARC-2)
NCT02056587	PHASE4	COMPLETED	Everolimus in Patients With Metastatic Renal Cell Carcinoma Following Progression on Prior Bevacizumab Treatment
NCT02338570	PHASE4	TERMINATED	Outcome-related Factors in Patients With Metastatic Renal Cell Carcinoma Treated With Everolimus (ORCHIDEE)
NCT02596035	PHASE4	COMPLETED	An Investigational Immuno-therapy Safety Trial of Nivolumab in Patients With Advanced or Metastatic Renal Cell Carcinoma
NCT02982954	PHASE4	COMPLETED	A Study to Evaluate the Safety of Nivolumab and Ipilimumab in Subjects With Previously Untreated Advanced or Metastatic Renal Cell Cancer
NCT05949424	PHASE4	UNKNOWN	OPTI - DOSE: Optimal Dosing of Oral Anticancer Drugs in Older Adults
NCT07028125	PHASE4	RECRUITING	Digital Monitoring of Self-reported Symptoms by Patients Treated With Cabozantinib Plus Nivolumab for Advanced Clear-cell Renal Carcinoma
NCT07405086	PHASE4	RECRUITING	Morning Versus Afternoon Administration of Immunotherapy for the Treatment of Advanced or Metastatic Solid Tumors, The Knight SHIFT Study
NCT00326898	PHASE3	COMPLETED	Sunitinib Malate or Sorafenib Tosylate in Treating Patients With Kidney Cancer That Was Removed By Surgery
NCT00397345	PHASE3	COMPLETED	TroVax Renal Immunotherapy Survival Trial
NCT01198158	PHASE3	TERMINATED	Everolimus With or Without Bevacizumab in Treating Patients With Advanced Kidney Cancer That Progressed After First-Line Therapy
NCT01575548	PHASE3	ACTIVE_NOT_RECRUITING	Pazopanib Hydrochloride in Treating Patients With Metastatic Kidney Cancer Who Have No Evidence of Disease After Surgery
NCT01599754	PHASE3	TERMINATED	Adjuvant Axitinib Therapy of Renal Cell Cancer in High Risk Patients
NCT02535351	PHASE3	TERMINATED	Targeted Therapy With or Without Nephrectomy in Metastatic Renal Cell Carcinoma: Liquid Biopsy for Biomarkers Discovery
NCT03793166	PHASE3	ACTIVE_NOT_RECRUITING	Immunotherapy With Nivolumab and Ipilimumab Followed by Nivolumab or Nivolumab With Cabozantinib for Patients With Advanced Kidney Cancer, The PDIGREE Study
NCT03849118	PHASE3	COMPLETED	89Zr-TLX250 for PET/CT Imaging of ccRCC- ZIRCON Study
NCT04510597	PHASE3	RECRUITING	Comparing the Outcome of Immunotherapy-Based Drug Combination Therapy With or Without Surgery to Remove the Kidney in Metastatic Kidney Cancer, the PROBE Trial
NCT04810078	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Subcutaneous Nivolumab Versus Intravenous Nivolumab in Participants With Previously Treated Clear Cell Renal Cell Carcinoma That is Advanced or Has Spread
NCT06661720	PHASE3	RECRUITING	Testing the Addition of the Anti-Cancer Drug Tivozanib to Immunotherapy (Pembrolizumab) After Surgery to Remove All Known Sites of Kidney Cancer
NCT06750419	PHASE3	RECRUITING	89Zr-TLX250 for PET/CT Imaging of ccRCC - ZIRCON-CP Study
NCT07000149	PHASE3	ACTIVE_NOT_RECRUITING	A Study to Investigate the Efficacy and Safety of Volrustomig ± Casdatifan vs Nivolumab + Ipilimumab as 1L Treatment for Advanced ccRCC
NCT07011719	PHASE3	RECRUITING	Study of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma
NCT07197580	PHASE3	RECRUITING	Phase 3 Study to Assess Safety and Efficacy of 177Lu-TLX250 in Advanced Relapsed or Recurrent ccRCC
NCT07383441	PHASE3	NOT_YET_RECRUITING	Adding Biotherapy or Placebo to Standard Treatment for Advanced Kidney Cancer
NCT00033904	PHASE3	COMPLETED	Survival Study Of Oncophage® vs. Observation In Patients With Kidney Cancer
NCT00126178	PHASE3	TERMINATED	Clinical Trial Studying a Personalized Cancer Vaccine in Patients With Non-metastatic Kidney Cancer
NCT00291369	PHASE3	COMPLETED	Cytokines in Patients With Metastatic Renal Cell Carcinoma of Intermediate Prognosis
NCT00410124	PHASE3	COMPLETED	RAD001 Plus Best Supportive Care (BSC) Versus BSC Plus Placebo in Patients With Metastatic Carcinoma of the Kidney Which Has Progressed After Treatment With Sorafenib and/or Sunitinib
NCT00474786	PHASE3	COMPLETED	Temsirolimus Versus Sorafenib As Second-Line Therapy In Patients With Advanced RCC Who Have Failed First-Line Sunitinib
NCT00478114	PHASE3	COMPLETED	Efficacy and Safety of Sorafenib in Advanced Renal Cell Carcinoma (RCC)
NCT00606632	PHASE3	COMPLETED	Pre-surgical Detection of Clear Cell Renal Cell Carcinoma (ccRCC) Using Radiolabeled G250-Antibody
NCT00606866	PHASE3	COMPLETED	MRI Study of BAY 43-9006 in Metastatic Renal Cell Carcinoma
NCT00631371	PHASE3	COMPLETED	Study Comparing Bevacizumab + Temsirolimus vs. Bevacizumab + Interferon-Alfa In Advanced Renal Cell Carcinoma Subjects
NCT00732914	PHASE3	COMPLETED	Sequential Study to Treat Renal Cell Carcinoma