CBX7

gene
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Summary

CBX7 (chromobox 7, HGNC:1557) is a protein-coding gene on chromosome 22q13.1, encoding Chromobox protein homolog 7 (O95931). Component of a Polycomb group (PcG) multiprotein PRC1-like complex, a complex class required to maintain the transcriptionally repressive state of many genes, including Hox genes, throughout development.

This gene encodes a protein that contains the CHROMO (CHRomatin Organization MOdifier) domain. The encoded protein is a component of the Polycomb repressive complex 1 (PRC1), and is thought to control the lifespan of several normal human cells.

Source: NCBI Gene 23492 — RefSeq curated summary.

At a glance

  • GWAS associations: 13
  • Clinical variants (ClinVar): 42 total
  • Druggable target: yes — 1 molecules with ChEMBL bioactivity
  • MANE Select transcript: NM_175709

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:1557
Approved symbolCBX7
Namechromobox 7
Location22q13.1
Locus typegene with protein product
StatusApproved
Ensembl geneENSG00000100307
Ensembl biotypeprotein_coding
OMIM608457
Entrez23492

Gene structure

Transcript identifiers

Ensembl transcripts: 20 — 16 protein_coding, 3 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000216133, ENST00000401405, ENST00000434260, ENST00000475962, ENST00000477827, ENST00000482294, ENST00000490741, ENST00000858776, ENST00000858777, ENST00000858778, ENST00000858779, ENST00000858780, ENST00000858781, ENST00000858782, ENST00000858783, ENST00000858784, ENST00000944728, ENST00000944729, ENST00000944730, ENST00000944731

RefSeq mRNA: 3 — MANE Select: NM_175709 NM_001346743, NM_001346744, NM_175709

CCDS: CCDS13986, CCDS87028

Canonical transcript exons

ENST00000216133 — 6 exons

ExonStartEnd
ENSE000006546843913440139134752
ENSE000012997643913077239134048
ENSE000013083143913863639138702
ENSE000013306073914137139141436
ENSE000019349503915237639152680
ENSE000036605263914978939149832

Expression profiles

Bgee: expression breadth ubiquitous, 296 present calls, max score 98.57.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 9.7980 / max 184.0461, expressed in 1513 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter IDTPM avgSamples expressed
1942705.63001238
1942713.3853817
1942690.5762254
1942680.2066134

Top tissues by expression

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

TissueAnatomy IDExpression scoreQuality
cerebellar vermisUBERON:000472098.57gold quality
paraflocculusUBERON:000535198.50gold quality
Brodmann (1909) area 10UBERON:001354197.64gold quality
right hemisphere of cerebellumUBERON:001489097.33gold quality
frontal poleUBERON:000279597.29gold quality
cerebellar cortexUBERON:000212997.28gold quality
cerebellar hemisphereUBERON:000224597.28gold quality
mucosa of stomachUBERON:000119997.23gold quality
cerebellumUBERON:000203797.18gold quality
ponsUBERON:000098897.14gold quality
middle frontal gyrusUBERON:000270297.14gold quality
right coronary arteryUBERON:000162597.02gold quality
right frontal lobeUBERON:000281096.94gold quality
popliteal arteryUBERON:000225096.89gold quality
tibial arteryUBERON:000761096.89gold quality
prefrontal cortexUBERON:000045196.84gold quality
lower esophagus muscularis layerUBERON:003583396.73gold quality
lower esophagusUBERON:001347396.67gold quality
parietal lobeUBERON:000187296.64gold quality
esophagogastric junction muscularis propriaUBERON:003584196.52gold quality
postcentral gyrusUBERON:000258196.51gold quality
superior vestibular nucleusUBERON:000722796.50gold quality
frontal cortexUBERON:000187096.41gold quality
cingulate cortexUBERON:000302796.41gold quality
frontal lobeUBERON:001652596.41gold quality
anterior cingulate cortexUBERON:000983596.38gold quality
saphenous veinUBERON:000731896.34gold quality
occipital lobeUBERON:000202196.30gold quality
olfactory bulbUBERON:000226496.27gold quality
aortaUBERON:000094796.24gold quality

Single-cell (SCXA)

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

ExperimentMarker?Max mean expression
E-ANND-3yes6.13

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

2 targets.

TargetRegulation
CCNE1Repression
CDH1Activation

miRNA regulators (miRDB)

142 targeting CBX7, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-4262100.0073.263931
HSA-MIR-4533100.0069.482758
HSA-MIR-4747-5P100.0067.902681
HSA-MIR-5196-5P100.0067.982761
HSA-MIR-4476100.0068.182030
HSA-MIR-9-5P100.0072.282361
HSA-MIR-6876-5P100.0067.682126
HSA-MIR-5692A100.0074.406850
HSA-MIR-3163100.0077.238605
HSA-MIR-8485100.0077.574731
HSA-MIR-181A-5P99.9972.962995
HSA-MIR-181B-5P99.9972.972996
HSA-MIR-181C-5P99.9972.952996
HSA-MIR-181D-5P99.9973.042997
HSA-MIR-551B-5P99.9671.283493
HSA-MIR-6825-5P99.9669.813431
HSA-MIR-570-3P99.9672.414910
HSA-MIR-9983-3P99.9471.483631
HSA-MIR-6721-5P99.9368.922981
HSA-MIR-218-5P99.9372.222103
HSA-MIR-990299.8969.152250
HSA-MIR-129-5P99.8870.263273
HSA-MIR-449299.8768.253611
HSA-MIR-444799.8567.812900
HSA-MIR-4728-5P99.8569.394718
HSA-MIR-607999.8468.541170
HSA-MIR-76599.8468.242442
HSA-MIR-3121-3P99.8271.963630
HSA-MIR-6756-5P99.8267.972466
HSA-MIR-4799-5P99.8270.602663

Literature-anchored findings (GeneRIF, showing 40)

  • controls cellular lifespan through regulation of both the p16(Ink4a)/Rb and the Arf/p53 pathways (PMID:14647293)
  • CBX7 is a chromobox protein causally linked to cancer development (PMID:17374722)
  • In human glioma, CBX7 is down-regulated by the inhibition of miR-9 at posttranscriptional level. (PMID:18686603)
  • Loss of the CBX7 gene expression correlates with a highly malignant phenotype in thyroid cancer (PMID:18701502)
  • Downregulation of CBX7 is associated with urothelial tumor progression. (PMID:18984978)
  • the ability of CBX7 to positively regulate E-cadherin expression by interacting with HDAC2 and inhibiting its activity on the E-cadherin promoter would account for the correlation between the loss of CBX7 expression and a highly malignant phenotype (PMID:19706751)
  • Data show that chromobox 7 (CBX7) within the polycomb repressive complex 1 binds to ANRIL, and both CBX7 and ANRIL are found at elevated levels in prostate cancer tissues. (PMID:20541999)
  • data reported indicate that the evaluation of CBX7 expression may represent a valid tool in the prognosis of colon cancer since a reduced survival of colorectal cancer patients is associated with the loss of CBX7 expression. (PMID:20542683)
  • CBX7 acts as an oncogene in the carcinogenesis and progression of gastric cancer, and it may regulate tumorigenesis, cell migration and cancer metastasis partially via p16(INK4a) regulatory pathway. (PMID:20723236)
  • found that expression of CBX7 in gastric carcinoma tissues with p16 methylation was significantly lower than that in their corresponding normal tissues, which showed a negative correlation with transcription of p16 in gastric mucosa (PMID:21060834)
  • cbx7 expression was significantly downregulated in multiple human cancer tissues. (PMID:22041561)
  • These data suggest that CBX7 is a tumor suppressor and that its loss plays a key role in the pathogenesis of cancer. (PMID:22214847)
  • MicroRNA regulation of Cbx7 mediates a switch of Polycomb orthologs during ESC differentiation. (PMID:22226354)
  • we showed for the first time that CBX7 was associated with a decreased prognosis for clear cell adenocarcinoma of the ovary (PMID:24375438)
  • Results suggest that the loss of CBX7 expression might play a critical role in advanced stages of carcinogenesis by deregulating the expression of specific effector genes. (PMID:24865347)
  • CBX7-mediated epigenetic induction of DKK-1 is crucial for the inhibition of breast tumorigenicity, suggesting that CBX7 could be a potential tumor suppressor in breast cancer. (PMID:25351982)
  • CBX7/HMGA1b/NF-kappaB could take part in the same transcriptional mechanism that finally leads to the regulation of SPP1 gene expression in papillary thyroid carcinoma. (PMID:25595895)
  • Aberrantly expressed miR-9 contributes to T24 cells invasion, partly through directly down-regulating CBX7 protein expression in bladder transitional cell carcinoma (PMID:25596753)
  • Cbx7 is downregulated in CCs, and Cbx7 expression-low tumors correlated with lymph metastasis and poor overall survival of CC patients. (PMID:25881303)
  • these results suggest that the retention of CBX7 expression may play a role in the modulation of chemosensitivity of lung cancer patients to the treatment with irinotecan and etoposide (PMID:26216446)
  • Data show that polycomb-group proteins BMI1, PHC3, CBX6 and CBX7 expression was significantly increased during imatinib treatment. (PMID:26343356)
  • the miR-9 family of microRNAs (miRNAS) downregulates the expression of CBX7. In turn, CBX7 represses miR-9-1 and miR-9-2 as part of a regulatory negative feedback loop. (PMID:26416703)
  • Study found that Cbx7 was downregulated in glioma cell lines and tumors and identifies it as an inhibitor of glioma cell migration through its inhibitory effect on YAP/TAZ-CTGF-hippo signaling axis and underscores the importance of epigenetic inactivation of Cbx7 in gliomagenesis. (PMID:27291091)
  • Data suggest that miR-375 leads to the activation of oncogenic signatures and tumor progression by targeting chromobox homolog 7 protein (CBX7). (PMID:27449098)
  • Suggest CBX7 is an important tumor suppressor that negatively modulates PTEN/Akt signaling during pancreatic tumorigenesis. (PMID:28030829)
  • CBX7 inhibits epithelial-to-mesenchymal transformation and invasion in glioma (PMID:28388562)
  • our results validate the assumption that CBX7 is a tumor suppressor of gliomas. Moreover, CBX7 is a potential and novel prognostic biomarker in glioma patients. We also clarified that CBX7 silences CCNE1 via the combination of CCNE1 promoter and the recruitment of HDAC2. (PMID:28460453)
  • CBX7 positively regulates stem cell-like characteristics of gastric cancer cells by inhibiting p16 and activating AKT-NF-kappaB-miR-21 pathway. (PMID:29422082)
  • Potential role of CBX7 in regulating pluripotency of adult human pluripotent-like olfactory stem cells in stroke model has been demonstrated. (PMID:29717132)
  • Mass spectrometry analysis revealed several non-histone protein interactions between CBX7 and the H3K9 methyltransferases SETDB1, EHMT1, and EHMT2. These CBX7-binding proteins possess a trimethylated lysine peptide motif highly similar to the canonical CBX7 target H3K27me3. (PMID:30759399)
  • CBX7 and PRMT1 contribute to regulate E-cadherin expression through several mechanisms. (PMID:30826432)
  • Decreased CBX7 expression levels were correlated with liver cirrhosis in HCC patients. Furthermore, the survival times of HCC patients who were CBX7-expression-negative were shorter than HCC patients who were CBX7-expression-positive. Results show that downregulation of CBX7 is related to HCC progression and a poor prognosis in HCC patients. (PMID:30990338)
  • findings suggest that CBX4 rs2289728 and CBX7 rs139394 are protective SNPs against HCC. The two SNPs may reduce the risk of HCC while suppressing the expression of CBX4 and CBX7. (PMID:31211140)
  • CBX7 binds the E-box to inhibit TWIST-1 function and inhibit tumorigenicity and metastatic potential. (PMID:32205869)
  • MicroRNA-18a suppresses ovarian carcinoma progression by targeting CBX7 and regulating ERK/MAPK signaling pathway and epithelial-to-mesenchymal transition. (PMID:32495862)
  • Multiomics integrative analysis reveals antagonistic roles of CBX2 and CBX7 in metabolic reprogramming of breast cancer. (PMID:33400401)
  • CBX7 suppresses urinary bladder cancer progression via modulating AKR1B10-ERK signaling. (PMID:34035231)
  • Expression and correlation analysis of Skp2 and CBX7 in cervical cancer. (PMID:34281957)
  • CBX7 represses the POU2F2 to inhibit the PD-L1 expression and regulate the immune response in bladder cancer. (PMID:35526483)
  • Subcellular expression pattern and clinical significance of CBX2 and CBX7 in breast cancer subtypes. (PMID:37553450)

Cross-species orthologs

6 orthologs

OrganismSymbolGene ID
danio_reriocbx7aENSDARG00000038025
danio_reriocbx7bENSDARG00000087181
mus_musculusCbx7ENSMUSG00000053411
rattus_norvegicusCbx7ENSRNOG00000016875
caenorhabditis_elegansWBGENE00001995
caenorhabditis_elegansWBGENE00007615

Paralogs (8): CBX5 (ENSG00000094916), CBX1 (ENSG00000108468), CBX3 (ENSG00000122565), CBX8 (ENSG00000141570), CBX4 (ENSG00000141582), CBX2 (ENSG00000173894), CBX6 (ENSG00000183741), NPTXR (ENSG00000221890)

Protein

Protein identifiers

Chromobox protein homolog 7O95931 (reviewed: O95931)

All UniProt accessions (3): O95931, B0QYP2, B0QYP3

UniProt curated annotations — full annotation on UniProt →

Function. Component of a Polycomb group (PcG) multiprotein PRC1-like complex, a complex class required to maintain the transcriptionally repressive state of many genes, including Hox genes, throughout development. PcG PRC1 complex acts via chromatin remodeling and modification of histones; it mediates monoubiquitination of histone H2A ‘Lys-119’, rendering chromatin heritably changed in its expressibility. Promotes histone H3 trimethylation at ‘Lys-9’ (H3K9me3). Binds to trimethylated lysine residues in histones, and possibly also other proteins. Regulator of cellular lifespan by maintaining the repression of CDKN2A, but not by inducing telomerase activity.

Subunit / interactions. Component of a PRC1-like complex. Interacts with RING1 and RNF2/RING1B, but not with BMI1, EED or EZH2. Interacts with PCGF1, PCGF2, PCGF3, PCGF5 and PCGF6.

Subcellular location. Nucleus.

Miscellaneous. The human orthologuous proteins of Drosophila Polycomb group protein Pc, CBX2, CBX4, CBX6, CBX7 and CBX8, show distinct nuclear localizations, contribute differently to transcriptional repression, and appear to be part of distinct PRC1-like protein complexes.

RefSeq proteins (3): NP_001333672, NP_001333673, NP_783640* (*=MANE)

Domains & families (InterPro)

IDNameType
IPR000953Chromo/chromo_shadow_domDomain
IPR016197Chromo-like_dom_sfHomologous_superfamily
IPR017984Chromo_dom_subgrDomain
IPR023779Chromodomain_CSConserved_site
IPR023780Chromo_domainDomain
IPR033773CBX7_CConserved_site
IPR043000CBX7Family

Pfam: PF00385, PF17218

UniProt features (19 total): strand 5, mutagenesis site 4, helix 3, region of interest 2, sequence conflict 2, chain 1, domain 1, turn 1

Structure

Experimental structures (PDB)

8 structures.

PDBMethodResolution (Å)
8SIIX-RAY DIFFRACTION1.37
4MN3X-RAY DIFFRACTION1.54
5EPJX-RAY DIFFRACTION1.6
6V2RX-RAY DIFFRACTION1.6
3GS2X-RAY DIFFRACTION1.7
2K1BSOLUTION NMR
2L12SOLUTION NMR
2L1BSOLUTION NMR

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-O95931-F167.010.26

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Mutagenesis-validated functional residues (4):

PositionPhenotype
31loss of cellular lifespan extension.
32loss of cellular lifespan extension.
234loss of interaction with rnf2.
244reduced interaction with rnf2.

Function

Pathways and Gene Ontology

Reactome pathways

0 pathways

MSigDB gene sets: 239 (showing top): RRAGTTGT_UNKNOWN, FAELT_B_CLL_WITH_VH_REARRANGEMENTS_DN, ZHAN_MULTIPLE_MYELOMA_PR_DN, ACEVEDO_NORMAL_TISSUE_ADJACENT_TO_LIVER_TUMOR_DN, GOBP_NEGATIVE_REGULATION_OF_GENE_EXPRESSION_EPIGENETIC, HNF4_01, VANHARANTA_UTERINE_FIBROID_DN, AACTTT_UNKNOWN, TCCAGAG_MIR518C, GOCC_NUCLEAR_UBIQUITIN_LIGASE_COMPLEX, GCM_MAPK10, YAMAZAKI_TCEB3_TARGETS_DN, GOBP_CHROMATIN_REMODELING, GTGACTT_MIR224, GOBP_HETEROCHROMATIN_ORGANIZATION

GO Biological Process (2): negative regulation of transcription by RNA polymerase II (GO:0000122), chromatin organization (GO:0006325)

GO Molecular Function (1): protein binding (GO:0005515)

GO Cellular Component (6): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytosol (GO:0005829), PcG protein complex (GO:0031519), PRC1 complex (GO:0035102)

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure3
regulation of transcription by RNA polymerase II1
transcription by RNA polymerase II1
negative regulation of DNA-templated transcription1
cellular component organization1
binding1
chromosome1
intracellular membrane-bounded organelle1
nuclear lumen1
cytoplasm1
nuclear protein-containing complex1
nuclear ubiquitin ligase complex1
PcG protein complex1

Protein interactions and networks

STRING

1099 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
CBX7BMI1P35226992
CBX7R4GMX3R4GMX3992
CBX7RING1Q06587989
CBX7EZH2Q15910964
CBX7SUZ12Q15022957
CBX7CBX8Q9HC52941
CBX7RNF2Q99496938
CBX7HDAC2Q92769906
CBX7CBX4O00257875
CBX7PCGF2P35227871
CBX7CBX2Q14781865
CBX7KDM2BQ8NHM5831
CBX7CDKN2AP42771810
CBX7RYBPQ8N488795
CBX7PHC2Q8IXK0746

IntAct

61 interactions, top by confidence:

ABTypeScore
RNF2CBX7psi-mi:“MI:0407”(direct interaction)0.960
RNF2CBX7psi-mi:“MI:0915”(physical association)0.960
BMI1CBX7psi-mi:“MI:0914”(association)0.940
CBX7BMI1psi-mi:“MI:0914”(association)0.940
CBX7BMI1psi-mi:“MI:0915”(physical association)0.940
BMI1CBX7psi-mi:“MI:0407”(direct interaction)0.940
BMI1CBX7psi-mi:“MI:0915”(physical association)0.940
BMI1CBX4psi-mi:“MI:0914”(association)0.900
PCGF2CBX4psi-mi:“MI:0914”(association)0.840
CBX7PCGF2psi-mi:“MI:0407”(direct interaction)0.840
CBX7PCGF2psi-mi:“MI:0915”(physical association)0.840
PHC1CBX4psi-mi:“MI:0914”(association)0.790

BioGRID (127): CBX7 (Affinity Capture-MS), CBX7 (Affinity Capture-MS), PHC3 (Affinity Capture-MS), PHC2 (Affinity Capture-MS), USP20 (Affinity Capture-MS), BCOR (Affinity Capture-MS), CSNK2B (Affinity Capture-MS), RNF2 (Affinity Capture-MS), PCGF1 (Affinity Capture-MS), PCGF6 (Affinity Capture-MS), BMI1 (Affinity Capture-MS), PCGF3 (Affinity Capture-MS), CBX7 (Affinity Capture-MS), CBX7 (Affinity Capture-Western), USP20 (Affinity Capture-MS)

ESM2 similar proteins: A0JPN4, A2AKB4, A6NDY0, A6NP61, A7E321, B0BNE4, B1ASB6, O54824, O88286, O95931, P60924, Q14005, Q14154, Q1XFL1, Q3T1H2, Q3TYG6, Q3ZBR0, Q49AM3, Q4R2Z8, Q4R747, Q4VXA5, Q5R7E7, Q5SU73, Q5SXM2, Q5SYB0, Q5XFR0, Q6NVP7, Q6P1D7, Q6ZUX3, Q7Z572, Q7ZXB8, Q80VM8, Q8BG34, Q8BIY3, Q8BLK9, Q8BP86, Q8IY92, Q8K124, Q93075, Q96FV0

Diamond homologs: A0A0P0VUY4, G3V8T1, O60016, O95931, P05205, P23198, P29227, P30658, P45968, P45973, P60889, P83916, P83917, Q10103, Q13185, Q14781, Q3TYA6, Q5F3W5, Q5KQL9, Q5R6X7, Q61686, Q6AYK9, Q8N8U2, Q8VDS3, Q94F87, Q99549, Q9AXT8, Q9D5D8, Q9WTK2, Q9Y232, Q9Y6F7, Q9Y6F8, G5EDE2, G5EET5, O00257, O43463, O54864, O55187, O95503, P26017

SIGNOR signaling

1 interactions.

AEffectBMechanism
CBX7“up-regulates quantity by expression”CDH1“transcriptional regulation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 23 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:

PathwayPartnersFoldFDR
SUMOylation of DNA methylation proteins9287.9×1e-19
RUNX1 interacts with co-factors whose precise effect on RUNX1 targets is not known10143.1×8e-19
SUMOylation of transcription cofactors9104.1×2e-15
SUMOylation of RNA binding proteins9102.0×2e-15
Transcriptional Regulation by E2F6797.6×5e-12
Regulation of PTEN gene transcription976.5×2e-14
SUMOylation of chromatin organization proteins968.0×5e-14
SUMOylation of DNA damage response and repair proteins962.8×9e-14

GO biological processes:

GO termPartnersFoldFDR
chromatin remodeling722.2×2e-06

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

ClassificationCount (floor)
Pathogenic0
Likely pathogenic0
Uncertain significance31
Likely benign3
Benign0

Top pathogenic / likely-pathogenic (0)

SpliceAI

1331 predictions. Top by Δscore:

VariantEffectΔscore
22:39133899:T:TAdonor_gain1.0000
22:39133900:C:Adonor_gain1.0000
22:39134058:C:CTacceptor_gain1.0000
22:39134399:AC:Adonor_gain1.0000
22:39134399:ACCCT:Adonor_gain1.0000
22:39134400:CC:Cdonor_gain1.0000
22:39134400:CCCTC:Cdonor_gain1.0000
22:39134403:T:Adonor_gain1.0000
22:39141369:A:ACdonor_gain1.0000
22:39141370:C:CCdonor_gain1.0000
22:39141370:CTT:Cdonor_gain1.0000
22:39141370:CTTCT:Cdonor_gain1.0000
22:39141372:T:TAdonor_gain1.0000
22:39141437:CTGG:Cacceptor_loss1.0000
22:39141438:T:Cacceptor_loss1.0000
22:39149787:A:ACdonor_gain1.0000
22:39149788:C:CCdonor_gain1.0000
22:39152371:CTCA:Cdonor_loss1.0000
22:39152373:CAC:Cdonor_loss1.0000
22:39152378:T:Adonor_gain1.0000
22:39133899:TCCC:Tdonor_gain0.9900
22:39134046:CTG:Cacceptor_gain0.9900
22:39134055:C:CTacceptor_gain0.9900
22:39134399:A:ACdonor_gain0.9900
22:39134400:C:CCdonor_gain0.9900
22:39134400:CCCT:Cdonor_gain0.9900
22:39141374:T:Adonor_gain0.9900
22:39141381:AGG:Adonor_gain0.9900
22:39141437:C:CCacceptor_gain0.9900
22:39149052:C:CAdonor_gain0.9900

AlphaMissense

1608 scored. Top likely-pathogenic:

VariantProtein changeam_pathogenicity
22:39141407:A:GI48T1.000
22:39141407:A:TI48N1.000
22:39141424:C:AW42C1.000
22:39141424:C:GW42C1.000
22:39141425:C:GW42S1.000
22:39141426:A:GW42R1.000
22:39141426:A:TW42R1.000
22:39149799:A:GW35R1.000
22:39149799:A:TW35R1.000
22:39149806:C:AW32C1.000
22:39149806:C:GW32C1.000
22:39149807:C:GW32S1.000
22:39149808:A:GW32R1.000
22:39149808:A:TW32R1.000
22:39149819:T:GY28S1.000
22:39149820:A:CY28D1.000
22:39149820:A:GY28H1.000
22:39152398:A:TI16N1.000
22:39152412:G:CF11L1.000
22:39152412:G:TF11L1.000
22:39152413:A:GF11S1.000
22:39152414:A:GF11L1.000
22:39133952:A:TV232D0.999
22:39141392:A:GL53P0.999
22:39141392:A:TL53H0.999
22:39141404:A:GL49S0.999
22:39141407:A:CI48S0.999
22:39141425:C:AW42L0.999
22:39141426:A:CW42G0.999
22:39141430:G:CS40R0.999

dbSNP variants (sampled 300 via entrez): RS1000032566 (22:39139062 A>G), RS1000077771 (22:39146085 G>A), RS1000295982 (22:39140252 C>T), RS1000358300 (22:39135452 A>C), RS1000373209 (22:39132630 G>A), RS1000502567 (22:39148361 A>G), RS1000535206 (22:39138438 G>A,C), RS1000582245 (22:39130405 C>T), RS1000604872 (22:39137383 T>C,G), RS1000696134 (22:39136461 G>T), RS1000708930 (22:39133651 C>T), RS1000725276 (22:39136613 C>A), RS1000946576 (22:39131648 G>A), RS1001013063 (22:39153509 C>T), RS1001200016 (22:39136495 T>C)

Disease associations

OMIM: gene MIM:608457 | disease phenotypes:

GenCC curated gene-disease

Mondo (1): prostate cancer (MONDO:0008315)

Orphanet (1): Familial prostate cancer (Orphanet:1331)

HPO phenotypes

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

GWAS associations

13 associations (top):

StudyTraitp-value
GCST002140_6Multiple myeloma8.000000e-16
GCST002541_121Menarche (age at onset)3.000000e-08
GCST002921_8Multiple myeloma3.000000e-07
GCST002922_9Multiple myeloma and monoclonal gammopathy9.000000e-06
GCST004028_10Immunoglobulin light chain (AL) amyloidosis8.000000e-08
GCST004610_103White blood cell count1.000000e-09
GCST004627_117Lymphocyte count2.000000e-16
GCST012396_13Multiple myeloma1.000000e-09
GCST90002383_110Hematocrit4.000000e-12
GCST90002384_506Hemoglobin7.000000e-12
GCST90002388_270Lymphocyte count1.000000e-37
GCST90002398_28Neutrophil count1.000000e-10
GCST90002407_199White blood cell count1.000000e-14

EFO canonical traits (5, from GWAS)

EFO IDTrait name
EFO:0004703age at menarche
EFO:0004587lymphocyte count
EFO:0004348hematocrit
EFO:0004509hemoglobin measurement
EFO:0004833neutrophil count

MeSH disease descriptors (1)

DescriptorNameTree numbers
D011471Prostatic NeoplasmsC04.588.945.440.770; C12.100.500.260.750; C12.100.500.565.625; C12.200.294.260.750; C12.200.294.565.625; C12.200.758.409.750; C12.900.619.750

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1764946 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

1 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 36,848 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL265502SURAMIN336,848

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

ChEMBL bioactivities

92 potent at pChembl≥5 of 172 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
7.96Kd11nMCHEMBL4647581
7.92Kd12nMCHEMBL3780251
7.70IC5020nMCHEMBL5715919
7.50IC5032nMCHEMBL3972289
7.46IC5035nMCHEMBL3958557
7.46IC5035nMCHEMBL3889586
7.43IC5037nMCHEMBL3939958
7.33IC5047nMCHEMBL3942693
7.27Kd53.8nMCHEMBL5715919
7.25IC5056nMCHEMBL3916023
7.23Kd59nMCHEMBL5715919
7.21IC5061nMCHEMBL3934881
7.20IC5063nMCHEMBL3987134
7.12IC5075nMCHEMBL3969494
7.09IC5081nMCHEMBL3953637
7.01Kd97nMCHEMBL3939958
7.01Kd97nMCHEMBL4449240
7.00Kd100nMCHEMBL3780251
6.89IC50130nMCHEMBL3933207
6.80Kd160nMCHEMBL3780663
6.80Kd160nMCHEMBL4635096
6.70Kd200nMCHEMBL3234442
6.70Kd200nMCHEMBL3234443
6.66Kd220nMCHEMBL3559502
6.66IC50220nMCHEMBL3925993
6.64IC50230nMCHEMBL3973366
6.62IC50240nMCHEMBL3898460
6.60IC50250nMCHEMBL3937936
6.55Kd280nMCHEMBL3234188
6.54Kd290nMCHEMBL3780663
6.52Kd300nMCHEMBL4640223
6.40Kd400nMCHEMBL3780712
6.24IC50570nMCHEMBL3943850
6.16Kd700nMCHEMBL4646516
6.13IC50740nMCHEMBL3944916
5.96IC501100nMCHEMBL3978944
5.96IC501100nMCHEMBL4640937
5.92IC501200nMCHEMBL3935965
5.82Kd1500nMCHEMBL4643012
5.82Kd1500nMCHEMBL4640186
5.80Kd1600nMCHEMBL4637043
5.77IC501700nMCHEMBL3781271
5.77IC501700nMCHEMBL3949885
5.75Kd1770nMCHEMBL3234145
5.70Kd2000nMCHEMBL3234136
5.70IC502000nMCHEMBL4642464
5.64IC502300nMCHEMBL3781271
5.62Kd2400nMCHEMBL4588523
5.58IC502600nMCHEMBL3980951
5.55Kd2800nMCHEMBL4469115

PubChem BioAssay actives

86 with measured affinity, of 334 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.

CompoundAssayTypeValueUnit
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd0.0110uM
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd0.0120uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[propan-2-yl(propyl)amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0320uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[ethyl(propan-2-yl)amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0350uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[[(2S)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0350uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0370uM
4-tert-butyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-(diethylamino)-1-[[(2S)-1-(dimethylamino)-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]benzamide1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0470uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-[4-[[(2-methylpropan-2-yl)oxycarbonylamino]methyl]phenyl]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0560uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-4-methyl-2-[[(2S)-2-[[(2S)-3-phenyl-2-[(4-propan-2-ylbenzoyl)amino]propanoyl]amino]propanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0610uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-3-[4-(aminomethyl)phenyl]-2-[(4-tert-butylbenzoyl)amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0630uM
4-tert-butyl-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-(diethylamino)-1-(2-hydroxyethylamino)-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]benzamide1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0750uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-ethylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.0810uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1578929: Inhibition of CBX7 (unknown origin) assessed as dissociation constant by isothermal titration calorimetrykd0.0970uM
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoic acid1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.1300uM
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-6-[5-[(3aS,4S,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-1-amino-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1288276: Binding affinity to N-terminal His6-tagged human CBX7 (8 to 62 residues) expressed in Escherichia coli BL21 by surface plasmon resonance assaykd0.1600uM
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]butanoyl]amino]-2-cyclopentylacetyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd0.1600uM
[(5S)-6-[[(2R)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-cyclopentyl-2-[[(2S)-2-[[(2S)-2-[(4-methoxycarbonylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]acetyl]amino]-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd0.2000uM
[(5S)-5-[[(2S)-2-cyclopentyl-2-[[(2S)-2-[[(2S)-2-[(4-methoxycarbonylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]acetyl]amino]-6-(1,3-dihydroxypropan-2-ylamino)-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd0.2000uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-4-methyl-2-[[(2S)-2-[[(2S)-2-[(4-methylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.2200uM
[(5S)-6-(2-aminoethylamino)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-2-cyclopentylacetyl]amino]-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd0.2200uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-4-methyl-2-[[(2S)-2-[[(2S)-3-phenyl-2-[[4-(trifluoromethyl)benzoyl]amino]propanoyl]amino]propanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.2300uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]butanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.2400uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-methoxybenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.2500uM
[(5S)-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd0.2800uM
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]butanoyl]amino]-3-phenylpropanoyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd0.3000uM
[(5S)-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]butanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1288269: Binding affinity to N-terminal His6-tagged human CBX7 (8 to 62) expressed in Escherichia coli BL21 using FITC-peptide-3 as competitive binding probe by fluorescence polarization assaykd0.4000uM
methyl 4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-(diethylamino)-1-[[(2S)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]benzoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.5700uM
[(5S)-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[3-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]propanoylamino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd0.7000uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-4-methyl-2-[[(2S)-2-[[(2S)-2-[(3-methylbenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic500.7400uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-4-methyl-2-[[(2S)-2-[[(2S)-2-[(2-naphthalen-2-ylacetyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]pentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic501.1000uM
[(5S)-6-[[(2S)-1-[[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1650081: Inhibition of CBX7 (unknown origin) assessed as inhibition of CBX4 disruption by competitive FP assayic501.1000uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-benzamido-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic501.2000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd1.5000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]butanoyl]amino]-2-cyclopentylacetyl]amino]-6-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]-1-oxohexan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd1.5000uM
[(5S)-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[3-[[3-carboxy-4-(3-hydroxy-6-oxoxanthen-9-yl)phenyl]carbamothioylamino]propanoylamino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-oxohexyl]-trimethylazanium1650078: Binding affinity to CBX7 (unknown origin) assessed as dissociation constant by fluorescence polarization analysiskd1.6000uM
[(5S)-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1288269: Binding affinity to N-terminal His6-tagged human CBX7 (8 to 62) expressed in Escherichia coli BL21 using FITC-peptide-3 as competitive binding probe by fluorescence polarization assayic501.7000uM
methyl (2S)-2-[[(2S)-6-(diethylamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-(1H-indol-3-yl)acetyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic501.7000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd1.7700uM
[(5S)-6-[[(2S)-1-[[(2S)-1-amino-4-carboxy-1-oxobutan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-bromobenzoyl)amino]-3-phenylpropanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-oxohexyl]-trimethylazanium1650081: Inhibition of CBX7 (unknown origin) assessed as inhibition of CBX4 disruption by competitive FP assayic502.0000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd2.0000uM
3-hydroxy-1-methyl-3-(2-naphthalen-1-yl-2-oxoethyl)indol-2-one1565817: Binding affinity to recombinant human N-terminal GST-tagged CBX7 (1 to 62 residues) expressed in Escherichia coli BL2 by SPR analysiskd2.4000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-benzamido-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[[(2S)-3-hydroxy-1-methoxy-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic502.6000uM
3-[2-[4-(diethylamino)piperidin-1-yl]-2-oxoethyl]-5-fluoro-1,3-benzoxazol-2-one1565817: Binding affinity to recombinant human N-terminal GST-tagged CBX7 (1 to 62 residues) expressed in Escherichia coli BL2 by SPR analysiskd2.8000uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(4-tert-butylbenzoyl)amino]-3-phenylpropanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic503.1000uM
5-fluoro-3-[2-(3-methoxyphenyl)-2-oxoethyl]-1,3-benzoxazol-2-one1565817: Binding affinity to recombinant human N-terminal GST-tagged CBX7 (1 to 62 residues) expressed in Escherichia coli BL2 by SPR analysiskd3.4000uM
3-[2-(3,4-dimethoxyphenyl)-2-oxoethyl]-5-methoxy-1,3-benzoxazol-2-one1565817: Binding affinity to recombinant human N-terminal GST-tagged CBX7 (1 to 62 residues) expressed in Escherichia coli BL2 by SPR analysiskd3.9000uM
[(5S)-5-[[(2S)-2-cyclopentyl-2-[[(2S)-2-[(2-phenylacetyl)amino]propanoyl]amino]acetyl]amino]-6-(1,3-dihydroxypropan-2-ylamino)-6-oxohexyl]-trimethylazanium1129997: Binding affinity to CBX7 (unknown origin) by isothermal titration calorimetry assaykd4.1000uM
methyl (2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-(4-tert-butylphenyl)acetyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-(diethylamino)hexanoyl]amino]-3-hydroxypropanoate1319522: Antagonist activity at recombinant human C-terminal His-tagged CBX7 chromodomain (8 to 62 residues) expressed in Escherichia coli Rosetta BL21(DE3)pLysS using biotin-labeled H3K9me3 measured after 30 mins by AlphaScreen assayic504.4000uM
[4-[2-[4-(2,3-dimethoxybenzoyl)piperazin-1-yl]-2-oxoethoxy]-2,6-dimethylphenyl]urea1313552: Binding affinity to CBX7ChD (7 to 66 residues) (unknown origin) expressed in RIPL-BL21 (DE3)-CodonPlus competent cells in presence of FITC-labeled SETDB1-K1170me3/H3K27me3/ANRIL-LoopC RNA by fluorescence anisotropy assayki4.8000uM
[(5S)-5-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-benzamido-5-(diaminomethylideneamino)pentanoyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-6-[[(2S)-3-hydroxy-1-[[(2S,3R)-3-hydroxy-1-[[(2S)-3-(1H-imidazol-5-yl)-1-[(2-methoxy-2-oxoethyl)amino]-1-oxopropan-2-yl]amino]-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-6-oxohexyl]-trimethylazanium1506814: Binding affinity to Cbx7 (unknown origin) by ITC methodkd5.0000uM

CTD chemical–gene interactions

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

ChemicalActions (top 5)PubMed papers
Valproic Acidaffects cotreatment, increases expression, affects expression4
bisphenol Adecreases methylation, increases expression, affects cotreatment3
Benzo(a)pyreneaffects methylation, decreases expression, decreases methylation3
sodium arseniteincreases expression2
Resveratroldecreases expression, decreases phosphorylation, decreases reaction, increases expression, affects cotreatment2
Nickeldecreases expression2
Phenylmercuric Acetateaffects cotreatment, decreases expression2
triphenyl phosphateaffects expression1
methylselenic acidincreases expression1
trichostatin Aincreases expression1
arsenitedecreases reaction, affects binding1
tris(1,3-dichloro-2-propyl)phosphatedecreases expression1
ferrous chloridedecreases expression1
CGP 52608affects binding, increases reaction1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamideaffects cotreatment, decreases expression1
abrinedecreases expression1
dorsomorphinaffects cotreatment, decreases expression1
jinfukangaffects cotreatment, increases expression1
Temozolomidedecreases expression1
Arsenic Trioxidedecreases expression1
Acetaminophendecreases expression1
Air Pollutantsincreases abundance, affects expression1
Cisplatinaffects cotreatment, increases expression1
Dexamethasoneaffects cotreatment, increases expression1
Doxorubicindecreases expression1
Estradiolaffects cotreatment, decreases expression1
Ethyl Methanesulfonateincreases expression1
Hydralazineaffects cotreatment, increases expression1
Hydrogen Peroxideaffects expression1
Indomethacinincreases expression, affects cotreatment1

ChEMBL screening assays

36 unique, capped per target: 35 binding, 1 functional

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1767464BindingBinding affinity to CBX7 by chemiluminescent assaySmall-molecule ligands of methyl-lysine binding proteins. — J Med Chem
CHEMBL5723067FunctionalAffinity Biochemical interaction: (AlphaScreen) EUB0001090a CBX7Affinity Biochemical Literature for EUbOPEN Chemogenomic Library

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

CellosaurusNameCategorySex
CVCL_E1IPHyCyte 786-O KO-hCBX7Cancer cell lineMale
CVCL_E1IQHyCyte A-498 KO-hCBX7Cancer cell lineMale

Clinical trials (associated diseases)

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

TrialPhaseStatusTitle
NCT00029224PHASE4COMPLETEDTreatment With Zoledronic Acid in Patients With Breast Cancer, Multiple Myeloma, and Prostate Cancer With Cancer Related Bone Lesions
NCT00035997PHASE4COMPLETEDOpen-label Trial on the Effect of I.V. Zoledronic Acid 4 mg on Bone Density in Hormone Sensitive Prostate Cancer Patients With Bone Metastasis
NCT00063609PHASE4COMPLETEDThe Effect of Zoledronic Acid on Bone Loss in Prostate Cancer Patients Undergoing Androgen Deprivation Therapy
NCT00103623PHASE4SUSPENDEDThe Plenaxis® Experience Study
NCT00106392PHASE4COMPLETEDA Safety and Efficacy Study of Prograf in the Prevention of Erectile Dysfunction After Radical Prostatectomy
NCT00185029PHASE4UNKNOWNMR-Lymphography and Lymph Node Staging in Prostate Cancer
NCT00199485PHASE4COMPLETEDAngelica Sinensis for the Treatment of Hot Flashes in Men Undergoing LHRH Therapy for Prostate Cancer
NCT00219219PHASE4COMPLETEDZoledronic Acid in the Prevention of Skeletal-related Events in Hormone Refractory and Hormone-sensitive Prostate Cancer Patients With Bone Metastases
NCT00219271PHASE4COMPLETEDEffect Of Zoledronic Acid On Circulating And Bone Marrow-Residing Prostate Cancer Cells In Patients With Clinically Localized Prostate Cancer
NCT00237146PHASE4COMPLETEDStudy to Evaluate Zoledronic Acid on Quality of Life and Skeletal-related Events as Adjuvant Treatment in Patients With Hormone-naïve Prostate Cancer and Bone Metastasis Who Have Undergone Orchiectomy
NCT00242554PHASE4COMPLETEDOpen-label Phase IV Clinical Trial to Evaluate the Safety and Tolerability of Zoledronic Acid in Patients With Prostate Cancer and Bone Metastases
NCT00280098PHASE4COMPLETEDDocetaxel in the Treatment of Hormone Refractory Prostate Cancer
NCT00293696PHASE4COMPLETEDCasodex/Zoladex Biomarkers in Localised Prostate Cancer
NCT00334139PHASE4COMPLETEDEffect of Zoledronic Acid on Bone Metabolism in Patients With Bone Metastasis and Prostate or Breast Cancer
NCT00375765PHASE4COMPLETEDEffects On Dihydrotestosterone Regulated Gene Expression In Benign Prostatic Hyperplasia Or Prostate Cancer
NCT00391690PHASE4COMPLETEDEvaluation of Bone Markers as Diagnostic Tools for Early Detection of Bone Metastases in Patients With High Risk Prostate Cancer
NCT00422708PHASE4COMPLETEDLocal Anesthesia for Prostate Biopsy
NCT00526331PHASE4COMPLETEDEvaluation of Arterial Pressure Based Cardiac Output for Goal-Directed Perioperative Therapy
NCT00590213PHASE4COMPLETEDCompare the Value of Prophylactic Versus Therapeutic Breast Radiotherapy in CASODEX
NCT00629330PHASE4TERMINATEDDissemination of Prostate Cancer Screening to PCP’s in African American Communities
NCT00771966PHASE4COMPLETEDRadical Prostatectomy and Perioperative Fluid Therapy
NCT00805701PHASE4COMPLETEDStudy Assessing The Efficacy And Safety Of Avodart (Dutasteride) At Improving Urinary Symptoms In Men With Prostate Cancer Who Are Undergoing Seed Implantation
NCT00859027PHASE4COMPLETEDEffect Of Risedronate On Bone Mass In Older Men Receiving Neoadjuvant Therapy For Prostate Cancer
NCT00906269PHASE4UNKNOWNCan Hyperbaric Oxygen Improve Erectile Function Following Surgery for Prostate Cancer
NCT00953277PHASE4COMPLETEDStudy of Nerve Reconstruction Using AVANCE in Subjects Who Undergo Robotic Assisted Prostatectomy for Treatment of Prostate Cancer
NCT00982800PHASE4COMPLETEDDoes Postoperative Gabapentin Reduce Pain, Opioid Consumption and Anxiety and Have a Positive Effect on Health Related Quality of Life After Radical Prostatectomy?
NCT01083199PHASE4COMPLETEDGlobal Performance Evaluation of the AMS CONTINUUM™ Device
NCT01136226PHASE4COMPLETEDEvaluate Recovery of Testosterone for Patients Using Eligard
NCT01161563PHASE4COMPLETEDRandomized Crossover Trial to Assess the Tolerability of Gonadotropin Releasing Hormone (GnRH) Analogue Administration
NCT01230905PHASE4COMPLETEDStudy to Monitor the Effects of Androgen Suppression Treatment on the Heart
NCT01296672PHASE4COMPLETED3 Month Finasteride Challenge Test Can Significantly Improve the Performance of Screening for Prostate Cancer
NCT01365143PHASE4TERMINATEDProspective Randomized Trial Comparing Robotic Versus Open Radical Prostatectomy
NCT01379742PHASE4UNKNOWNComparison of Between ThinSeed™ and OncoSeed™ for Permanent Prostate Brachytherapy
NCT01486563PHASE4COMPLETEDHydroxyethyl Starch and Renal Function After Radical Prostatectomy
NCT01511874PHASE4COMPLETEDEfficacy and Safety Study of ELIGARD 22.5mg With Prostate Cancer
NCT01512472PHASE4TERMINATEDFirmagon (Degarelix) Intermittent Therapy
NCT01547416PHASE4COMPLETEDThe Effect of Combined General/Epidural Anesthesia Versus General Anesthesia on Diaphragmatic Function
NCT01571544PHASE4COMPLETEDThe Use of Thermal Suits as Preventing Hypothermia During Surgery
NCT01581749PHASE4UNKNOWNEvaluation of Truebeam for Low-Intermediate Risk Prostate Cancer
NCT01649635PHASE4COMPLETEDStudy of Cabazitaxel Combined With Prednisone and Prophylaxis of Neutropenia Complications in the Treatment of Patients With Metastatic Castration-resistant Prostate Cancer