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bromodomain containing 9

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Target id: 2728

Nomenclature: bromodomain containing 9

Abbreviated Name: BRD9

Family: Bromodomain kinase (BRDK) family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 597 5p15.33 BRD9 bromodomain containing 9
Mouse - 596 13 C1 Brd9 bromodomain containing 9
Rat - 589 1p11 Brd9 bromodomain containing 9
Database Links Click here for help
Alphafold Q9H8M2 (Hs), Q3UQU0 (Mm)
CATH/Gene3D 1.20.920.10
ChEMBL Target CHEMBL3108640 (Hs), CHEMBL3822347 (Mm)
Ensembl Gene ENSG00000028310 (Hs), ENSMUSG00000057649 (Mm), ENSRNOG00000015676 (Rn)
Entrez Gene 65980 (Hs), 105246 (Mm), 308067 (Rn)
Human Protein Atlas ENSG00000028310 (Hs)
KEGG Gene hsa:65980 (Hs), mmu:105246 (Mm), rno:308067 (Rn)
Pharos Q9H8M2 (Hs)
RefSeq Nucleotide NM_001009877 (Hs), NM_001024508 (Mm), NM_001107453 (Rn)
RefSeq Protein NP_001009877 (Hs), NP_001019679 (Mm), NP_001100923 (Rn)
SynPHARM 83214 (in complex with BI-9564)
82102 (in complex with I-BRD9)
82362 (in complex with LP99)
UniProtKB Q9H8M2 (Hs), Q3UQU0 (Mm)
Wikipedia BRD9 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  BROMODOMAIN OF HUMAN BRD9 WITH N-(1,1-dioxo-1-thian-4-yl)-5-ethyl-4-oxo-7-3-(trifluoromethyl)phenyl-4H,5H-thieno-3,2-c-pyridine-2- carboximidamide.
PDB Id:  4UIW
Ligand:  I-BRD9
Resolution:  1.73Å
Species:  Human
References:  8
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the BRD9 bromodamian in complex with BI-9564
PDB Id:  5F1H
Ligand:  BI-9564
Resolution:  1.82Å
Species:  Human
References:  4
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of BRD9 in complex with BI-7273.
PDB Id:  5EU1
Ligand:  BI-7273
Resolution:  1.6Å
Species:  Human
References:  4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BI-9564 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pKd 6
⤷ pKd 7.8 (Kd 1.4x10-8 M) [6]
LP99 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.0 pKd 2
⤷ pKd 7.0 (Kd 9.9x10-8 M) [2]
Description: Isothermal titration calorimetry (ITC) assay
BI-7273 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.7 pIC50 4
⤷ pIC50 7.7 (IC50 1.9x10-8 M) [4]
TP-472 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 7
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [7]
Description: By isothermal titration calorimetry.
I-BRD9 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Binding 7.1 pIC50 8
⤷ pIC50 7.1 (IC50 7.94x10-8 M) [8]
Description: Binding affinity for endogenous BRD9 from HuT-78 cell lysates, measured in a chemoproteomic competition binding assay followed by Western blot analysis.
compound 50 [PMID: 24313754] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.5 pIC50 3
⤷ pIC50 6.5 (IC50 3.16x10-7 M) [3]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
dBRD9-A Small molecule or natural product Hs Binding 7.1 pIC50 1
⤷ pIC50 7.1 (IC50 8.31x10-8 M) [1]
Description: In vitro binding affinity determined by an AlphaScreen displacement ligand binding assay.
dBRD9 Small molecule or natural product Click here for species-specific activity table Hs Binding 7.0 pIC50 5
⤷ pIC50 7.0 (IC50 1.04x10-7 M) [5]
Description: AlphaScreen competitive ligand binding assay using recombinant BRD9.

References

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1. Brien GL, Remillard D, Shi J, Hemming ML, Chabon J, Wynne K, Dillon ET, Cagney G, Van Mierlo G, Baltissen MP et al.. (2018) Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma. Elife, 7: e41305. DOI: 10.7554/eLife.41305 [PMID:30431433]

2. Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S et al.. (2015) LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl, 54 (21): 6217-21. [PMID:25864491]

3. Fedorov O, Lingard H, Wells C, Monteiro OP, Picaud S, Keates T, Yapp C, Philpott M, Martin SJ, Felletar I et al.. (2014) [1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains. J Med Chem, 57 (2): 462-76. [PMID:24313754]

4. Martin LJ, Koegl M, Bader G, Cockcroft XL, Fedorov O, Fiegen D, Gerstberger T, Hofmann MH, Hohmann AF, Kessler D et al.. (2016) Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem, 59 (10): 4462-75. [PMID:26914985]

5. Remillard D, Buckley DL, Paulk J, Brien GL, Sonnett M, Seo HS, Dastjerdi S, Wühr M, Dhe-Paganon S, Armstrong SA et al.. (2017) Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl, 56 (21): 5738-5743. [PMID:28418626]

6. SCC. BI-9564 A chemical probe for BRD9 and BRD7. Accessed on 11/12/2015. Modified on 11/12/2015. thesgc.org, http://www.thesgc.org/chemical-probes/BI-9564

7. SGC. TP-472 A BRD9/7 Probe. Accessed on 05/04/2017. Modified on 04/08/2023. Structural Genomics Consortium., https://www.thesgc.org/chemical-probes/TP-472

8. Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH et al.. (2016) Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem, 59 (4): 1425-39. [PMID:25856009]

How to cite this page

Bromodomain kinase (BRDK) family: bromodomain containing 9. Last modified on 12/11/2019. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2728.