bromodomain containing 9 | Bromodomain kinase (BRDK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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bromodomain containing 9

Target not currently curated in GtoImmuPdb

Target id: 2728

Nomenclature: bromodomain containing 9

Abbreviated Name: BRD9

Family: Bromodomain kinase (BRDK) family

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 544 5p15.33 BRD9 bromodomain containing 9
Mouse - 597 13 C1 Brd9 bromodomain containing 9
Rat - 589 1p11 Brd9 bromodomain containing 9
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
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

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
BI-9564 Hs Inhibition 7.8 pKd 7
pKd 7.8 (Kd 1.4x10-8 M) [7]
LP99 Hs Inhibition 7.0 pKd 2
pKd 7.0 (Kd 9.9x10-8 M) [2]
Description: Isothermal titration calorimetry (ITC) assay
BI-7273 Hs Inhibition 7.7 pIC50 4
pIC50 7.7 (IC50 1.9x10-8 M) [4]
TP-472 Hs Inhibition 7.5 pIC50 6
pIC50 7.5 (IC50 3.3x10-8 M) [6]
Description: By isothermal titration calorimetry.
I-BRD9 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] 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 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 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. SGC. TP-472 A BRD9/7 Probe. Accessed on 05/04/2017. Modified on 05/04/2017. Structural Genomics Consortium., http://www.thesgc.org/chemical-probes/TP-472

7. Structural Genomics Consortium. BI-9564 A chemical probe for BRD9 and BRD7. Accessed on 11/12/2015. Modified on 11/12/2015. The Structural Genomics Consortium, http://www.thesgc.org/chemical-probes/BI-9564

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 15/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2728.