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
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
RefSeq Nucleotide
RefSeq Protein
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.
Ligand:  I-BRD9
Resolution:  1.73Å
Species:  Human
References:  6
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:  3
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:  3

Download all structure-activity data for this target as a CSV file

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 5
pKd 7.8 (Kd 1.4x10-8 M) [5]
LP99 Hs Inhibition 7.0 pKd 1
pKd 7.0 (Kd 9.9x10-8 M) [1]
Description: Isothermal titration calorimetry (ITC) assay
BI-7273 Hs Inhibition 7.7 pIC50 3
pIC50 7.7 (IC50 1.9x10-8 M) [3]
TP-472 Hs Inhibition 7.5 pIC50 4
pIC50 7.5 (IC50 3.3x10-8 M) [4]
Description: By isothermal titration calorimetry.
I-BRD9 Hs Binding 7.1 pIC50 6
pIC50 7.1 (IC50 7.94x10-8 M) [6]
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 2
pIC50 6.5 (IC50 3.16x10-7 M) [2]


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1. 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]

2. 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]

3. 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]

4. SGC. TP-472 A BRD9/7 Probe. Accessed on 05/04/2017. Modified on 05/04/2017. Structural Genomics Consortium.,

5. 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,

6. 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 05/04/2017. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY,