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bromodomain containing 3

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Target id: 2725

Nomenclature: bromodomain containing 3

Abbreviated Name: BRD3

Family: Bromodomain kinase (BRDK) family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 726 9q34.2 BRD3 bromodomain containing 3
Mouse - 726 2 A3 Brd3 bromodomain containing 3
Rat - 725 3p12 Brd3 bromodomain containing 3
Previous and Unofficial Names Click here for help
ORFX | RING3L
Database Links Click here for help
Alphafold
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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
ARV-771 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pKd 8
pKd 8.1 (Kd 7.6x10-9 M) [8]
Description: Binding affinity for bromodomain 2 of hBRD3.
XD14 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pKd 4
pKd 6.4 (Kd 3.8x10-7 M) [4]
Description: Assay using recombinant BRD3-BD1.
LY 294002 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.0 pKd 3
pKd 6.0 (Kd 9.3x10-7 M) [3]
MS363 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pKi 10
pKi 6.6 (Ki 2.4x10-7 M) [10]
Description: Affinity at bromodomain 1 of BRD3.
GW841819X Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 1
pIC50 7.6 (IC50 2.84x10-8 M) [1]
Description: Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD3.
molibresib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.4 pIC50 1
pIC50 7.4 (IC50 4.22x10-8 M) [1]
Description: Displacement of a tetra-acetylated histone H4 peptide from the tandem BET bromodomains of BRD3.
WNY0824 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 9
pIC50 6.8 (IC50 1.51x10-7 M) [9]
I-BET151 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.6 pIC50 2
pIC50 6.6 (IC50 2.5x10-7 M) [2]
compound 38 [PMID: 24000170] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.6 pIC50 6
pIC50 6.6 (IC50 2.51x10-7 M) [6]
compound 36 [PMID: 24000170] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 6
pIC50 6.3 (IC50 5.01x10-7 M) [6]
apabetalone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 4.1 – 5.3 pIC50 7
pIC50 5.3 (IC50 4.9x10-6 M) [7]
Description: AlphaScreen data assessing the bromodomain 2 domain of BRD3.
pIC50 4.1 (IC50 8.7x10-5 M) [7]
Description: AlphaScreen data for bromodomain 1 of BRD3.
Inhibitor Comments
Data for RVX-208 is shown in two separate rows to highlight the difference in inhibitor affinity between the two bromodomains of BRD3.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
apabetalone Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist 6.6 pIC50 5
pIC50 6.6 (IC50 2.8x10-7 M) [5]
Description: Measured using a TR-FRET assay to evaluate binding to BD2 of BRD3.

References

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1. Chung CW, Coste H, White JH, Mirguet O, Wilde J, Gosmini RL, Delves C, Magny SM, Woodward R, Hughes SA et al.. (2011) Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem, 54 (11): 3827-38. [PMID:21568322]

2. Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM et al.. (2011) Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature, 478 (7370): 529-33. [PMID:21964340]

3. Dittmann A, Werner T, Chung CW, Savitski MM, Fälth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK et al.. (2014) The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains. ACS Chem Biol, 9 (2): 495-502. [PMID:24533473]

4. Lucas X, Wohlwend D, Hügle M, Schmidtkunz K, Gerhardt S, Schüle R, Jung M, Einsle O, Günther S. (2013) 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl, 52 (52): 14055-9. [PMID:24272870]

5. McLure KG, Gesner EM, Tsujikawa L, Kharenko OA, Attwell S, Campeau E, Wasiak S, Stein A, White A, Fontano E et al.. (2013) RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS ONE, 8 (12): e83190. [PMID:24391744]

6. Mirguet O, Lamotte Y, Chung CW, Bamborough P, Delannée D, Bouillot A, Gellibert F, Krysa G, Lewis A, Witherington J et al.. (2014) Naphthyridines as novel BET family bromodomain inhibitors. ChemMedChem, 9 (3): 580-9. [PMID:24000170]

7. Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H et al.. (2013) RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci USA, 110 (49): 19754-9. [PMID:24248379]

8. Raina K, Lu J, Qian Y, Altieri M, Gordon D, Rossi AM, Wang J, Chen X, Dong H, Siu K et al.. (2016) PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci USA, 113 (26): 7124-9. [PMID:27274052]

9. Wang NY, Xu Y, Xiao KJ, Zuo WQ, Zhu YX, Hu R, Wang WL, Shi YJ, Yu LT, Liu ZH. (2020) Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem, 191: 112152. [PMID:32088495]

10. Zhang G, Plotnikov AN, Rusinova E, Shen T, Morohashi K, Joshua J, Zeng L, Mujtaba S, Ohlmeyer M, Zhou MM. (2013) Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains. J Med Chem, 56 (22): 9251-64. [PMID:24144283]

How to cite this page

Bromodomain kinase (BRDK) family: bromodomain containing 3. Last modified on 23/08/2022. Accessed on 12/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2725.