bromodomain containing 3 | Bromodomain kinase (BRDK) family | IUPHAR/BPS Guide to PHARMACOLOGY

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bromodomain containing 3

Target not currently curated in GtoImmuPdb

Target id: 2725

Nomenclature: bromodomain containing 3

Abbreviated Name: BRD3

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 - 726 9q34 BRD3 bromodomain containing 3
Mouse - 743 2 A3 Brd3 bromodomain containing 3
Rat - 725 3p12 Brd3 bromodomain containing 3
Previous and Unofficial Names
ORFX | RING3L
Database Links
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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
XD14 Hs Inhibition 6.4 pKd 4
pKd 6.4 (Kd 3.8x10-7 M) [4]
Description: Assay using recombinant BRD3-BD1.
LY 294002 Hs Inhibition 6.0 pKd 3
pKd 6.0 (Kd 9.3x10-7 M) [3]
MS363 Hs Inhibition 6.6 pKi 8
pKi 6.6 (Ki 2.4x10-7 M) [8]
Description: Affinity at bromodomain 1 of BRD3.
GW841819X 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 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.
I-BET151 Hs Inhibition 6.6 pIC50 2
pIC50 6.6 (IC50 2.5x10-7 M) [2]
compound 38 [PMID: 24000170] Hs Inhibition 6.6 pIC50 6
pIC50 6.6 (IC50 2.51x10-7 M) [6]
compound 36 [PMID: 24000170] Hs Inhibition 6.3 pIC50 6
pIC50 6.3 (IC50 5.01x10-7 M) [6]
RVX 208 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
RVX 208 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. U.S.A., 110 (49): 19754-9. [PMID:24248379]

8. 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 15/10/2015. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2725.