Target family: Bromodomain kinase (BRDK) family (type: enzyme)
Target: bromodomain containing 3

Ligand: XD14 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.420000076293945 pKd
Reference (Journal): 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading.
Published in: Angew Chem Int Ed Engl

Ligand: WNY0824 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors.
Published in: Eur J Med Chem

Ligand: MS363 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pKi
Reference (Journal): Structure-guided design of potent diazobenzene inhibitors for the BET bromodomains.
Published in: J Med Chem

Ligand: molibresib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.369999885559082 pIC50
Reference (Journal): Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Published in: J Med Chem

Ligand: LY 294002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.03000020980835 pKd
Reference (Journal): The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains.
Published in: ACS Chem Biol

Ligand: I-BET151 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Published in: Nature

Ligand: GW841819X (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pIC50
Reference (Journal): Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Published in: J Med Chem

Ligand: compound 38 [PMID: 24000170] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Naphthyridines as novel BET family bromodomain inhibitors.
Published in: ChemMedChem

Ligand: compound 36 [PMID: 24000170] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Naphthyridines as novel BET family bromodomain inhibitors.
Published in: ChemMedChem

Ligand: ARV-771 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.119999885559082 pKd
Reference (Journal): PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Published in: Proc Natl Acad Sci USA

Ligand: apabetalone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 pIC50
Reference (Journal): RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Published in: Proc Natl Acad Sci USA

Ligand: apabetalone (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.059999942779541 pIC50
Reference (Journal): RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.
Published in: Proc Natl Acad Sci USA

Ligand: apabetalone (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.550000190734863 pIC50
Reference (Journal): RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
Published in: PLoS ONE