Target family: Bromodomain kinase (BRDK) family (type: enzyme)
Target: bromodomain containing 2

Ligand: XD14 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.769999980926514 pKd
Reference (Journal): 4-Acyl pyrroles: mimicking acetylated lysines in histone code reading.
Published in: Angew Chem Int Ed Engl

Ligand: SIM1 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 10.479999542236328 pKd
Reference (Journal): Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity.
Published in: Nat Chem Biol

Ligand: molibresib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 pIC50
Reference (Journal): Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Published in: J Med Chem

Ligand: ME bromodomain inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.
Published in: Science

Ligand: LY 294002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.849999904632568 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: 6.300000190734863 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: 7.519999980926514 pIC50
Reference (Journal): Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Published in: J Med Chem

Ligand: GSK852 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Journal): Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Published in: J Med Chem

Ligand: GSK852 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pKd
Reference (Journal): Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Published in: J Med Chem

Ligand: ET bromodomain inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.
Published in: Science

Ligand: compound 4d [PMID: 21851057] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): 3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
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: 6.300000190734863 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 pIC50
Reference (Journal): Naphthyridines as novel BET family bromodomain inhibitors.
Published in: ChemMedChem

Ligand: BIC1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.550000190734863 pKd
Reference (Journal): Real-time imaging of histone H4K12-specific acetylation determines the modes of action of histone deacetylase and bromodomain inhibitors.
Published in: Chem Biol

Ligand: ARV-771 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 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: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.050000190734863 pIC50
Reference (Journal): RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist.
Published in: PLoS ONE