BDBM50103503 CHEMBL2393130::US11117865, Compound RVX-208
SMILES COc1cc(OC)c2c(c1)nc([nH]c2=O)-c1cc(C)c(OCCO)c(C)c1
InChI Key InChIKey=NETXMUIMUZJUTB-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 96 hits for monomerid = 50103503
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 645nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by europium based LANCE TR-FRET assayMore data for this Ligand-Target Pair
3D Structure (crystal)TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 303nMAssay Description:Binding affinity to human BRD4 bromodomain 2 by isothermal titration calorimetryMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 8.93E+3nMAssay Description:Binding affinity to human BRD4 bromodomain 1 by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 206nMAssay Description:Binding affinity to human BRD2 bromodomain 2 by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 1.69E+4nMAssay Description:Binding affinity to human BRD2 bromodomain 1 by isothermal titration calorimetryMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 140nMAssay Description:Binding affinity to human BRD4 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetryMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 1.10E+3nMAssay Description:Binding affinity to human BRD4 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 250nMAssay Description:Binding affinity to human BRD2 bromodomain 2 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetryMore data for this Ligand-Target Pair
Affinity DataKd: 5.80E+3nMAssay Description:Binding affinity to human BRD2 bromodomain 1 expressed in Escherichia coli BL21 (DE3) cells by isothermal titration calorimetryMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataIC50: 510nMAssay Description:Inhibition of human His-tagged BRD3 bromodomain 2 using biotin-H4K5acK8acK12acK16ac as substrate incubated for 30 mins by alphascreen assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 1.10E+3nMAssay Description:Binding affinity to BRD4 bromodomain 1 (unknown origin) by isothermal titration calorimetric analysisMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 140nMAssay Description:Binding affinity to BRD4 bromodomain 2 (unknown origin) by isothermal titration calorimetric analysisMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of human His-tagged BRD4 BD1 (49 to 170 residues) using H-SGRGK(Ac)GGK(Ac)GLGK-(Ac)GGAK(Ac)RHRK(Biotin)-OH as substrate preincubated for 3...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 610nMAssay Description:Inhibition of human BRD4 BD2 (342 to 460 residues) at 30 uM preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of His/thioredoxin-tagged human recombinant BRD4 bromodomain-1 (43 to 166 residues) expressed in Escherichia coli BL21 Star (DE3) pre-incu...More data for this Ligand-Target Pair
Affinity DataKd: 5.78E+3nMAssay Description:Inhibition of recombinant human His6-tagged BRD2 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cellsMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 1.14E+3nMAssay Description:Inhibition of recombinant human His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins follo...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataKd: 4.07E+3nMAssay Description:Inhibition of recombinant human His6-tagged BRD3 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cellsMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 67nMAssay Description:Inhibition of human BRD4 bromo domain 2More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 3.85E+3nMAssay Description:Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced IL-8 RNA expression preincubated for 24 hrs followed b...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataIC50: 3.96E+3nMAssay Description:Inhibition of BRD3 BD1 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 251nMAssay Description:Inhibition of BRD2 BD2 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataIC50: 203nMAssay Description:Inhibition of BRD3 BD2 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 2.63E+3nMAssay Description:Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG54 RNA expression preincubated for 24 hrs followed ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 2.74E+3nMAssay Description:Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced ISG56 RNA expression preincubated for 24 hrs followed ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 1.14E+3nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 3.73E+3nMAssay Description:Inhibition of BRD4 in human SAE cells assessed as reduction in TLR3 agonist poly(I:C) -induced grobeta RNA expression preincubated for 24 hrs followe...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 135nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 5.78E+3nMAssay Description:Inhibition of BRD2 BD1 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain testis-specific protein(Homo sapiens (Human))
University Of Texas Medical Branch
Curated by ChEMBL
University Of Texas Medical Branch
Curated by ChEMBL
Affinity DataIC50: 4.84E+3nMAssay Description:Inhibition of BRDT BD1 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain testis-specific protein(Homo sapiens (Human))
University Of Texas Medical Branch
Curated by ChEMBL
University Of Texas Medical Branch
Curated by ChEMBL
Affinity DataIC50: 708nMAssay Description:Inhibition of BRDT BD2 (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of CBP (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 1.59E+3nMAssay Description:Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataKd: 4.00E+3nMAssay Description:Binding affinity to human BRD3 BD2 by ITC methodMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 6.31E+3nMAssay Description:Displacement of (+)-JQ1 from 6H-Thr BRD4 Y390A mutant BD1 (unknown origin) after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 135nMAssay Description:Inhibition of His-tagged BRD4 bromodomain 1 (K57 to E168 residues) (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataKd: 251nMAssay Description:Inhibition of recombinant His-tagged BRD4 bromodomain 2 (E352 to E168 residues) (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataKd: 195nMAssay Description:Inhibition of recombinant His-tagged BRD4 bromodomain 2 (E352 to E168 residues) (unknown origin) after 1 hr by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 1.99E+3nMAssay Description:Inhibition of C-terminal biotin-labelled BCoR/wild-type BCL6 BTB domain (unknown origin) protein-protein interaction by ELISAMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 510nMAssay Description:Inhibition of C-terminal biotin-labelled BCoR/wild-type BCL6 BTB domain (unknown origin) protein-protein interaction by ELISAMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 130nMAssay Description:Inhibition of human 6x-His-tagged BRD4 bromodomain 2 expressed in Escherichia coliMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataKd: 4.00E+3nMAssay Description:Inhibition of human 6x-His-tagged BRD3 bromodomain 1 expressed in Escherichia coliMore data for this Ligand-Target Pair
Affinity DataKd: 5.80E+3nMAssay Description:Inhibition of human 6x-His-tagged BRD2 bromodomain 1 expressed in Escherichia coliMore data for this Ligand-Target Pair
Affinity DataKd: 250nMAssay Description:Inhibition of human 6x-His-tagged BRD2 bromodomain 2 expressed in Escherichia coliMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataKd: 190nMAssay Description:Inhibition of human 6x-His-tagged BRD3 bromodomain 2 expressed in Escherichia coliMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataKd: 1.10E+3nMAssay Description:Inhibition of human 6x-His-tagged BRD4 bromodomain 1 expressed in Escherichia coliMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 510nMAssay Description:Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using his...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Guangzhou Institutes Of Biomedicine And Health
Curated by ChEMBL
Affinity DataIC50: 510nMAssay Description:Displacement of tetra-acetylated histone H4 peptide from recombinant human His-tagged BRD3 BD2 expressed in bacterial expression system by alphascree...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 1.80E+3nMAssay Description:Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD1 incubated for 2 hrs by TR-FRET assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
The University Of Tokyo
Curated by ChEMBL
The University Of Tokyo
Curated by ChEMBL
Affinity DataIC50: 40nMAssay Description:Displacement of tetra-acetylated histone H4 peptide from recombinant human N-terminal His-tagged BRD4 BD2 incubated for 2 hrs by TR-FRET assayMore data for this Ligand-Target Pair