Affinity DataIC50: 0.100nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.130nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
Affinity DataIC50: 0.152nMAssay Description:3x Complete Substrate plus Inhibitor Solution in Assay Medium (Opti-MEM I Reduced Serum Medium, no phenol red, and no serum) was prepared just before...More data for this Ligand-Target Pair
Affinity DataIC50: 0.152nMAssay Description:3x Complete Substrate plus Inhibitor Solution in Assay Medium (Opti-MEM I Reduced Serum Medium, no phenol red, and no serum) was prepared just before...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
Affinity DataIC50: 0.200nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
Affinity DataIC50: 0.240nMpH: 7.4 T: 2°CAssay Description:BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.240nMAssay Description:The binding activity of lead compounds with the BRD4 site 2 was determined by Alpha-assay with a 12-point dose response curveMore data for this Ligand-Target Pair
Affinity DataIC50: 0.240nMAssay Description:All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.25nMAssay Description:In the present application, the IC50 value of the compound of formula (I) in inhibiting BRD4 (BD1) enzyme binding reaction were determined by homogen...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.25nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.270nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
Affinity DataIC50: 0.300nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
Affinity DataIC50: 0.300nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
Affinity DataIC50: 0.323nMAssay Description:3x Complete Substrate plus Inhibitor Solution in Assay Medium (Opti-MEM I Reduced Serum Medium, no phenol red, and no serum) was prepared just before...More data for this Ligand-Target Pair
Affinity DataIC50: 0.330nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.340nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.340nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
Affinity DataIC50: 0.340nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.350nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.350nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
Affinity DataIC50: 0.390nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.398nMAssay Description:Inhibition of human BRD4 bromodomain 1 by BROMOscan assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.398nMAssay Description:Inhibition of human BRD4 bromodomain 1/2 by BROMOscan assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:The following experiment was performed to evaluate the ability of [1,2,4]triazolo[4,3-a]quinoxaline derivative of the present invention to inhibit th...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
Ligand InfoSimilars
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.400nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.400nMAssay Description:The assays of BRD4 (D1) and BRD4 (D2) were conducted in a 384-well polystyrene plate. The test compounds were first serially diluted in DMSO and the ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of BRD4 (unknown origin) incubated for 2 hrs by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.400nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 0.410nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.420nMAssay Description:Inhibition of poly His-tagged BRD4 BD2 (unknown origin) (348 to 455 residues) by BROMOscan assayMore data for this Ligand-Target Pair
Affinity DataIC50: 0.427nMpH: 7.4 T: 2°CAssay Description:BRD4(2): Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents wer...More data for this Ligand-Target Pair
Affinity DataIC50: 0.427nMAssay Description:All reagents were diluted in 50 mM HEPES, 100 mM NaCl, 0.1% BSA, pH 7.4 supplemented with 0.05% CHAPS and allowed to equilibrate to room temperature ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.427nMAssay Description:The binding activity of lead compounds with the BRD4 site 2 was determined by Alpha-assay with a 12-point dose response curveMore data for this Ligand-Target Pair
Affinity DataIC50: 0.430nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD1 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.450nMAssay Description:In the present application, IC50 values of the compounds in inhibiting BRD4 (BD2) enzyme binding reaction were determined by homogeneous time resolve...More data for this Ligand-Target Pair
Affinity DataIC50: 0.450nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.460nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.473nMAssay Description:3x Complete Substrate plus Inhibitor Solution in Assay Medium (Opti-MEM I Reduced Serum Medium, no phenol red, and no serum) was prepared just before...More data for this Ligand-Target Pair
Affinity DataIC50: 0.480nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
Affinity DataIC50: 0.490nMAssay Description:Briefly, 20 nL of compounds were transferred to the 384-well plate by Echo 550 liquid handler (Labcyte, USA), then 5 μL of BRD4(BD1) (Reaction B...More data for this Ligand-Target Pair
Affinity DataIC50: 0.490nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.490nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin) using biotinylated substrate after 1 hr by AlphaLisa assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.5nMAssay Description:The assays of BRD4 (D1) and BRD4 (D2) were conducted in a 384-well polystyrene plate. The test compounds were first serially diluted in DMSO and the ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4 [349-460](Human)
Chia Tai Tianqing Pharmaceutical Group
US Patent
Chia Tai Tianqing Pharmaceutical Group
US Patent
Affinity DataIC50: 0.5nMAssay Description:The assays of BRD4 (D1) and BRD4 (D2) were conducted in a 384-well polystyrene plate. The test compounds were first serially diluted in DMSO and the ...More data for this Ligand-Target Pair
Affinity DataIC50: 0.5nMAssay Description:Inhibition of C-terminal His6-tagged BRD4 BD2 (unknown origin) using H-YSGRGK(Ac)GGK(Ac)GLGK(Ac)-GGAK(Ac)RHRK-Biotin-OH as substrate incubated for 1 ...More data for this Ligand-Target Pair











































