Affinity DataKd: 0.0950nMAssay Description:Inhibition of recombinant human BRD4-1 (44 to 168 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
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
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: 0.240nMpH: 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
Affinity DataKi: 0.25nM ΔG°: -54.8kJ/molepH: 6.0 T: 2°CAssay Description:A time-resolved fluorescence resonance energy transfer (TR-FRET) assay was used to determine the affinities of compounds of the Examples listed in Ta...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
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: 0.270nMAssay 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 DataKd: 0.290nMAssay Description:Binding affinity to BRD4-T (unknown origin)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: 0.300nMAssay 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 DataKd: 0.300nMAssay Description:Binding affinity to human partial length BRD4 BD2 expressed in bacterial expression system assessed as dissociation constant by BROMOscan assayMore data for this Ligand-Target Pair
Affinity DataKd: 0.320nMAssay Description:Inhibition of recombinant human BRD4-2 (333 to 460 residues) expressed in bacterial expression system by bromoscan assayMore data for this Ligand-Target Pair
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
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
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
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: 0.350nMAssay 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
























3D Structure (crystal)





