Compile Data Set for Download or QSAR
Report error Found 94 Enz. Inhib. hit(s) with all data for entry = 50000746
TargetBromodomain-containing protein 3(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd: >3.00E+5nMAssay Description:Inhibition of poly-His tagged BRD3 bromodomain 2 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
Affinity DataKd:  135nMAssay Description:Inhibition of recombinant human His6-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells preincubated for 30 mins follo...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260087(CHEMBL4098784)
Affinity DataKd:  1.30nMAssay Description:Inhibition of biotin-labeled acetylated peptide binding to BRD4 bromodomain 1 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by BROMO...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 2(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
Affinity DataKd:  251nMAssay Description:Inhibition of recombinant human His6-tagged BRD2 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260088(GW841819X | CHEMBL2153434)
Affinity DataEC50:  440nMAssay Description:Inhibition of BRD4 in human HepG2 cells assessed as upregulation of ApoA1 by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 3(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
Affinity DataKd:  195nMAssay Description:Inhibition of recombinant human His6-tagged BRD3 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 3(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd:  3.70E+3nMAssay Description:Inhibition of poly-His tagged BRD3 bromodomain 2 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd:  8.60E+3nMAssay Description:Inhibition of poly-His tagged BRD2 bromodomain 1 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCREB-binding protein(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd:  3.30E+4nMAssay Description:Inhibition of poly-His tagged CREBBP (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
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
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 3(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50103503(CHEMBL2393130 | US11117865, Compound RVX-208)
Affinity DataKd:  4.07E+3nMAssay Description:Inhibition of poly-His tagged BRD3 bromodomain 1 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd: >3.00E+5nMAssay Description:Inhibition of poly-His tagged BRD4 bromodomain 2 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM298350(US10124009, Compound 5)
Affinity DataKd:  0.430nMAssay Description:Inhibition of biotin-labeled acetylated peptide binding to BRD4 bromodomain 1 (unknown origin) expressed in Escherichia coli BL21 after 1 hr by BROMO...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd:  3.30E+3nMAssay Description:Inhibition of poly-His tagged BRD4 bromodomain 1 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 2(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50148603(CHEMBL3770724)
Affinity DataKd: >3.00E+5nMAssay Description:Inhibition of poly-His tagged BRD2 bromodomain 2 (unknown origin) expressed in Escherichia coli BL21(DE3) by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260101(CHEMBL4068487 | US10689390, Compound 38 | US113193...)
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
In DepthDetails Article
PubMed
TargetSerine/threonine-protein kinase PLK1(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM25121(4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,...)
Affinity DataIC50: 0.830nMAssay Description:Inhibition of recombinant human N-terminal GST-tagged PLK1 (1 to 603 residues) expressed in baculovirus expression system using casein as substrate a...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260099(CHEMBL4075567)
Affinity DataIC50: 0.930nMAssay Description:Inhibition of recombinant His-tagged BRD4 (unknown origin) using biotinylated acetyl-histone H4 as substrate by AlphaLisa assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260074(CHEMBL4105618)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of recombinant His-tagged BRD4 (unknown origin) using biotinylated acetyl-histone H4 as substrate by AlphaLisa assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260073(CHEMBL4086168)
Affinity DataIC50: 2nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260078(CHEMBL4095826 | US10689390, Compound 26 | US113193...)
Affinity DataIC50: 2nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin) using biotinylated substrate after 1 hr by AlphaLisa assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM245884(US9428514, 72)
Affinity DataIC50: 2.30nMAssay 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
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260080(CHEMBL4088097 | US10689390, Compound 14 | US113193...)
Affinity DataIC50: 3nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin) using biotinylated substrate after 1 hr by AlphaLisa assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260095(CHEMBL4077359)
Affinity DataIC50: 3.10nMAssay Description:Inhibition of recombinant human His-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21(DE3) after 30 mins by AlphaScre...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260098(CHEMBL4082119)
Affinity DataIC50: 5nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM296964(2-[3-(Dimethyl-1H-1,2,3-triazol-5-yl)-6-fluoro-5-[...)
Affinity DataIC50: 5nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) using biotinylated histone peptide ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260093(CHEMBL4078100)
Affinity DataIC50: 5nMAssay Description:Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length BRD4 (unknown origin) expressed in HCT116 cells after 18 hrs by NanoBRET ass...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM296964(2-[3-(Dimethyl-1H-1,2,3-triazol-5-yl)-6-fluoro-5-[...)
Affinity DataIC50: 5nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) using biotinylated histone peptide ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260092(CHEMBL4076638)
Affinity DataIC50: 5nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) using biotinylated histone peptide ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetTyrosine-protein kinase JAK2(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM192755(TG101209 | US11643396, Example TG101209 | US112797...)
Affinity DataIC50: 6nMAssay Description:Inhibition of JAK2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50156344(CHEMBL3787210)
Affinity DataIC50: 8nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 (1 to 477 residues) expressed in Escherichia coli using tetra-acetylated histone peptide ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260069(CHEMBL4097251)
Affinity DataIC50: 9nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260100(CHEMBL4099187)
Affinity DataIC50: 10nMAssay Description:Inhibition of human BRD4 using acetylated histone H4 peptide as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260096(CHEMBL4087197)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (67 to 152 residues) expressed in Escherichia coli preincubated for 10 mins...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260086(CHEMBL4079312)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (67 to 152 residues) expressed in Escherichia coli preincubated for 10 mins...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260085(CHEMBL4103582)
Affinity DataIC50: 10nMAssay Description:Inhibition of recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (67 to 152 residues) expressed in Escherichia coli preincubated for 10 mins...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM274319(6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-di methyl-...)
Affinity DataIC50: 11nMAssay Description:Inhibition of His-tagged BRD4 (44 to 477 residues) (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM274304(1-(1-acetylazetidin-3-yl)-6-(4-chlorophenyl)-3-cyc...)
Affinity DataIC50: 11nMAssay Description:Inhibition of His-tagged BRD4 (44 to 477 residues) (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM150133(US8975417, 166)
Affinity DataIC50: 11nMAssay Description:Inhibition of His-tagged BRD4 (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM150062(US8975417, 122)
Affinity DataIC50: 11nMAssay Description:Inhibition of His-tagged BRD4 (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM245853(US9428514, 41)
Affinity DataIC50: 11nMAssay 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
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM215675(US9296748, I-11)
Affinity DataIC50: 12nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM274223(6-(4-chlorophenyl)-3-cyclopropyl-5-(3,8-dimethyl-[...)
Affinity DataIC50: 12nMAssay Description:Inhibition of His-tagged BRD4 (44 to 477 residues) (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260097(CHEMBL4067492)
Affinity DataIC50: 12nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260102(CHEMBL4059589)
Affinity DataIC50: 14nMAssay Description:Inhibition of GST-tagged BRD4 (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 mins by AlphaScreen assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260077(CHEMBL4065777)
Affinity DataIC50: 14nMAssay Description:Inhibition of human full length BRD4 using acetylated histone H4 peptide as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM150102(US8975417, 170)
Affinity DataIC50: 15nMAssay Description:Inhibition of His-tagged BRD4 (unknown origin) using acetyl-histone H4 as substrate after 35 mins by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260070(CHEMBL4080729)
Affinity DataIC50: 17nMAssay Description:Inhibition of GST-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) using biotinylated acetyl-histone H4 peptide as substrate after 30 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
University of Texas Medical Branch

Curated by ChEMBL
LigandPNGBDBM50260076(CHEMBL4072227)
Affinity DataIC50: 21nMAssay Description:Inhibition of human BRD4 using acetylated histone H4 peptide as substrate by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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