BDBM205429 (R)-JQ1 (3)::US10407441, Compound (R)-JQ1::US10925881, Name (R)-JQ1::US11028051, Cmpd (+)-JQ1::US11117865, Compound JQ1::US11306105, Compound JQ1::US11406645, Compound JQ1::US11542273, Example (+)-JQ1::US9320741, (R)-JQ1

SMILES Cc1nnc2[C@@H](CC(=O)OC(C)(C)C)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1

InChI Key InChIKey=DNVXATUJJDPFDM-QGZVFWFLSA-N

Data  25 IC50  16 Kd

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 41 hits for monomerid = 205429   

TargetBromodomain-containing protein 2 [71-194](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  27nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [44-167](Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  29nMAssay Description:Acetyl-Histone Binding Assay. Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElme...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [71-194,348-455](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  5.60nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3 [24-144](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  14nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3 [306-416](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  19nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3 [24-144,306-416](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  14nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [44-168](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  14nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [333-460](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  8.20nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [44-168,333-460](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  7.30nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsoform C of Bromodomain-containing protein 4 (Short)(Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  11nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein [21-137](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  47nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein [251-382](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  35nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein [21-137,251-382](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  46nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [44-168](Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  21nMpH: 7.5 T: 2°CAssay Description:Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIsoform C of Bromodomain-containing protein 4 (Short)(Homo sapiens (Human))
Dana-Farber Cancer Institute

LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  7.76E+3nMpH: 7.5 T: 2°CAssay Description:Assays were performed with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were diluted in 50 mM HEPES, 150...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  8.35E+6nMpH: 7.4 T: 2°CAssay Description:BRD4(1): 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
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  5.21E+7nMpH: 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
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [75-147](Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  8.35E+6nMAssay 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
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [368-440](Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  5.21E+7nMAssay 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
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  49nMAssay Description:Inhibition of human BRD4 bromodomain1 expressed in BL21(DE3) cells by isothermal calorimetryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4 [44-167](Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  8.35E+6nMAssay Description:The binding activity of lead compounds with the BRD4 site 1 was determined by Alpha-assay with a 12-point dose response curveMore data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [349-460](Homo sapiens (Human))
Tensha Therapeutics

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  5.21E+7nMAssay 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
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [91-163](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  78nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [364-436](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  52nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 3 [51-123](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  81nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 3 [326-398](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  69nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain testis-specific protein [22-138](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  183nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain testis-specific protein [287-359](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  217nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCREB-binding protein(Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  9.60E+3nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [49-170](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  92nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [342-460](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  62nMAssay Description:Determine the binding ability of BRD4 compounds to bromodomains of BRD2 and BRD4. 96 well plate based commercial TR-FRET Assay kits (Cayman Chemical,...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [74-94](Homo sapiens (Human))
St. Jude Children'S Research Hospital

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  89nMAssay Description:Binding of compounds to BRD2 was monitored using an ITC200 (Microcal, Piscataway, N.J.). Either Brd2.1 (74-194) or Brd2.2 (348-455) was dialyzed over...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [348-455](Homo sapiens (Human))
St. Jude Children'S Research Hospital

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  112nMAssay Description:Binding of compounds to BRD2 was monitored using an ITC200 (Microcal, Piscataway, N.J.). Either Brd2.1 (74-194) or Brd2.2 (348-455) was dialyzed over...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  77nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  33nMAssay Description:Inhibition of human His-tagged BRD4 bromodomain2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells using H4K5acK8acK12acK16ac as substrate prei...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain testis-specific protein [22-138](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  77nMAssay Description:Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were dil...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4 [44-167](Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  29nMAssay Description:Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElmer, USA). All reagents were dil...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  7.40E+3nMAssay Description:Table 4-1: The inhibitory action of the compound of the present invention on the binding of BRD4 protein and a ligand thereof was evaluated by the ti...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 4(Homo sapiens (Human))
Dana-Farber Cancer Institute

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  550nMAssay Description:Table 4-2: The inhibitory action of the compound of the present invention on the binding of BRD4 protein and a ligand thereof (acetylated histone H4)...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain testis-specific protein [22-138](Homo sapiens (Human))
Board Of Regents, The University Of Texas System

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataIC50:  77nMAssay Description:Acetyl-Histone Binding Assay. Assays were performed as described previously with minor modifications from the manufacturer's protocol (PerkinElme...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetBromodomain-containing protein 2 [348-455](Homo sapiens (Human))
St. Jude Children'S Research Hospital

US Patent
LigandPNGBDBM205429( (R)-JQ1 (3) | US10407441, Compound (R)-JQ1 | US10...)
Affinity DataKd:  18nMAssay Description:Refer to DiscoverXMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed