BDBM50092312 Birabresib::MK-8628::OTX-015

SMILES [H][C@@]1(CC(=O)Nc2ccc(O)cc2)N=C(c2c(C)c(C)sc2-n2c(C)nnc12)c1ccc(Cl)cc1

InChI Key InChIKey=GNMUEVRJHCWKTO-FQEVSTJZSA-N

Data  20 KI  33 IC50

PDB links: 1 PDB ID matches this monomer.

  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 53 hits for monomerid = 50092312   

TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  4nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  4nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  5.40nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  5.40nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  5.70nMAssay Description:Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  6nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  6nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by f...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  8.70nMAssay Description:Binding affinity to human recombinant BRD3 BD1 (24 to 144 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  9.90nMAssay Description:Binding affinity to human recombinant BRD4 BD2 (333 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  10nMAssay Description:Binding affinity to human recombinant BRD2 BD2 (349 to 460 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  11nMAssay Description:Binding affinity to human recombinant BRD3 BD2 (306 to 417 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  12nMAssay Description:Binding affinity to human recombinant BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  17nMAssay Description:Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fl...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  17nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  27nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) using FAM-labeled JQ-1 as fluorescent substrate assessed as inhibition constant incubated for 30 mins by comp...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataKi:  33nMAssay Description:Binding affinity to human recombinant BRD2 BD1 (72 to 205 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  197nMAssay Description:Inhibition of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K-Biotin binding to N-terminal His6-tagged BRD4 bromodomain 2 (344 to 455 residues) (un...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair
TargetHistone deacetylase 1(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of HDAC1 (unknown origin) by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone deacetylase 6(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of HDAC6 (unknown origin) by fluorescence based assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  9.20nMAssay Description:Inhibition of His-tagged BRD4 bromodomain 1 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  15nMAssay Description:Inhibition of His-tagged BRD4 bromodomain 2 (unknown origin) using [Lys (5,8,12,16) Ac] H4(1-21) as substrate by fluorescence based assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  15nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) fluorescence polarization methodMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  12nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) fluorescence polarization methodMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  15nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) by fluorescence based assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  12nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) by fluorescence based assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of BRD2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  41nMAssay Description:Inhibition of SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K-Biotin binding to N-terminal His6-tagged BRD4 bromodomain 1 (49 to 170 residues) (unk...More data for this Ligand-Target Pair
TargetHistone acetyltransferase p300(Homo sapiens (Human))
Chinese Academy Of Sciences

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50: >3.30E+4nMAssay Description:Inhibition of MSGRGK(Ac)-GGK(Ac)GLGK(Ac)GGAKRHR-biotin binding to EP300 (1040 to 1160 residues) (unknown origin) expressed in Escherichia coli BL21 (...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  34nMAssay Description:Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incu...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  34nMAssay Description:Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incu...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  23nMAssay Description:Binding affinity to human BRD4 BD1 (44 to 168 residues) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay 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))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  21nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 2 (306 to 417residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  17nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) (unknown origin) expressed in...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  33nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 1 (72 to 205 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  25nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD2 bromodomain 2 (349 to 460 residues) (unknown origin) expressed in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  39nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD3 bromodomain 1 (24 to 144 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  26nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) (unknown origin) expressed in ...More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by AlphaScreen assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 2(Homo sapiens (Human))
University Of Michigan

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of acetylated H4 binding to BRD2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 3(Homo sapiens (Human))
University Of Michigan Comprehensive Cancer Center

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of acetylated H4 binding to BRD3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  92nMAssay Description:Inhibition of acetylated H4 binding to BRD4 (unknown origin)More data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50:  16nMAssay Description:Inhibition of BRD4 BD1-BD2 (unknown origin) using tetraacetylated histone peptide as substrate after 2 hrs by alphascreen assayMore data for this Ligand-Target Pair
TargetBromodomain-containing protein 4(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50092312(Birabresib | MK-8628 | OTX-015)
Affinity DataIC50: <20nMAssay Description:Inhibition of BRD4 bromodomain 1 (unknown origin)More data for this Ligand-Target Pair
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