BDBM50365463 CHEMBL1232461

SMILES CCNC(=O)C[C@@H]1N=C(c2ccc(Cl)cc2)c2cc(OC)ccc2-n2c(C)nnc12

InChI Key InChIKey=AAAQFGUYHFJNHI-UHFFFAOYSA-N

Data  20 KI  47 IC50  30 Kd  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 98 hits for monomerid = 50365463   

TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 68nMAssay Description:Inhibition of His-tagged human BRD4-BD1 using H4K5acK8acK12acK16ac as substrate preincubated for 30 mins followed by substrate addition measured afte...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataEC50:  440nMAssay Description:Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced TNFalpha secretion preincubated for 1 hr followed by LPS-stimulation and measur...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 320nMAssay Description:Displacement of APC-labeled biotinylated-avidin from Euphorium-chelated recombinant human N-terminal GST-tagged BRD4 bromodomain 1 expressed in Esche...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 33nMAssay 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
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  37nMAssay Description:Displacement of biotinylated acetylated peptide from recombinant human partial length BRD4 long isoform bromodomain 1/2 (N44 to E460 residues) expres...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 40nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD1) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 20nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-screen ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 40nMAssay Description:Inhibition of N-terminal His-tagged BRD4 (BD1/BD2) (unknown origin) using biotinylated tetra-acetylated histone H4 peptide after 30 mins by alpha-scr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 78nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 D...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 145nMAssay Description:Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 132nMAssay Description:Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  25nMAssay Description:Binding affinity to human partial length BRD2-BD2 (E348 to D455 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 93nMAssay Description:Displacement of FITC-JQ1 from His6-tagged BRD4 bromodomain-1 (unknown origin) expressed in Escherichia coli BL21(DE3) after 4 hrs by fluorescence ani...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 631nMAssay Description:Inhibition of BRD4 bromodomain-1 (unknown origin) by FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 32.5nMAssay Description:Displacement of tetra-acetylated H4 peptide from human Brd2 bromodomain BD12 after 1 hr by FRET analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 260nMAssay Description:Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in da...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 61nMAssay Description:Binding affinity to BRD4 BD1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 631nMAssay Description:Binding affinity to His6-tagged BRD4 (unknown origin) after 60 mins by fluorescence anisotropy binding AssayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 120nMAssay Description:Inhibition of His-FLAG-tagged BRD4 binding domain1 (unknown origin) binding to H4-TetraAc-biotin peptide after 20 mins by AlphaLISAMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 190nMAssay Description:Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 810nMAssay Description:Inhibition of His6-tagged BRD2 expressed in Escherichia coli after 60 mins by fluorescence anisotropy assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 590nMAssay Description:Inhibition of BRD4-BD1 (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
University of Modena and Reggio Emilia

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 32nMAssay Description:Inhibition of BRD2/3 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 30nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 126nMAssay Description:Inhibition of BRD4 BD1 (unknown origin) measured by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 126nMAssay Description:Inhibition of BRD4 BD2 (unknown origin) measured by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails
PubMed
TargetCytochrome P450 3A4(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of recombinant human CYP3A4 expressed in Escherichia coli using DEF as probe substrate incubated for 15 to 60 mins by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2C9(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of recombinant human CYP2C9 expressed in Escherichia coli using FCA as substrate incubated for 15 to 60 mins by fluorometric assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 631nMAssay Description:Inhibition of BRD4 in human whole blood assessed as reduction in LPS-induced IL-6 secretion preincubated for 30 mins followed by LPS stimulation and ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 316nMAssay Description:Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced IL-6 secretion incubated for 18 to 24 hrs by MSD assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 33nMAssay Description:Displacement of tetra-acetylated Histone H4 peptide from BRD4 (unknown origin) incubated for 1 hr by FRET analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  37nMAssay Description:Competitive binding affinity to human partial length BRD4 (BD1,2) (N44 to E460 residues) expressed in bacterial expression system by BROMOscan assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataIC50: 630nMAssay Description:Inhibition of BRD4 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 3(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  22nMAssay Description:Binding affinity to human partial length BRD3-BD1 (P24 to E144 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  110nMAssay Description:Binding affinity to human partial length BRD2-BD1 (K71 to N194 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHistone acetyltransferase p300(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  7.10E+4nMAssay Description:Binding affinity to human partial length EP300 (A1040 to G1161 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCREB-binding protein(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  8.30E+4nMAssay Description:Binding affinity to human partial length CREBBP (R1081 to G1197 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain testis-specific protein(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  60nMAssay Description:Binding affinity to human partial length BRDT-BD2 (K250 to E382 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain testis-specific protein(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  112nMAssay Description:Binding affinity to human partial length BRDT-BD1 (N21 to E137 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  19nMAssay Description:Binding affinity to human partial length BRD4-BD2 (K333 to E460 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  41nMAssay Description:Binding affinity to human partial length BRD4-BD1 (N44 to E168 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 3(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  23nMAssay Description:Binding affinity to human partial length BRD3-BD2 (G306 to P416 residues) expressed in bacterial expression system by BROMOscan methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  45nMAssay Description:Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 2(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  100nMAssay Description:Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  95nMAssay Description:Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  65nMAssay Description:Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetATPase family AAA domain-containing protein 2(Human)
University of Michigan

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to biotinylated ATAD2A (981 to 1108 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCREB-binding protein(Human)
Kyorin Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd: >1.00E+4nMAssay Description:Binding affinity to biotinylated CREBBP (1043 to 1159 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  48nMAssay Description:Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferomet...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBromodomain-containing protein 4(Human)
Celgene Quanticel Research

Curated by ChEMBL
LigandPNGBDBM50365463(CHEMBL1232461)
Affinity DataKd:  99nMAssay Description:Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometr...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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