BDBM50200445 CHEMBL3897393::US9763922, Example 300

SMILES CC(=O)N1CCc2c(c(nn2[C@H]3CCOC3)Nc4ccc(cc4F)c5cnn(c5)C)C1

InChI Key InChIKey=NKOJNOBJGYTLLZ-UHFFFAOYSA-N

Data  5 IC50  2 EC50

PDB links: 2 PDB IDs match this monomer.

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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 50200445   

LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataEC50:  1.90E+3nMAssay Description:Inhibition of CBP/EP300 in human MV4-11 cells assessed as inhibition of MYC expression measured after 4 hrs by luminescence analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/26/2018
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCREB-binding protein(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataIC50: 22nMAssay Description:His/Flag epitope tagged CBP was cloned, expressed, and purified to homogeneity. CBP binding and inhibition was assessed by monitoring the engagement ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/30/2019
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataIC50: 5.49E+3nMAssay Description:His/Flag epitope tagged BRD4 BD142-168 was cloned, expressed, and purified to. BRD4 binding and inhibition was assessed by monitoring the engagement ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/30/2019
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetCREB-binding protein(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataIC50: 410nMAssay Description:Inhibition of Halo-tagged histone H3.3 binding to NanoLuc luciferase conjugated human CBP expressed in HEK293 cells after overnight incubation by BRE...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCREB-binding protein(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataIC50: 20nMAssay Description:Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged CBP measured after 10 mins by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCREB-binding protein(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataEC50:  910nMAssay Description:Inhibition of CBP in human MV-4-11 cells assessed as decrease in MYC expression incubated for 4 hrs measured by luminescence methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetBromodomain-containing protein 4(Human)
Genentech

US Patent
LigandPNGBDBM50200445(CHEMBL3897393 | US9763922, Example 300)
Affinity DataIC50: 1.30E+4nMAssay Description:Displacement of biotinylated histone H3K14 peptide ligand from human recombinant His-tagged BRD4 bromodomain-1 measured after 10 mins by TR-FRET assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)