BDBM50467836 CHEMBL4282264

SMILES C[C@@H](C(F)(F)F)N(Cc1ccc(cc1)F)C(=O)CN2C(=O)[C@]3(CCc4c3ccc(c4)NC(=O)NC)OC2=O

InChI Key InChIKey=VRVJKILQRBSEAG-UHFFFAOYSA-N

Data  8 IC50  2 Kd

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 10 hits for monomerid = 50467836   

TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 60nMAssay Description:Inhibition of human P300 bromodomain HAT-C/H3 domain using histone as substrate in presence of acetyl-CoA by TR-FRET analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 60nMAssay Description:Inhibition of recombinant human N-terminal 6His-FLAG-tagged p300 BHC domain (1036 to 1822 residues) expressed in baculovirus infected Sf9 insect cell...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 67nMAssay Description:Inhibition of p300 (unknown origin) using histone H3 (1 to 21 residues) as substrate preincubated for 15 mins followed by substrate and [3H]acetyl-Co...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 60nMAssay Description:Inhibition of p300 HAT domain (unknown origin) using Biotin-C6-GRGKGGKGLGKGGAK as substrate pretreated with enzyme for 30 mins followed by incubation...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/20/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 60nMAssay Description:Inhibition of p300 HAT domain (unknown origin) preincubated for 30 mins followed by histone H4 Peptide (Biotin-C6-GRGKGGKGLGKGGAK) and acetyl coenzym...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataKd:  0.00128nMAssay Description:Binding affinity to human Biotin-Avi-P300 assessed as dissociation constant using Neutravidin as ligand measured by Surface Plasmon Resonance methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataKd:  1.40nMAssay Description:Binding affinity to human Biotin-Avi-P300 using Neutravidin as ligand measured by Surface Plasmon Resonance methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/29/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 15nMAssay Description:Inhibition of p300 (unknown origin) preincubated for 15 mins followed by addition of substrate [3H] Ac-CoA and measured after 60 mins by liquid scint...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCREB-binding protein(Human)
China Pharmaceutical University

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 61nMAssay Description:Inhibition of CBP (unknown origin) preincubated for 15 mins followed by addition of substrate [3H] Ac-CoA and measured after 60 mins by liquid scinti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/5/2023
Entry Details Article
PubMed
TargetHistone acetyltransferase p300(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM50467836(CHEMBL4282264)
Affinity DataIC50: 60nMAssay Description:Inhibition of human recombinant p300 HAT domain using histone H4 peptide and acetyl-coA as substrates preincubated for 30 mins followed by substrate ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/21/2023
Entry Details
PubMedPDB3D3D Structure (crystal)