- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: CBP30 targets the CBP/p300 bromodomain, with much improved selectivity compared to the pan-BET bromodomain inhibitor (+)-JQ1 . CBP30 has therapeutic potential against autoimmune diseases characterised by aberrant Th17 responses.
This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection.
The compound also has antimalarial activity. The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|Guide to Malaria Pharmacology Comments|
|Although SGC-CBP30 demonstrates low potency against P. falciparum, the compound is ~7-fold more selective for the parasite and could provide a starting point for the design of more potent analogues .
Potential Target/Mechanism Of Action: In silico docking studies predict that SGC-CBP30 participates in a typical hydrogen bond interaction with the conserved asparagine (Asn1436) of the P. falciparum histone acetyltransferase GCN5 (PfGCN5) bromodomain .