General
Preferred name
CC-885
Synonyms
3 ()
1(CC-885) ()
CC-885 ()
P&D ID
PD057043
CAS
1010100-07-8
Tags
available
molecular glue
PROTAC
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Structural studies have shown that immunomodulatory drugs bind in a shallow hydrophobic pocket on the surface of cereblon, mediated by a glutarimide ring. The broad activity profile of CC-885 is highly differentiated from that of , and . The anti-tumour activity of CC-885 is mediated through the cereblon-dependent ubiquitination and degradation of the translation termination factor GSPT1. Patient-derived acute myeloid leukaemia tumour cells exhibit high sensitivity to CC-885, indicating the clinical potential of this mechanism .
DESCRIPTION Structural studies have shown that thalidomide class immunomodulatory drugs bind in a shallow hydrophobic pocket on the surface of cereblon, that is mediated by a glutarimide ring of the ligand. Binding of small molecules to cereblon can alter its substrate specificity . Thalidomide and its related drugs enhance recruitment of Ikaros and Aiolos to the E3 ubiquitin ligase complex. CC-885 has a different mechanism of action compared to , and . The anti-tumour activity of CC-885 is mediated through the cereblon-dependent ubiquitination and degradation of the translation termination factor GSPT1. Patient-derived acute myeloid leukaemia tumour cells exhibit high sensitivity to CC-885, indicating the clinical potential of this mechanism . (GtoPdb)
DESCRIPTION CC-885 is a cereblon modulator (EC50 = 0.0019nM) with antiproliferative effects. (Enamine Bioactive Compounds)
DESCRIPTION CC-885 is a modulator of cereblon (CRBN). It has potent anti-tumour activity. (TargetMol Bioactive Compound Library)
Cell lines
20
Organisms
0
Compound Sets
9
Axon Medchem Screening Library
Cayman Chemical Bioactives
Enamine Bioactive Compounds
Guide to Pharmacology
MedChem Express Bioactive Compound Library
MolGlueDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
13
Properties
(calculated by RDKit )
Molecular Weight
440.13
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
2
cLogP
2.73
TPSA
107.61
Fraction CSP3
0.27
Chiral centers
1.0
Largest ring
6.0
QED
0.64
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Cereblon
Ligand for E3 Ligase
E1/E2/E3 Enzyme
Cereblon (CRBN) modulator
Ligands for E3 Ligase
Molecular Glues
E3 Ligase
Pathway
Metabolic Enzyme/Protease
Source data