Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity. Nat Commun. 2020 Apr 24;11(1):1996. PMID:32332723 DOI:10.1038/s41467-020-15838-0
Target: BCL2L1 Bcl-2-like protein 1 Q07817 Homo sapiens
E3 ligase: Cereblon
E3 binder: Pomalidomide
SMILES: show

Ligand Name: ABT-263
Ligand PDB Id: 1XJ
PDB with Ligand: 6QGH
SMILES: show

Calculated Values
MW: 1,484.16
Hbond donors: 4
Hbond acceptors: 21
cLogP: 8.76
TPSA: 284.19

SMILES: show

Linker type: Other
Incubation time (hours): 16
Cells: WI38 platelets
DC50: = 46 nM
Dmax: = 96.2 %
Tested a non-binding E3 control?: Yes
Tested competition with ligand?: Yes
Tested proteaseome inhibitor?: Yes
Proteomics data available?: No
Tested engagement in cells?: No
Contributed by: Barr Tivon