PROTACpedia
Androgen receptor degraders overcome common resistance mechanisms developed during prostate cancer treatment. Neoplasia. 2020 Jan 10;22(2):111-119. PMID:31931431 DOI:10.1016/j.neo.2019.12.003
Target: AR Androgen receptor P10275 Homo sapiens
E3 ligase: VHL
E3 binder: VH Ligand 6
SMILES: show
Ligand Name: ARI-16
SMILES: show
Calculated Values
MW: 1,095.81
Hbond donors: 3
Hbond acceptors: 12
cLogP: 9.26
TPSA: 194.23

SMILES: show
Linker type: Alkane
Incubation time (hours): 6
Cells: LnCap
DC50: = 8.0 nM
Tested a non-binding E3 control?: No
Tested competition with ligand?: Yes
Tested proteaseome inhibitor?: Yes
Proteomics data available?: Yes
Tested engagement in cells?: No
Off-targets reported?: No
Contributed by: Paul Gehrtz
E3 ligase: VHL
E3 binder: VH Ligand 6
SMILES: show
Ligand Name: Apalutamide
SMILES: show
Calculated Values
MW: 1,115.32
Hbond donors: 2
Hbond acceptors: 13
cLogP: 8.46
TPSA: 192.34

SMILES: show
Linker type: Alkane
Incubation time (hours): 6
Cells: LnCap
Tested a non-binding E3 control?: No
Tested competition with ligand?: Yes
Tested proteaseome inhibitor?: Yes
Proteomics data available?: No
Tested engagement in cells?: No
Off-targets reported?: No
Contributed by: Paul Gehrtz
E3 ligase: VHL
E3 binder: VH Ligand 6
SMILES: show
Ligand Name: Enzalutamide
SMILES: show
Calculated Values
MW: 1,102.32
Hbond donors: 2
Hbond acceptors: 12
cLogP: 8.93
TPSA: 179.45

SMILES: show
Linker type: Alkane
Incubation time (hours): 6
Cells: LnCap
Tested a non-binding E3 control?: No
Tested competition with ligand?: Yes
Tested proteaseome inhibitor?: Yes
Proteomics data available?: No
Tested engagement in cells?: No
Off-targets reported?: No
Contributed by: Paul Gehrtz