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Assay Detail

CHEMBL5501647

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at androgen receptor (unknown origin) transfected in HEK293T cells co-transfected with luciferase reporter gene assessed as inhibition of transcriptional activity incubated for 18 to 20 hrs by luminescence plate reader analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel selective agents for the degradation of AR/AR-V7 to treat advanced prostate cancer.
Yang Y, Lv G, Xiu R, Yang H, Wang W, Yu P, Zhang J, Ye L, Wang H, Tian J.
Eur J Med Chem (2024) 271 : 116400 -116400
PubMed 38626524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.94 7.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5559421 1 7.59
CHEMBL5517689 1 7.44
CHEMBL5558125 1 7.42
CHEMBL5518016 1 7.23
CHEMBL5437141 1 7.22
CHEMBL5505831 1 7.00
CHEMBL5542890 1 6.99
CHEMBL5542581 1 6.94
CHEMBL5517813 1 6.84
CHEMBL5559204 1 6.76
CHEMBL5557813 1 6.51
CHEMBL5531958 1 6.50
CHEMBL5557418 1 6.41
CHEMBL5531949 1 6.25
CHEMBL5532063 1 -
CHEMBL5558969 1 -
CHEMBL5523394 1 -
CHEMBL5555049 1 -
CHEMBL5512492 1 -
CHEMBL5557950 1 -
CHEMBL5555724 1 -
CHEMBL5532027 1 -
CHEMBL5527850 1 -
CHEMBL5559036 1 -
CHEMBL5559462 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5559421 IC50 = 25.89 nM 7.59
CHEMBL5517689 IC50 = 36.67 nM 7.44
CHEMBL5558125 IC50 = 37.65 nM 7.42
CHEMBL5518016 IC50 = 59.36 nM 7.23
CHEMBL5437141 IC50 = 60.79 nM 7.22
CHEMBL5505831 IC50 = 99.54 nM 7.00
CHEMBL5542890 IC50 = 101.37 nM 6.99
CHEMBL5542581 IC50 = 115.58 nM 6.94
CHEMBL5517813 IC50 = 145.98 nM 6.84
CHEMBL5559204 IC50 = 172.85 nM 6.76
CHEMBL5557813 IC50 = 311.27 nM 6.51
CHEMBL5531958 IC50 = 318.84 nM 6.50
CHEMBL5557418 IC50 = 393.98 nM 6.41
CHEMBL5531949 IC50 = 569.21 nM 6.25
CHEMBL5532063 IC50 > 10000.0 nM -
CHEMBL5558969 IC50 - -
CHEMBL5523394 IC50 - -
CHEMBL5555049 IC50 - -
CHEMBL5512492 IC50 - -
CHEMBL5557950 IC50 - -
CHEMBL5555724 IC50 > 10000.0 nM -
CHEMBL5532027 IC50 - -
CHEMBL5527850 IC50 - -
CHEMBL5559036 IC50 - -
CHEMBL5559462 IC50 - -