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Assay Detail

CHEMBL4844396

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

Functional
Growth inhibition of human LNCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type LNCaP
Confidence 1 — Organism
Curated By Autocuration

Target

LNCaP (CHEMBL612518)
Type CELL-LINE
Organism Homo sapiens

Publication

Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer.
Han X, Zhao L, Xiang W, Qin C, Miao B, McEachern D, Wang Y, Metwally H, Wang L, Matvekas A, Wen B, Sun D, Wang S.
J Med Chem (2021) 64 : 12831 -12854
PubMed 34431670 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.57 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4877348 1 8.30
CHEMBL4747369 1 8.00
CHEMBL4861919 1 7.96
CHEMBL4867584 1 7.89
CHEMBL4879244 1 7.85
CHEMBL4863542 1 7.09
CHEMBL1082407 ENZALUTAMIDE 4.0 1 6.88
CHEMBL4849514 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4877348 IC50 = 5.0 nM 8.30
CHEMBL4747369 IC50 = 10.0 nM 8.00
CHEMBL4861919 IC50 = 11.0 nM 7.96
CHEMBL4867584 IC50 = 13.0 nM 7.89
CHEMBL4879244 IC50 = 14.0 nM 7.85
CHEMBL4863542 IC50 = 81.0 nM 7.09
CHEMBL1082407 ENZALUTAMIDE IC50 = 133.0 nM 6.88
CHEMBL4849514 IC50 = 237.0 nM 6.62