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Assay Detail

CHEMBL4844615

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

Functional
Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability 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

Discovery of ARD-2585 as an Exceptionally Potent and Orally Active PROTAC Degrader of Androgen Receptor for the Treatment of Advanced Prostate Cancer.
Xiang W, Zhao L, Han X, Qin C, Miao B, McEachern D, Wang Y, Metwally H, Kirchhoff PD, Wang L, Matvekas A, He M, Wen B, Sun D, Wang S.
J Med Chem (2021) 64 : 13487 -13509
PubMed 34473519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.65 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862569 1 7.94
CHEMBL4849497 1 7.94
CHEMBL4849315 1 7.82
CHEMBL4870803 1 7.79
CHEMBL4872965 1 7.66
CHEMBL4854467 1 7.65
CHEMBL4862963 BAVDEGALUTAMIDE 1.0 1 7.48
CHEMBL1082407 ENZALUTAMIDE 4.0 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862569 IC50 = 11.4 nM 7.94
CHEMBL4849497 IC50 = 11.6 nM 7.94
CHEMBL4849315 IC50 = 15.3 nM 7.82
CHEMBL4870803 IC50 = 16.2 nM 7.79
CHEMBL4872965 IC50 = 21.7 nM 7.66
CHEMBL4854467 IC50 = 22.3 nM 7.65
CHEMBL4862963 BAVDEGALUTAMIDE IC50 = 33.1 nM 7.48
CHEMBL1082407 ENZALUTAMIDE IC50 = 133.0 nM 6.88