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Assay Detail

CHEMBL4477893

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Functional
Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay
12
Total Activities
6
Compounds Tested
2
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

Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer.
Bassetto M, Ferla S, Pertusati F, Kandil S, Westwell AD, Brancale A, McGuigan C.
Eur J Med Chem (2016) 118 : 230 -243
PubMed 27131065 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.20 6.08
IC70 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4572299 2 6.08
CHEMBL4577418 2 5.79
CHEMBL4555717 2 5.48
CHEMBL409 BICALUTAMIDE 4.0 2 4.33
CHEMBL63560 (R)-BICALUTAMIDE 2 4.33
CHEMBL4513407 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4572299 IC50 = 828.0 nM 6.08
CHEMBL4577418 IC50 = 1638.0 nM 5.79
CHEMBL4555717 IC50 = 3278.0 nM 5.48
CHEMBL409 BICALUTAMIDE IC50 = 47266.0 nM 4.33
CHEMBL63560 (R)-BICALUTAMIDE IC50 = 47002.0 nM 4.33
CHEMBL4572299 IC70 = 1.326 uM -
CHEMBL4555717 IC70 = 3.547 uM -
CHEMBL409 BICALUTAMIDE IC70 = 60.92 uM -
CHEMBL4513407 IC50 > 100000.0 nM -
CHEMBL4513407 IC70 > 100.0 uM -
CHEMBL63560 (R)-BICALUTAMIDE IC70 = 59.32 uM -
CHEMBL4577418 IC70 = 7.887 uM -