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Assay Detail

CHEMBL4828552

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

Binding
Antagonist activity at androgen receptor in human LNCaP cells harboring eGFP/ARRIPB incubated for 3 days by fluorescence method
ChEMBL ↗
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Androgen receptor (CHEMBL1871) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of 2-(5,6,7-Trifluoro-1<i>H</i>-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer.
Leblanc E, Ban F, Cavga AD, Lawn S, Huang CF, Mohan S, Chang MEK, Flory MR, Ghaidi F, Lingadahalli S, Chen G, Yu IPL, Morin H, Lallous N, Gleave ME, Mohammed H, Young RN, Rennie PS, Lack NA, Cherkasov A.
J Med Chem (2021) 64 : 14968 -14982
PubMed 34661404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.61 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4845915 — — 1 7.52
CHEMBL4856070 — — 1 7.52
CHEMBL4849023 — — 1 7.40
CHEMBL4870389 — — 1 7.22
CHEMBL4872533 — — 1 7.16
CHEMBL4847082 — — 1 7.16
CHEMBL1082407 ENZALUTAMIDE 4.0 1 7.12
CHEMBL4852876 — — 1 7.05
CHEMBL4857183 — — 1 7.00
CHEMBL4870138 — — 1 7.00
CHEMBL4875734 — — 1 7.00
CHEMBL4876258 — — 1 6.96
CHEMBL4852991 — — 1 6.89
CHEMBL4871740 — — 1 6.80
CHEMBL4852542 — — 1 6.77
CHEMBL4849002 — — 1 6.75
CHEMBL4869391 — — 1 6.75
CHEMBL4866292 — — 1 6.72
CHEMBL4850974 — — 1 6.72
CHEMBL4856585 — — 1 6.70
CHEMBL4868944 — — 1 6.64
CHEMBL4877104 — — 1 6.64
CHEMBL4868764 — — 1 6.62
CHEMBL4864867 — — 1 6.52
CHEMBL4875909 — — 1 6.30
CHEMBL4871449 — — 1 6.26
CHEMBL4848581 — — 1 6.18
CHEMBL4854145 — — 1 6.13
CHEMBL4876467 — — 1 5.82
CHEMBL4877237 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4845915 — IC50 = 30.0 nM 7.52
CHEMBL4856070 — IC50 = 30.0 nM 7.52
CHEMBL4849023 — IC50 = 40.0 nM 7.40
CHEMBL4870389 — IC50 = 60.0 nM 7.22
CHEMBL4872533 — IC50 = 70.0 nM 7.16
CHEMBL4847082 — IC50 = 70.0 nM 7.16
CHEMBL1082407 ENZALUTAMIDE IC50 = 75.0 nM 7.12
CHEMBL4852876 — IC50 = 90.0 nM 7.05
CHEMBL4857183 — IC50 = 100.0 nM 7.00
CHEMBL4870138 — IC50 = 100.0 nM 7.00
CHEMBL4875734 — IC50 = 100.0 nM 7.00
CHEMBL4876258 — IC50 = 110.0 nM 6.96
CHEMBL4852991 — IC50 = 130.0 nM 6.89
CHEMBL4871740 — IC50 = 160.0 nM 6.80
CHEMBL4852542 — IC50 = 170.0 nM 6.77
CHEMBL4849002 — IC50 = 180.0 nM 6.75
CHEMBL4869391 — IC50 = 180.0 nM 6.75
CHEMBL4850974 — IC50 = 190.0 nM 6.72
CHEMBL4866292 — IC50 = 190.0 nM 6.72
CHEMBL4856585 — IC50 = 200.0 nM 6.70
CHEMBL4868944 — IC50 = 230.0 nM 6.64
CHEMBL4877104 — IC50 = 230.0 nM 6.64
CHEMBL4868764 — IC50 = 240.0 nM 6.62
CHEMBL4864867 — IC50 = 300.0 nM 6.52
CHEMBL4875909 — IC50 = 500.0 nM 6.30
CHEMBL4871449 — IC50 = 550.0 nM 6.26
CHEMBL4848581 — IC50 = 660.0 nM 6.18
CHEMBL4854145 — IC50 = 740.0 nM 6.13
CHEMBL4876467 — IC50 = 1500.0 nM 5.82
CHEMBL4877237 — IC50 = 1590.0 nM 5.80
CHEMBL4852702 — IC50 = 1650.0 nM 5.78
CHEMBL4860114 — IC50 = 1900.0 nM 5.72
CHEMBL4846981 — IC50 = 2170.0 nM 5.66
CHEMBL4870661 — IC50 = 32000.0 nM 4.50
CHEMBL4874089 — IC50 - — -
CHEMBL4847627 — IC50 - — -