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Assay Detail

CHEMBL1121349

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

Functional
Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Structure-activity relationships of bioisosteric replacement of the carboxylic acid in novel androgen receptor pure antagonists.
Yoshino H, Sato H, Tachibana K, Shiraishi T, Nakamura M, Ohta M, Ishikura N, Nagamuta M, Onuma E, Nakagawa T, Arai S, Ahn KH, Jung KY, Kawata H.
Bioorg Med Chem (2010) 18 : 3159 -3168
PubMed 20381361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.11 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1099086 1 7.92
CHEMBL1095862 1 7.75
CHEMBL1095863 1 7.52
CHEMBL1098173 1 7.29
CHEMBL1099142 1 7.26
CHEMBL1097855 1 7.10
CHEMBL1095224 1 7.05
CHEMBL1098171 1 6.96
CHEMBL1095223 1 6.70
CHEMBL1099141 1 6.40
CHEMBL409 BICALUTAMIDE 4.0 1 6.26
CHEMBL1094117 1 -
CHEMBL1099087 1 -
CHEMBL1098174 1 -
CHEMBL1098172 1 -
CHEMBL1095864 1 -
CHEMBL1095861 1 -
CHEMBL1099158 1 -
CHEMBL1099140 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1099086 IC50 = 12.0 nM 7.92
CHEMBL1095862 IC50 = 18.0 nM 7.75
CHEMBL1095863 IC50 = 30.0 nM 7.52
CHEMBL1098173 IC50 = 51.0 nM 7.29
CHEMBL1099142 IC50 = 55.0 nM 7.26
CHEMBL1097855 IC50 = 79.0 nM 7.10
CHEMBL1095224 IC50 = 89.0 nM 7.05
CHEMBL1098171 IC50 = 110.0 nM 6.96
CHEMBL1095223 IC50 = 200.0 nM 6.70
CHEMBL1099141 IC50 = 400.0 nM 6.40
CHEMBL409 BICALUTAMIDE IC50 = 550.0 nM 6.26
CHEMBL1094117 IC50 - -
CHEMBL1099087 IC50 - -
CHEMBL1098174 IC50 - -
CHEMBL1098172 IC50 - -
CHEMBL1095864 IC50 - -
CHEMBL1095861 IC50 - -
CHEMBL1099158 IC50 - -
CHEMBL1099140 IC50 - -