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Assay Detail

CHEMBL884023

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

Functional
Antagonistic activity (IC50) against human androgen receptor (hAR) in co-transfected CV-1 cell
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CV-1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2(1H)-pyrrolidino[3,2-g] quinolinone.
Edwards JP, West SJ, Pooley CL, Marschke KB, Farmer LJ, Jones TK.
Bioorg Med Chem Lett (1998) 8 : 745 -750
PubMed 9871534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.25 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351465 1 8.15
CHEMBL351022 1 8.00
CHEMBL351519 1 7.66
CHEMBL166323 1 7.64
CHEMBL162368 1 7.58
CHEMBL163142 1 7.57
CHEMBL165912 1 7.57
CHEMBL161892 1 7.44
CHEMBL165219 1 7.32
CHEMBL165803 1 7.32
CHEMBL423620 1 7.29
CHEMBL163143 1 7.28
CHEMBL161980 1 7.27
CHEMBL162503 1 7.25
CHEMBL349631 1 7.25
CHEMBL409 BICALUTAMIDE 4.0 1 6.80
CHEMBL162103 1 6.71
CHEMBL352456 1 6.64
CHEMBL348918 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351465 IC50 = 7.0 nM 8.15
CHEMBL351022 IC50 = 10.0 nM 8.00
CHEMBL351519 IC50 = 22.0 nM 7.66
CHEMBL166323 IC50 = 23.0 nM 7.64
CHEMBL162368 IC50 = 26.0 nM 7.58
CHEMBL163142 IC50 = 27.0 nM 7.57
CHEMBL165912 IC50 = 27.0 nM 7.57
CHEMBL161892 IC50 = 36.0 nM 7.44
CHEMBL165219 IC50 = 48.0 nM 7.32
CHEMBL165803 IC50 = 48.0 nM 7.32
CHEMBL423620 IC50 = 51.0 nM 7.29
CHEMBL163143 IC50 = 53.0 nM 7.28
CHEMBL161980 IC50 = 54.0 nM 7.27
CHEMBL162503 IC50 = 56.0 nM 7.25
CHEMBL349631 IC50 = 56.0 nM 7.25
CHEMBL409 BICALUTAMIDE IC50 = 157.0 nM 6.80
CHEMBL162103 IC50 = 197.0 nM 6.71
CHEMBL352456 IC50 = 230.0 nM 6.64
CHEMBL348918 IC50 = 9182.0 nM 5.04