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Assay Detail

CHEMBL648595

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Functional
Agonistic activity (EC50) against human androgen receptor (hAR) in co-transfected CV-1 cell
15
Total Activities
15
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
EC50 15 7.29 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL162569 1 8.30
CHEMBL350932 1 8.30
CHEMBL163425 1 8.00
CHEMBL348918 1 7.82
CHEMBL163366 1 7.70
CHEMBL351447 1 7.60
CHEMBL422196 1 7.48
CHEMBL351022 1 7.38
CHEMBL349229 1 7.21
CHEMBL166212 1 7.19
CHEMBL165219 1 7.00
CHEMBL351465 1 6.78
CHEMBL165912 1 6.49
CHEMBL351519 1 6.42
CHEMBL166323 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL162569 EC50 = 5.0 nM 8.30
CHEMBL350932 EC50 = 5.0 nM 8.30
CHEMBL163425 EC50 = 10.0 nM 8.00
CHEMBL348918 EC50 = 15.0 nM 7.82
CHEMBL163366 EC50 = 20.0 nM 7.70
CHEMBL351447 EC50 = 25.0 nM 7.60
CHEMBL422196 EC50 = 33.0 nM 7.48
CHEMBL351022 EC50 = 42.0 nM 7.38
CHEMBL349229 EC50 = 62.0 nM 7.21
CHEMBL166212 EC50 = 64.0 nM 7.19
CHEMBL165219 EC50 = 99.0 nM 7.00
CHEMBL351465 EC50 = 168.0 nM 6.78
CHEMBL165912 EC50 = 324.0 nM 6.49
CHEMBL351519 EC50 = 380.0 nM 6.42
CHEMBL166323 EC50 = 1897.0 nM 5.72