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Assay Detail

CHEMBL935527

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

Functional
Agonist activity at human androgen receptor in CV1 cells by transcriptional activation assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Long YO, Higuchi RI, Caferro TR, Lau TL, Wu M, Cummings ML, Martinborough EA, Marschke KB, Chang WY, López FJ, Karanewsky DS, Zhi L.
Bioorg Med Chem Lett (2008) 18 : 2967 -2971
PubMed 18400499 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 8.04 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224263 1 8.96
CHEMBL256326 1 8.89
CHEMBL402039 1 8.70
CHEMBL401805 1 8.70
CHEMBL257396 1 8.49
CHEMBL429311 1 8.42
CHEMBL255655 1 8.38
CHEMBL402835 1 8.28
CHEMBL27769 STANOLONE 2.0 1 8.24
CHEMBL256330 1 8.23
CHEMBL436644 1 8.18
CHEMBL404512 1 7.96
CHEMBL257379 1 7.72
CHEMBL256284 1 7.64
CHEMBL404483 1 7.64
CHEMBL255918 1 7.55
CHEMBL256126 1 7.52
CHEMBL254798 1 7.46
CHEMBL256544 1 7.44
CHEMBL257988 1 7.38
CHEMBL404568 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224263 EC50 = 1.1 nM 8.96
CHEMBL256326 EC50 = 1.3 nM 8.89
CHEMBL402039 EC50 = 2.0 nM 8.70
CHEMBL401805 EC50 = 2.0 nM 8.70
CHEMBL257396 EC50 = 3.2 nM 8.49
CHEMBL429311 EC50 = 3.8 nM 8.42
CHEMBL255655 EC50 = 4.2 nM 8.38
CHEMBL402835 EC50 = 5.3 nM 8.28
CHEMBL27769 STANOLONE EC50 = 5.7 nM 8.24
CHEMBL256330 EC50 = 5.9 nM 8.23
CHEMBL436644 EC50 = 6.6 nM 8.18
CHEMBL404512 EC50 = 11.0 nM 7.96
CHEMBL257379 EC50 = 19.0 nM 7.72
CHEMBL256284 EC50 = 23.0 nM 7.64
CHEMBL404483 EC50 = 23.0 nM 7.64
CHEMBL255918 EC50 = 28.0 nM 7.55
CHEMBL256126 EC50 = 30.0 nM 7.52
CHEMBL254798 EC50 = 35.0 nM 7.46
CHEMBL256544 EC50 = 36.0 nM 7.44
CHEMBL257988 EC50 = 42.0 nM 7.38
CHEMBL404568 EC50 = 77.0 nM 7.11