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Assay Detail

CHEMBL930492

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

Binding
Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Zhao S, Shen Y, van Oeveren A, Marschke KB, Zhi L.
Bioorg Med Chem Lett (2008) 18 : 3431 -3435
PubMed 18442912 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.43 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.70
CHEMBL253535 1 8.89
CHEMBL257751 1 8.52
CHEMBL427898 1 8.40
CHEMBL427731 1 8.30
CHEMBL450334 1 8.10
CHEMBL401711 1 8.06
CHEMBL256769 1 8.00
CHEMBL401629 1 7.96
CHEMBL256768 1 7.68
CHEMBL257151 1 7.58
CHEMBL402136 1 7.57
CHEMBL450933 1 7.55
CHEMBL403219 1 7.30
CHEMBL256947 1 7.23
CHEMBL256977 1 7.21
CHEMBL409 BICALUTAMIDE 4.0 1 6.82
CHEMBL253744 1 6.60
CHEMBL258397 1 6.21
CHEMBL258241 1 6.00
CHEMBL258190 1 5.89
CHEMBL258384 1 5.80
CHEMBL253746 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE Ki = 0.2 nM 9.70
CHEMBL253535 Ki = 1.3 nM 8.89
CHEMBL257751 Ki = 3.0 nM 8.52
CHEMBL427898 Ki = 4.0 nM 8.40
CHEMBL427731 Ki = 5.0 nM 8.30
CHEMBL450334 Ki = 8.0 nM 8.10
CHEMBL401711 Ki = 8.7 nM 8.06
CHEMBL256769 Ki = 10.0 nM 8.00
CHEMBL401629 Ki = 11.0 nM 7.96
CHEMBL256768 Ki = 21.0 nM 7.68
CHEMBL257151 Ki = 26.0 nM 7.58
CHEMBL402136 Ki = 27.0 nM 7.57
CHEMBL450933 Ki = 28.0 nM 7.55
CHEMBL403219 Ki = 50.0 nM 7.30
CHEMBL256947 Ki = 59.0 nM 7.23
CHEMBL256977 Ki = 62.0 nM 7.21
CHEMBL409 BICALUTAMIDE Ki = 151.0 nM 6.82
CHEMBL253744 Ki = 250.0 nM 6.60
CHEMBL258397 Ki = 610.0 nM 6.21
CHEMBL258241 Ki = 1000.0 nM 6.00
CHEMBL258190 Ki = 1300.0 nM 5.89
CHEMBL258384 Ki = 1593.0 nM 5.80
CHEMBL253746 Ki = 2346.0 nM 5.63