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Assay Detail

CHEMBL3371979

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

Binding
Agonist activity at human androgen receptor expressed in mouse C2C12 cells by androgen-specific response element-driven luciferase reporter gene assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type C2C12
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-alkoxy-pyrrolo[1,2-b]pyrazolines as selective androgen receptor modulators with ideal physicochemical properties for transdermal administration.
Ullrich T, Sasmal S, Boorgu V, Pasagadi S, Cheera S, Rajagopalan S, Bhumireddy A, Shashikumar D, Chelur S, Belliappa C, Pandit C, Krishnamurthy N, Mukherjee S, Ramanathan A, Ghadiyaram C, Ramachandra M, Santos PG, Lagu B, Bock MG, Perrone MH, Weiler S, Keller H.
J Med Chem (2014) 57 : 7396 -7411
PubMed 25121964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 8.69 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27769 STANOLONE 2.0 1 9.89
CHEMBL3326461 1 9.80
CHEMBL3326466 1 9.52
CHEMBL3326458 1 9.40
CHEMBL3326454 1 9.30
CHEMBL3326457 1 9.03
CHEMBL3326455 1 9.00
CHEMBL3326464 1 8.85
CHEMBL3326460 1 8.82
CHEMBL3326456 1 8.35
CHEMBL3326459 1 8.15
CHEMBL3326462 1 8.01
CHEMBL3326465 1 7.58
CHEMBL3326453 1 6.01
CHEMBL3326463 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27769 STANOLONE EC50 = 0.13 nM 9.89
CHEMBL3326461 EC50 = 0.16 nM 9.80
CHEMBL3326466 EC50 = 0.3 nM 9.52
CHEMBL3326458 EC50 = 0.4 nM 9.40
CHEMBL3326454 EC50 = 0.5 nM 9.30
CHEMBL3326457 EC50 = 0.93 nM 9.03
CHEMBL3326455 EC50 = 1.0 nM 9.00
CHEMBL3326464 EC50 = 1.4 nM 8.85
CHEMBL3326460 EC50 = 1.5 nM 8.82
CHEMBL3326456 EC50 = 4.5 nM 8.35
CHEMBL3326459 EC50 = 7.1 nM 8.15
CHEMBL3326462 EC50 = 9.7 nM 8.01
CHEMBL3326465 EC50 = 26.0 nM 7.58
CHEMBL3326453 EC50 = 978.0 nM 6.01
CHEMBL3326463 EC50 - -