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Assay Detail

CHEMBL896729

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Functional
Agonist activity at androgen receptor in mouse C2C12 cells by receptor transactivation assay
18
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type C2C12
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL3056)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Manfredi MC, Bi Y, Nirschl AA, Sutton JC, Seethala R, Golla R, Beehler BC, Sleph PG, Grover GJ, Ostrowski J, Hamann LG.
Bioorg Med Chem Lett (2007) 17 : 4487 -4490
PubMed 17574413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 6.84 9.36
Intrinsic activity 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL229264 1 9.36
CHEMBL425646 1 8.64
CHEMBL1170 TESTOSTERONE PROPIONATE 4.0 1 8.55
CHEMBL393048 1 8.55
CHEMBL233773 1 7.92
CHEMBL391768 2 5.90
CHEMBL233774 2 5.53
CHEMBL391769 2 5.45
CHEMBL234187 1 5.13
CHEMBL234185 2 5.11
CHEMBL391770 2 5.05
CHEMBL234394 1 -
CHEMBL233977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL229264 EC50 = 0.44 nM 9.36
CHEMBL425646 EC50 = 2.3 nM 8.64
CHEMBL1170 TESTOSTERONE PROPIONATE EC50 = 2.8 nM 8.55
CHEMBL393048 EC50 = 2.8 nM 8.55
CHEMBL233773 EC50 = 11.9 nM 7.92
CHEMBL391768 EC50 = 1251.0 nM 5.90
CHEMBL233774 EC50 = 2959.0 nM 5.53
CHEMBL391769 EC50 = 3517.0 nM 5.45
CHEMBL234187 EC50 = 7459.0 nM 5.13
CHEMBL234185 EC50 = 7729.0 nM 5.11
CHEMBL391770 EC50 = 8962.0 nM 5.05
CHEMBL234185 Intrinsic activity <= 50.0 % -
CHEMBL391770 Intrinsic activity <= 50.0 % -
CHEMBL391769 Intrinsic activity <= 50.0 % -
CHEMBL391768 Intrinsic activity <= 50.0 % -
CHEMBL233774 Intrinsic activity <= 50.0 % -
CHEMBL233977 EC50 - -
CHEMBL234394 EC50 > 3000.0 nM -