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Assay Detail

CHEMBL1007111

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

Functional
Inhibition of carbachol-induced increase in intravesical pressure in intraduodenally dosed Beagle dog OAB model for 30 mins measured for 180 mins
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Confidence 1 — Organism
Curated By Autocuration

Target

Canis familiaris (CHEMBL373)
Type ORGANISM
Organism Canis lupus familiaris

Publication

Discovery of highly potent and selective biphenylacylsulfonamide-based beta3-adrenergic receptor agonists and evaluation of physical properties as potential overactive bladder therapies: part 5.
Hattori K, Toda S, Imanishi M, Itou S, Nakajima Y, Washizuka K, Araki T, Hamashima H, Tomishima Y, Sakurai M, Matsui S, Imamura E, Ueshima K, Yamamoto T, Yamamoto N, Ishikawa H, Nakano K, Unami N, Hamada K, Matsumura Y, Takamura F.
J Med Chem (2009) 52 : 3063 -3072
PubMed 19366244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
ED50 13 - -
EC50 13 8.11 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446806 2 8.92
CHEMBL473702 2 8.74
CHEMBL488224 2 8.40
CHEMBL471060 2 8.15
CHEMBL470856 2 8.09
CHEMBL271574 2 7.95
CHEMBL469821 2 7.85
CHEMBL270026 2 7.73
CHEMBL271945 2 7.70
CHEMBL445481 2 7.58
CHEMBL515397 2 -
CHEMBL469395 2 -
CHEMBL469396 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446806 EC50 = 1.2 nM 8.92
CHEMBL473702 EC50 = 1.8 nM 8.74
CHEMBL488224 EC50 = 4.0 nM 8.40
CHEMBL471060 EC50 = 7.1 nM 8.15
CHEMBL470856 EC50 = 8.2 nM 8.09
CHEMBL271574 EC50 = 11.2 nM 7.95
CHEMBL469821 EC50 = 14.2 nM 7.85
CHEMBL270026 EC50 = 18.7 nM 7.73
CHEMBL271945 EC50 = 20.0 nM 7.70
CHEMBL445481 EC50 = 26.5 nM 7.58
CHEMBL515397 ED50 - -
CHEMBL515397 EC50 - -
CHEMBL469395 ED50 - -
CHEMBL469395 EC50 - -
CHEMBL469396 ED50 - -
CHEMBL469396 EC50 - -
CHEMBL471060 ED50 = 0.0349 mg.kg-1 -
CHEMBL473702 ED50 = 0.0161 mg.kg-1 -
CHEMBL469821 ED50 = 0.0247 mg.kg-1 -
CHEMBL271574 ED50 = 0.047 mg.kg-1 -
CHEMBL470856 ED50 = 0.0145 mg.kg-1 -
CHEMBL270026 ED50 = 0.0459 mg.kg-1 -
CHEMBL445481 ED50 = 0.0162 mg.kg-1 -
CHEMBL446806 ED50 = 0.0143 mg.kg-1 -
CHEMBL271945 ED50 = 0.0259 mg.kg-1 -
CHEMBL488224 ED50 = 0.065 mg.kg-1 -