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Assay Detail

CHEMBL1021864

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 180 mins
16
Total Activities
8
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 a novel series of biphenyl benzoic acid derivatives as highly potent and selective human beta3 adrenergic receptor agonists with good oral bioavailability. Part II.
Imanishi M, Itou S, Washizuka K, Hamashima H, Nakajima Y, Araki T, 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, Hattori K.
J Med Chem (2008) 51 : 4002 -4020
PubMed 18553954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
ED50 8 - -
EC50 8 8.20 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507506 2 9.55
CHEMBL487682 2 8.74
CHEMBL486051 2 8.60
CHEMBL488224 2 8.40
CHEMBL470292 2 8.11
CHEMBL453047 2 8.02
CHEMBL271945 2 7.70
CHEMBL59765 2 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507506 EC50 = 0.28 nM 9.55
CHEMBL487682 EC50 = 1.8 nM 8.74
CHEMBL486051 EC50 = 2.5 nM 8.60
CHEMBL488224 EC50 = 4.0 nM 8.40
CHEMBL470292 EC50 = 7.8 nM 8.11
CHEMBL453047 EC50 = 9.5 nM 8.02
CHEMBL271945 EC50 = 20.0 nM 7.70
CHEMBL59765 EC50 = 352.0 nM 6.45
CHEMBL507506 ED50 = 0.0048 mg.kg-1 -
CHEMBL271945 ED50 = 0.0259 mg.kg-1 -
CHEMBL453047 ED50 = 0.02 mg.kg-1 -
CHEMBL486051 ED50 = 0.0035 mg.kg-1 -
CHEMBL487682 ED50 = 0.0161 mg.kg-1 -
CHEMBL488224 ED50 = 0.065 mg.kg-1 -
CHEMBL470292 ED50 = 0.0284 mg.kg-1 -
CHEMBL59765 ED50 = 0.27 mg.kg-1 -