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Assay Detail

CHEMBL1002998

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

Functional
Inhibition of KCl-induced tonic contraction in Beagle dog detrusor muscle strips preincubated for 15 mins before KCl challenge
21
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
EC50 21 8.28 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471060 1 8.92
CHEMBL452134 1 8.90
CHEMBL515397 2 8.90
CHEMBL492401 1 8.90
CHEMBL469821 1 8.59
CHEMBL473702 1 8.44
CHEMBL446806 2 8.40
CHEMBL488224 2 8.30
CHEMBL271945 1 8.17
CHEMBL491726 1 8.10
CHEMBL470292 1 8.10
CHEMBL270026 1 8.06
CHEMBL271574 1 7.96
CHEMBL470856 1 7.94
CHEMBL469395 2 7.90
CHEMBL445481 1 7.21
CHEMBL469396 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471060 EC50 = 1.2 nM 8.92
CHEMBL452134 EC50 = 1.259 nM 8.90
CHEMBL492401 EC50 = 1.259 nM 8.90
CHEMBL515397 EC50 = 1.259 nM 8.90
CHEMBL469821 EC50 = 2.6 nM 8.59
CHEMBL473702 EC50 = 3.6 nM 8.44
CHEMBL446806 EC50 = 3.981 nM 8.40
CHEMBL446806 EC50 = 4.4 nM 8.36
CHEMBL488224 EC50 = 5.012 nM 8.30
CHEMBL271945 EC50 = 6.8 nM 8.17
CHEMBL491726 EC50 = 7.943 nM 8.10
CHEMBL470292 EC50 = 7.943 nM 8.10
CHEMBL270026 EC50 = 8.7 nM 8.06
CHEMBL271574 EC50 = 11.0 nM 7.96
CHEMBL470856 EC50 = 11.4 nM 7.94
CHEMBL469395 EC50 = 12.59 nM 7.90
CHEMBL488224 EC50 = 14.1 nM 7.85
CHEMBL445481 EC50 = 62.0 nM 7.21
CHEMBL469396 EC50 - -
CHEMBL469395 EC50 > 50.0 nM -
CHEMBL515397 EC50 - -