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Assay Detail

CHEMBL1007087

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Functional
Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL ↗
53
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-3 adrenergic receptor (CHEMBL246) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 53 9.41 10.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446806 — — 2 10.54
CHEMBL470857 — — 1 10.46
CHEMBL452696 — — 1 10.21
CHEMBL452134 — — 2 10.20
CHEMBL473702 — — 1 10.18
CHEMBL490733 — — 1 10.10
CHEMBL491726 — — 2 9.90
CHEMBL469395 — — 2 9.90
CHEMBL445481 — — 1 9.89
CHEMBL455773 — — 1 9.85
CHEMBL491891 — — 1 9.72
CHEMBL473495 — — 1 9.72
CHEMBL479530 — — 1 9.70
CHEMBL492401 — — 2 9.70
CHEMBL488224 — — 2 9.60
CHEMBL521406 — — 1 9.59
CHEMBL479727 — — 1 9.54
CHEMBL270964 — — 1 9.54
CHEMBL409718 — — 1 9.52
CHEMBL516209 — — 1 9.49
CHEMBL470856 — — 1 9.49
CHEMBL472293 — — 1 9.48
CHEMBL273006 — — 1 9.47
CHEMBL479341 — — 1 9.42
CHEMBL511968 — — 1 9.39
CHEMBL469821 — — 1 9.34
CHEMBL256418 — — 1 9.34
CHEMBL479342 — — 1 9.30
CHEMBL513419 — — 1 9.27
CHEMBL271574 — — 1 9.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446806 — EC50 = 0.029 nM 10.54
CHEMBL446806 — EC50 = 0.03162 nM 10.50
CHEMBL470857 — EC50 = 0.035 nM 10.46
CHEMBL452696 — EC50 = 0.062 nM 10.21
CHEMBL452134 — EC50 = 0.0631 nM 10.20
CHEMBL473702 — EC50 = 0.066 nM 10.18
CHEMBL490733 — EC50 = 0.08 nM 10.10
CHEMBL469395 — EC50 = 0.1259 nM 9.90
CHEMBL491726 — EC50 = 0.1259 nM 9.90
CHEMBL445481 — EC50 = 0.13 nM 9.89
CHEMBL491726 — EC50 = 0.14 nM 9.85
CHEMBL455773 — EC50 = 0.14 nM 9.85
CHEMBL473495 — EC50 = 0.19 nM 9.72
CHEMBL491891 — EC50 = 0.19 nM 9.72
CHEMBL479530 — EC50 = 0.2 nM 9.70
CHEMBL492401 — EC50 = 0.1995 nM 9.70
CHEMBL488224 — EC50 = 0.2512 nM 9.60
CHEMBL521406 — EC50 = 0.26 nM 9.59
CHEMBL488224 — EC50 = 0.26 nM 9.59
CHEMBL270964 — EC50 = 0.29 nM 9.54
CHEMBL479727 — EC50 = 0.29 nM 9.54
CHEMBL409718 — EC50 = 0.3 nM 9.52
CHEMBL516209 — EC50 = 0.32 nM 9.49
CHEMBL470856 — EC50 = 0.32 nM 9.49
CHEMBL472293 — EC50 = 0.33 nM 9.48
CHEMBL273006 — EC50 = 0.34 nM 9.47
CHEMBL479341 — EC50 = 0.38 nM 9.42
CHEMBL511968 — EC50 = 0.41 nM 9.39
CHEMBL469395 — EC50 = 0.43 nM 9.37
CHEMBL469821 — EC50 = 0.46 nM 9.34
CHEMBL256418 — EC50 = 0.46 nM 9.34
CHEMBL479342 — EC50 = 0.5 nM 9.30
CHEMBL452134 — EC50 = 0.5 nM 9.30
CHEMBL513419 — EC50 = 0.54 nM 9.27
CHEMBL271574 — EC50 = 0.56 nM 9.25
CHEMBL270026 — EC50 = 0.6 nM 9.22
CHEMBL471060 — EC50 = 0.6 nM 9.22
CHEMBL469396 — EC50 = 0.6 nM 9.22
CHEMBL472090 — EC50 = 0.62 nM 9.21
CHEMBL515397 — EC50 = 0.631 nM 9.20
CHEMBL523149 — EC50 = 0.68 nM 9.17
CHEMBL434 ISOPROTERENOL EC50 = 0.97 nM 9.01
CHEMBL469610 — EC50 = 1.0 nM 9.00
CHEMBL272584 — EC50 = 1.1 nM 8.96
CHEMBL473493 — EC50 = 1.4 nM 8.85
CHEMBL470292 — EC50 = 1.5 nM 8.82
CHEMBL470292 — EC50 = 1.585 nM 8.80
CHEMBL271945 — EC50 = 2.0 nM 8.70
CHEMBL472089 — EC50 = 2.8 nM 8.55
CHEMBL515397 — EC50 = 3.1 nM 8.51