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Assay Detail

CHEMBL1007085

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

Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
45
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-1 adrenergic receptor (CHEMBL213)
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 45 6.65 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 9.08
CHEMBL470857 1 7.41
CHEMBL256418 1 7.26
CHEMBL523149 1 7.03
CHEMBL473495 1 6.89
CHEMBL469610 1 6.89
CHEMBL446806 1 6.85
CHEMBL473702 1 6.82
CHEMBL472089 1 6.80
CHEMBL270964 1 6.77
CHEMBL491726 1 6.70
CHEMBL479341 1 6.66
CHEMBL491891 1 6.62
CHEMBL272383 1 6.60
CHEMBL471060 1 6.58
CHEMBL409718 1 6.58
CHEMBL479530 1 6.50
CHEMBL513419 1 6.43
CHEMBL490733 1 6.41
CHEMBL488224 1 6.32
CHEMBL516209 1 6.31
CHEMBL470858 1 6.14
CHEMBL272584 1 6.14
CHEMBL472090 1 6.12
CHEMBL445481 1 6.10
CHEMBL479342 1 6.08
CHEMBL455773 1 6.05
CHEMBL273006 1 6.01
CHEMBL271945 1 -
CHEMBL479727 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 0.84 nM 9.08
CHEMBL470857 EC50 = 39.0 nM 7.41
CHEMBL256418 EC50 = 55.0 nM 7.26
CHEMBL523149 EC50 = 93.0 nM 7.03
CHEMBL473495 EC50 = 130.0 nM 6.89
CHEMBL469610 EC50 = 130.0 nM 6.89
CHEMBL446806 EC50 = 140.0 nM 6.85
CHEMBL473702 EC50 = 150.0 nM 6.82
CHEMBL472089 EC50 = 160.0 nM 6.80
CHEMBL270964 EC50 = 170.0 nM 6.77
CHEMBL491726 EC50 = 200.0 nM 6.70
CHEMBL479341 EC50 = 220.0 nM 6.66
CHEMBL491891 EC50 = 240.0 nM 6.62
CHEMBL272383 EC50 = 250.0 nM 6.60
CHEMBL409718 EC50 = 260.0 nM 6.58
CHEMBL471060 EC50 = 260.0 nM 6.58
CHEMBL479530 EC50 = 320.0 nM 6.50
CHEMBL513419 EC50 = 370.0 nM 6.43
CHEMBL490733 EC50 = 390.0 nM 6.41
CHEMBL488224 EC50 = 480.0 nM 6.32
CHEMBL516209 EC50 = 490.0 nM 6.31
CHEMBL272584 EC50 = 720.0 nM 6.14
CHEMBL470858 EC50 = 730.0 nM 6.14
CHEMBL472090 EC50 = 750.0 nM 6.12
CHEMBL445481 EC50 = 800.0 nM 6.10
CHEMBL479342 EC50 = 840.0 nM 6.08
CHEMBL455773 EC50 = 900.0 nM 6.05
CHEMBL273006 EC50 = 980.0 nM 6.01
CHEMBL469821 EC50 > 1000.0 nM -
CHEMBL511968 EC50 > 1000.0 nM -
CHEMBL469396 EC50 > 1000.0 nM -
CHEMBL469395 EC50 > 1000.0 nM -
CHEMBL472293 EC50 > 1000.0 nM -
CHEMBL515397 EC50 > 1000.0 nM -
CHEMBL473493 EC50 > 1000.0 nM -
CHEMBL452134 EC50 > 1000.0 nM -
CHEMBL270026 EC50 > 1000.0 nM -
CHEMBL470856 EC50 > 1000.0 nM -
CHEMBL271574 EC50 > 1000.0 nM -
CHEMBL470292 EC50 > 1000.0 nM -
CHEMBL521406 EC50 > 1000.0 nM -
CHEMBL492401 EC50 > 1000.0 nM -
CHEMBL452696 EC50 > 1000.0 nM -
CHEMBL479727 EC50 > 1000.0 nM -
CHEMBL271945 EC50 > 1000.0 nM -