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Assay Detail

CHEMBL951065

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Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL ↗
43
Total Activities
43
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 a novel series of biphenyl benzoic acid derivatives as potent and selective human beta3-adrenergic receptor agonists with good oral bioavailability. Part I.
Imanishi M, Tomishima Y, Itou S, Hamashima H, Nakajima Y, Washizuka K, 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 : 1925 -1944
PubMed 18307290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 43 8.30 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL270964 — — 1 9.54
CHEMBL409718 — — 1 9.52
CHEMBL273006 — — 1 9.47
CHEMBL256418 — — 1 9.34
CHEMBL411028 — — 1 9.27
CHEMBL271574 — — 1 9.25
CHEMBL272583 — — 1 9.23
CHEMBL270026 — — 1 9.22
CHEMBL270889 — — 1 9.21
CHEMBL409533 — — 1 9.09
CHEMBL434 ISOPROTERENOL 4.0 1 9.01
CHEMBL272584 — — 1 8.96
CHEMBL273028 — — 1 8.74
CHEMBL271945 — — 1 8.70
CHEMBL257297 — — 1 8.70
CHEMBL408693 — — 1 8.66
CHEMBL271401 — — 1 8.40
CHEMBL269816 — — 1 8.37
CHEMBL409827 — — 1 8.34
CHEMBL272383 — — 1 8.32
CHEMBL408145 — — 1 8.31
CHEMBL273098 — — 1 8.26
CHEMBL271576 — — 1 8.17
CHEMBL271765 — — 1 8.12
CHEMBL272234 — — 1 8.06
CHEMBL271367 — — 1 8.01
CHEMBL257106 — — 1 8.01
CHEMBL270460 — — 1 7.92
CHEMBL536330 — — 1 7.92
CHEMBL269920 — — 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL270964 — EC50 = 0.29 nM 9.54
CHEMBL409718 — EC50 = 0.3 nM 9.52
CHEMBL273006 — EC50 = 0.34 nM 9.47
CHEMBL256418 — EC50 = 0.46 nM 9.34
CHEMBL411028 — EC50 = 0.54 nM 9.27
CHEMBL271574 — EC50 = 0.56 nM 9.25
CHEMBL272583 — EC50 = 0.59 nM 9.23
CHEMBL270026 — EC50 = 0.6 nM 9.22
CHEMBL270889 — EC50 = 0.62 nM 9.21
CHEMBL409533 — EC50 = 0.81 nM 9.09
CHEMBL434 ISOPROTERENOL EC50 = 0.97 nM 9.01
CHEMBL272584 — EC50 = 1.1 nM 8.96
CHEMBL273028 — EC50 = 1.8 nM 8.74
CHEMBL271945 — EC50 = 2.0 nM 8.70
CHEMBL257297 — EC50 = 2.0 nM 8.70
CHEMBL408693 — EC50 = 2.2 nM 8.66
CHEMBL271401 — EC50 = 4.0 nM 8.40
CHEMBL269816 — EC50 = 4.3 nM 8.37
CHEMBL409827 — EC50 = 4.6 nM 8.34
CHEMBL272383 — EC50 = 4.8 nM 8.32
CHEMBL408145 — EC50 = 4.9 nM 8.31
CHEMBL273098 — EC50 = 5.5 nM 8.26
CHEMBL271576 — EC50 = 6.7 nM 8.17
CHEMBL271765 — EC50 = 7.5 nM 8.12
CHEMBL272234 — EC50 = 8.7 nM 8.06
CHEMBL271367 — EC50 = 9.8 nM 8.01
CHEMBL257106 — EC50 = 9.7 nM 8.01
CHEMBL270460 — EC50 = 12.0 nM 7.92
CHEMBL536330 — EC50 = 12.0 nM 7.92
CHEMBL269920 — EC50 = 15.0 nM 7.82
CHEMBL59765 — EC50 = 16.0 nM 7.80
CHEMBL269823 — EC50 = 17.0 nM 7.77
CHEMBL270025 — EC50 = 18.0 nM 7.75
CHEMBL408694 — EC50 = 32.0 nM 7.50
CHEMBL273097 — EC50 = 33.0 nM 7.48
CHEMBL409828 — EC50 = 39.0 nM 7.41
CHEMBL270027 — EC50 = 39.0 nM 7.41
CHEMBL537693 — EC50 = 48.0 nM 7.32
CHEMBL408958 — EC50 = 61.0 nM 7.21
CHEMBL408957 — EC50 = 85.0 nM 7.07
CHEMBL260100 — EC50 = 91.0 nM 7.04
CHEMBL411234 — EC50 = 100.0 nM 7.00
CHEMBL536108 — EC50 > 100.0 nM -