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Assay Detail

CHEMBL947243

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Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL ↗
50
Total Activities
50
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 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
EC50 50 7.04 10.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 10.08
CHEMBL459645 — — 1 7.96
CHEMBL459646 — — 1 7.92
CHEMBL488431 — — 1 7.92
CHEMBL488430 — — 1 7.89
CHEMBL453575 — — 1 7.82
CHEMBL507003 — — 1 7.66
CHEMBL453056 — — 1 7.62
CHEMBL509156 — — 1 7.55
CHEMBL487443 — — 1 7.43
CHEMBL529659 — — 1 7.41
CHEMBL461301 — — 1 7.28
CHEMBL256418 — — 1 7.26
CHEMBL488051 — — 1 7.21
CHEMBL510102 — — 1 7.12
CHEMBL452798 — — 1 7.10
CHEMBL451772 — — 1 7.08
CHEMBL520903 — — 1 7.08
CHEMBL486051 — — 1 7.07
CHEMBL459862 — — 1 7.04
CHEMBL452034 — — 1 6.96
CHEMBL452033 — — 1 6.92
CHEMBL488223 — — 1 6.89
CHEMBL453322 — — 1 6.89
CHEMBL487682 — — 1 6.82
CHEMBL512147 — — 1 6.82
CHEMBL459863 — — 1 6.75
CHEMBL507506 — — 1 6.72
CHEMBL460256 — — 1 6.68
CHEMBL409718 — — 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 0.084 nM 10.08
CHEMBL459645 — EC50 = 11.0 nM 7.96
CHEMBL488431 — EC50 = 12.0 nM 7.92
CHEMBL459646 — EC50 = 12.0 nM 7.92
CHEMBL488430 — EC50 = 13.0 nM 7.89
CHEMBL453575 — EC50 = 15.0 nM 7.82
CHEMBL507003 — EC50 = 22.0 nM 7.66
CHEMBL453056 — EC50 = 24.0 nM 7.62
CHEMBL509156 — EC50 = 28.0 nM 7.55
CHEMBL487443 — EC50 = 37.0 nM 7.43
CHEMBL529659 — EC50 = 39.0 nM 7.41
CHEMBL461301 — EC50 = 52.0 nM 7.28
CHEMBL256418 — EC50 = 55.0 nM 7.26
CHEMBL488051 — EC50 = 62.0 nM 7.21
CHEMBL510102 — EC50 = 75.0 nM 7.12
CHEMBL452798 — EC50 = 80.0 nM 7.10
CHEMBL451772 — EC50 = 84.0 nM 7.08
CHEMBL520903 — EC50 = 83.0 nM 7.08
CHEMBL486051 — EC50 = 86.0 nM 7.07
CHEMBL459862 — EC50 = 91.0 nM 7.04
CHEMBL452034 — EC50 = 110.0 nM 6.96
CHEMBL452033 — EC50 = 120.0 nM 6.92
CHEMBL488223 — EC50 = 130.0 nM 6.89
CHEMBL453322 — EC50 = 130.0 nM 6.89
CHEMBL512147 — EC50 = 150.0 nM 6.82
CHEMBL487682 — EC50 = 150.0 nM 6.82
CHEMBL459863 — EC50 = 180.0 nM 6.75
CHEMBL507506 — EC50 = 190.0 nM 6.72
CHEMBL460256 — EC50 = 210.0 nM 6.68
CHEMBL409718 — EC50 = 260.0 nM 6.58
CHEMBL453323 — EC50 = 280.0 nM 6.55
CHEMBL451760 — EC50 = 300.0 nM 6.52
CHEMBL516804 — EC50 = 320.0 nM 6.50
CHEMBL460257 — EC50 = 400.0 nM 6.40
CHEMBL518168 — EC50 = 440.0 nM 6.36
CHEMBL488224 — EC50 = 480.0 nM 6.32
CHEMBL510100 — EC50 = 500.0 nM 6.30
CHEMBL461282 — EC50 = 500.0 nM 6.30
CHEMBL516785 — EC50 = 510.0 nM 6.29
CHEMBL453048 — EC50 = 690.0 nM 6.16
CHEMBL272584 — EC50 = 720.0 nM 6.14
CHEMBL453047 — EC50 = 780.0 nM 6.11
CHEMBL521406 — EC50 > 1000.0 nM -
CHEMBL472105 — EC50 > 1000.0 nM -
CHEMBL470292 — EC50 > 1000.0 nM -
CHEMBL469884 — EC50 > 1000.0 nM -
CHEMBL469685 — EC50 > 1000.0 nM -
CHEMBL270026 — EC50 > 1000.0 nM -
CHEMBL453835 — EC50 > 1000.0 nM -
CHEMBL271945 — EC50 > 1000.0 nM -