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Assay Detail

CHEMBL653376

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Functional
Antagonistic activity against beta-1 adrenergic receptor of isolated guinea pig atria
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-1 adrenergic receptor (CHEMBL5471)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

An interdisciplinary approach to the design of new structures active at the beta-adrenergic receptor. Aliphatic oxime ether derivatives.
Macchia B, Balsamo A, Lapucci A, Martinelli A, Macchia F, Breschi MC, Fantoni B, Martinotti E.
J Med Chem (1985) 28 : 153 -160
PubMed 2857200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 5.03 6.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40626 1 6.02
CHEMBL289858 1 5.90
CHEMBL6995 PRACTOLOL 4.0 1 5.78
CHEMBL287766 1 5.33
CHEMBL289868 1 5.08
CHEMBL288140 1 4.84
CHEMBL41839 1 4.77
CHEMBL41378 1 4.70
CHEMBL40783 1 4.68
CHEMBL431713 1 4.61
CHEMBL289093 BUTOXAMINE 2.0 1 4.35
CHEMBL40971 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40626 Kd = 954.99 nM 6.02
CHEMBL289858 Kd = 1258.93 nM 5.90
CHEMBL6995 PRACTOLOL Kd = 1659.59 nM 5.78
CHEMBL287766 Kd = 4677.35 nM 5.33
CHEMBL289868 Kd = 8317.64 nM 5.08
CHEMBL288140 Kd = 14454.4 nM 4.84
CHEMBL41839 Kd = 16982.44 nM 4.77
CHEMBL41378 Kd = 19952.62 nM 4.70
CHEMBL40783 Kd = 20892.96 nM 4.68
CHEMBL431713 Kd = 24547.09 nM 4.61
CHEMBL289093 BUTOXAMINE Kd = 44668.36 nM 4.35
CHEMBL40971 Kd = 53703.18 nM 4.27