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Assay Detail

CHEMBL651630

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Functional
Antagonist activity against beta-2 adrenergic receptor in isolated guinea pig trachea
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Beta-2 adrenergic receptor (CHEMBL5414)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Role of the (acyloxy)methyl moiety in eliciting the adrenergic beta-blocking activity of 3-(acyloxy)propanolamines.
Macchia B, Balsamo A, Lapucci A, Macchia F, Martinelli A, Ammon HL, Prasad SM, Breschi MC, Ducci M, Martinotti E.
J Med Chem (1987) 30 : 616 -622
PubMed 2882026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 5.62 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL156603 1 7.72
CHEMBL289093 BUTOXAMINE 2.0 1 6.89
CHEMBL156147 1 6.33
CHEMBL157557 1 5.64
CHEMBL156682 1 5.60
CHEMBL156271 1 5.37
CHEMBL156683 1 5.00
CHEMBL156304 1 4.58
CHEMBL449651 1 4.54
CHEMBL6995 PRACTOLOL 4.0 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL156603 Kd = 19.05 nM 7.72
CHEMBL289093 BUTOXAMINE Kd = 128.82 nM 6.89
CHEMBL156147 Kd = 467.74 nM 6.33
CHEMBL157557 Kd = 2290.87 nM 5.64
CHEMBL156682 Kd = 2511.89 nM 5.60
CHEMBL156271 Kd = 4265.8 nM 5.37
CHEMBL156683 Kd = 10000.0 nM 5.00
CHEMBL156304 Kd = 26302.68 nM 4.58
CHEMBL449651 Kd = 28840.32 nM 4.54
CHEMBL6995 PRACTOLOL Kd = 31622.78 nM 4.50