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Assay Detail

CHEMBL653375

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

Functional
Antagonist activity against beta-1 adrenergic receptor in isolated guinea pig atria
11
Total Activities
11
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

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 11 5.29 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266548 1 6.90
CHEMBL156603 1 6.34
CHEMBL156147 1 5.80
CHEMBL6995 PRACTOLOL 4.0 1 5.78
CHEMBL156682 1 5.10
CHEMBL156683 1 4.96
CHEMBL449651 1 4.94
CHEMBL157557 1 4.91
CHEMBL156271 1 4.57
CHEMBL156304 1 4.55
CHEMBL289093 BUTOXAMINE 2.0 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266548 Kd = 125.89 nM 6.90
CHEMBL156603 Kd = 457.09 nM 6.34
CHEMBL156147 Kd = 1584.89 nM 5.80
CHEMBL6995 PRACTOLOL Kd = 1659.59 nM 5.78
CHEMBL156682 Kd = 7943.28 nM 5.10
CHEMBL156683 Kd = 10964.78 nM 4.96
CHEMBL449651 Kd = 11481.54 nM 4.94
CHEMBL157557 Kd = 12302.69 nM 4.91
CHEMBL156271 Kd = 26915.35 nM 4.57
CHEMBL156304 Kd = 28183.83 nM 4.55
CHEMBL289093 BUTOXAMINE Kd = 44668.36 nM 4.35