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Assay Detail

CHEMBL3256334

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

Binding
Antagonist activity at beta1 adrenoceptor in guinea pig atrium assessed as inhibition of isoproterenol-induced response after 20 mins
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Cardiac atrium
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents.
Williams LR, Lap BV, Lim CH, Temple DM, Easson PA, Letts GL.
J Med Chem (1978) 21 : 1081 -1084
PubMed 31474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 12 6.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 8.70
CHEMBL3246228 1 8.24
CHEMBL3246232 1 8.00
CHEMBL24 ATENOLOL 4.0 1 7.36
CHEMBL3246231 1 6.90
CHEMBL3246227 1 6.80
CHEMBL6995 PRACTOLOL 4.0 1 6.67
CHEMBL3246226 1 6.21
CHEMBL3246229 1 6.20
CHEMBL3246233 1 6.10
CHEMBL3246230 1 5.83
CHEMBL3246235 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL Kd = 1.995 nM 8.70
CHEMBL3246228 Kd = 5.754 nM 8.24
CHEMBL3246232 Kd = 10.0 nM 8.00
CHEMBL24 ATENOLOL Kd = 43.65 nM 7.36
CHEMBL3246231 Kd = 125.89 nM 6.90
CHEMBL3246227 Kd = 158.49 nM 6.80
CHEMBL6995 PRACTOLOL Kd = 213.8 nM 6.67
CHEMBL3246226 Kd = 616.6 nM 6.21
CHEMBL3246229 Kd = 630.96 nM 6.20
CHEMBL3246233 Kd = 794.33 nM 6.10
CHEMBL3246230 Kd = 1479.11 nM 5.83
CHEMBL3246235 Kd = 2511.89 nM 5.60