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Assay Detail

CHEMBL650923

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

Binding
Ability to block Beta-1 adrenergic receptor in guinea pig right atria preparation
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function.
Erhardt PW, Woo CM, Anderson WG, Gorczynski RJ.
J Med Chem (1982) 25 : 1408 -1412
PubMed 6130154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 27 6.87 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13365 1 8.80
CHEMBL27 PROPRANOLOL 4.0 1 8.70
CHEMBL281967 1 8.60
CHEMBL281294 1 8.50
CHEMBL13284 1 8.30
CHEMBL31335 1 8.00
CHEMBL30289 1 7.30
CHEMBL281298 1 7.30
CHEMBL768 ESMOLOL 4.0 1 7.00
CHEMBL31768 1 6.80
CHEMBL13504 1 6.80
CHEMBL279777 1 6.70
CHEMBL6995 PRACTOLOL 4.0 1 6.60
CHEMBL286894 1 6.60
CHEMBL30622 1 6.60
CHEMBL30899 1 6.50
CHEMBL31025 1 6.50
CHEMBL31638 1 6.50
CHEMBL31608 1 6.50
CHEMBL30292 1 6.40
CHEMBL31583 1 6.10
CHEMBL31677 1 5.90
CHEMBL31416 1 5.90
CHEMBL285233 1 5.50
CHEMBL31117 1 5.40
CHEMBL767 1 4.70
CHEMBL31542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13365 Kd = 1.585 nM 8.80
CHEMBL27 PROPRANOLOL Kd = 1.995 nM 8.70
CHEMBL281967 Kd = 2.512 nM 8.60
CHEMBL281294 Kd = 3.162 nM 8.50
CHEMBL13284 Kd = 5.012 nM 8.30
CHEMBL31335 Kd = 10.0 nM 8.00
CHEMBL30289 Kd = 50.12 nM 7.30
CHEMBL281298 Kd = 50.12 nM 7.30
CHEMBL768 ESMOLOL Kd = 100.0 nM 7.00
CHEMBL31768 Kd = 158.49 nM 6.80
CHEMBL13504 Kd = 158.49 nM 6.80
CHEMBL279777 Kd = 199.53 nM 6.70
CHEMBL6995 PRACTOLOL Kd = 251.19 nM 6.60
CHEMBL286894 Kd = 251.19 nM 6.60
CHEMBL30622 Kd = 251.19 nM 6.60
CHEMBL30899 Kd = 316.23 nM 6.50
CHEMBL31025 Kd = 316.23 nM 6.50
CHEMBL31638 Kd = 316.23 nM 6.50
CHEMBL31608 Kd = 316.23 nM 6.50
CHEMBL30292 Kd = 398.11 nM 6.40
CHEMBL31583 Kd = 794.33 nM 6.10
CHEMBL31677 Kd = 1258.93 nM 5.90
CHEMBL31416 Kd = 1258.93 nM 5.90
CHEMBL285233 Kd = 3162.28 nM 5.50
CHEMBL31117 Kd = 3981.07 nM 5.40
CHEMBL767 Kd = 19952.62 nM 4.70
CHEMBL31542 Kd > 10000.0 nM -