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Assay Detail

CHEMBL655219

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

Binding
Ability to block Beta-2 adrenergic receptor in guinea pig trachea preparation
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

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 6.51 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281967 1 8.90
CHEMBL27 PROPRANOLOL 4.0 1 8.90
CHEMBL13365 1 8.90
CHEMBL281294 1 8.80
CHEMBL284909 1 7.90
CHEMBL13284 1 7.90
CHEMBL31335 1 7.80
CHEMBL281298 1 7.40
CHEMBL31450 1 7.20
CHEMBL13358 1 7.10
CHEMBL30622 1 6.60
CHEMBL31608 1 6.10
CHEMBL30289 1 6.10
CHEMBL31025 1 5.90
CHEMBL6995 PRACTOLOL 4.0 1 5.80
CHEMBL31036 1 5.70
CHEMBL286894 1 5.50
CHEMBL13504 1 5.50
CHEMBL30899 1 5.40
CHEMBL30292 1 5.40
CHEMBL279777 1 5.20
CHEMBL768 ESMOLOL 4.0 1 5.20
CHEMBL31638 1 5.20
CHEMBL31117 1 5.20
CHEMBL31416 1 4.90
CHEMBL31583 1 4.80
CHEMBL31677 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281967 Kd = 1.259 nM 8.90
CHEMBL27 PROPRANOLOL Kd = 1.259 nM 8.90
CHEMBL13365 Kd = 1.259 nM 8.90
CHEMBL281294 Kd = 1.585 nM 8.80
CHEMBL284909 Kd = 12.59 nM 7.90
CHEMBL13284 Kd = 12.59 nM 7.90
CHEMBL31335 Kd = 15.85 nM 7.80
CHEMBL281298 Kd = 39.81 nM 7.40
CHEMBL31450 Kd = 63.1 nM 7.20
CHEMBL13358 Kd = 79.43 nM 7.10
CHEMBL30622 Kd = 251.19 nM 6.60
CHEMBL31608 Kd = 794.33 nM 6.10
CHEMBL30289 Kd = 794.33 nM 6.10
CHEMBL31025 Kd = 1258.93 nM 5.90
CHEMBL6995 PRACTOLOL Kd = 1584.89 nM 5.80
CHEMBL31036 Kd = 1995.26 nM 5.70
CHEMBL286894 Kd = 3162.28 nM 5.50
CHEMBL13504 Kd = 3162.28 nM 5.50
CHEMBL30899 Kd = 3981.07 nM 5.40
CHEMBL30292 Kd = 3981.07 nM 5.40
CHEMBL279777 Kd = 6309.57 nM 5.20
CHEMBL768 ESMOLOL Kd = 6309.57 nM 5.20
CHEMBL31638 Kd = 6309.57 nM 5.20
CHEMBL31117 Kd = 6309.57 nM 5.20
CHEMBL31416 Kd = 12589.25 nM 4.90
CHEMBL31583 Kd = 15848.93 nM 4.80
CHEMBL31677 Kd > 10000.0 nM -