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Assay Detail

CHEMBL651631

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

Functional
Antagonistic activity against beta-2 adrenergic receptor on isolated guinea pig tracheal strips
11
Total Activities
11
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

An interdisciplinary approach to the design of new structures active at the beta-adrenergic receptor. Aliphatic oxime ether derivatives.
Macchia B, Balsamo A, Lapucci A, Martinelli A, Macchia F, Breschi MC, Fantoni B, Martinotti E.
J Med Chem (1985) 28 : 153 -160
PubMed 2857200 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 7.38 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287766 1 8.62
CHEMBL41839 1 8.52
CHEMBL40626 1 8.38
CHEMBL40783 1 8.20
CHEMBL289858 1 7.98
CHEMBL289868 1 7.41
CHEMBL41378 1 7.14
CHEMBL289093 BUTOXAMINE 2.0 1 6.89
CHEMBL431713 1 6.81
CHEMBL40971 1 6.76
CHEMBL6995 PRACTOLOL 4.0 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287766 Kd = 2.399 nM 8.62
CHEMBL41839 Kd = 3.02 nM 8.52
CHEMBL40626 Kd = 4.169 nM 8.38
CHEMBL40783 Kd = 6.31 nM 8.20
CHEMBL289858 Kd = 10.47 nM 7.98
CHEMBL289868 Kd = 38.9 nM 7.41
CHEMBL41378 Kd = 72.44 nM 7.14
CHEMBL289093 BUTOXAMINE Kd = 128.82 nM 6.89
CHEMBL431713 Kd = 154.88 nM 6.81
CHEMBL40971 Kd = 173.78 nM 6.76
CHEMBL6995 PRACTOLOL Kd = 31622.78 nM 4.50