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Assay Detail

CHEMBL655650

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

Functional
Compound was tested for its Beta-1 adrenergic receptor antagonistic activity on guinea pig arteria
3
Total Activities
3
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

Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
Baldwin JJ, McClure DE, Gross DM, Williams M.
J Med Chem (1982) 25 : 931 -936
PubMed 6126588 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.36 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL148306 (S)-METOPROLOL 1 8.12
CHEMBL13 METOPROLOL 4.0 1 7.83
CHEMBL1741004 (R)-METOPROLOL 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL148306 (S)-METOPROLOL Kd = 7.586 nM 8.12
CHEMBL13 METOPROLOL Kd = 14.79 nM 7.83
CHEMBL1741004 (R)-METOPROLOL Kd = 741.31 nM 6.13