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Assay Detail

CHEMBL655651

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 atria
8
Total Activities
8
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 8 7.76 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499 TIMOLOL 4.0 1 9.44
CHEMBL1788270 1 7.88
CHEMBL2110257 1 7.78
CHEMBL1744069 1 7.57
CHEMBL368457 1 7.47
CHEMBL173976 1 7.46
CHEMBL305153 1 7.43
CHEMBL26917 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499 TIMOLOL Kd = 0.3631 nM 9.44
CHEMBL1788270 Kd = 13.18 nM 7.88
CHEMBL2110257 Kd = 16.6 nM 7.78
CHEMBL1744069 Kd = 26.92 nM 7.57
CHEMBL368457 Kd = 33.88 nM 7.47
CHEMBL173976 Kd = 34.67 nM 7.46
CHEMBL305153 Kd = 37.15 nM 7.43
CHEMBL26917 Kd = 97.72 nM 7.01