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Assay Detail

CHEMBL652717

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

Binding
Inhibitory activity against beta adrenergic receptor of rat frontal cortex homogenate using (1.0 nM) [3H]- dihydroalprenolol
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor beta (CHEMBL2095166)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Design and synthesis of propranolol analogues as serotonergic agents.
Pierson ME, Lyon RA, Titeler M, Schulman SB, Kowalski P, Glennon RA.
J Med Chem (1989) 32 : 859 -863
PubMed 2539480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.88 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 8.62
CHEMBL138136 1 5.62
CHEMBL139103 1 5.35
CHEMBL138907 1 5.30
CHEMBL140417 1 5.28
CHEMBL169956 1 5.08
CHEMBL334465 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL Ki = 2.4 nM 8.62
CHEMBL138136 Ki = 2400.0 nM 5.62
CHEMBL139103 Ki = 4500.0 nM 5.35
CHEMBL138907 Ki = 5000.0 nM 5.30
CHEMBL140417 Ki = 5300.0 nM 5.28
CHEMBL169956 Ki = 8300.0 nM 5.08
CHEMBL334465 Ki > 10000.0 nM -