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Assay Detail

CHEMBL650243

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

Functional
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Parmee ER, Brockunier LL, He J, Singh SB, Candelore MR, Cascieri MA, Deng L, Liu Y, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
Bioorg Med Chem Lett (2000) 10 : 2283 -2286
PubMed 11055339 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.51 8.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL174984 TRETOQUINOL 2.0 1 8.46
CHEMBL75604 1 6.47
CHEMBL312074 1 6.24
CHEMBL421871 1 5.82
CHEMBL308868 1 5.57
CHEMBL74860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL174984 TRETOQUINOL EC50 = 3.5 nM 8.46
CHEMBL75604 EC50 = 340.0 nM 6.47
CHEMBL312074 EC50 = 580.0 nM 6.24
CHEMBL421871 EC50 = 1500.0 nM 5.82
CHEMBL308868 EC50 = 2700.0 nM 5.57
CHEMBL74860 EC50 > 1000.0 nM -