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Assay Detail

CHEMBL822565

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

Functional
Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Beta-3 adrenergic receptor (CHEMBL246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carboxyl-promoted enhancement of selectivity for the 3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-3 binding selectivity
Sher PM, Mathur A, Fisher LG, Wu G, Skwish S, Michel IM, Seiler SM, Dickinson KE
Bioorg Med Chem Lett (1997) 7 : 1583 -1588
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 6.16 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38538 1 7.22
CHEMBL38486 1 6.38
CHEMBL40966 1 6.21
CHEMBL284782 1 6.17
CHEMBL41113 1 6.12
CHEMBL39596 1 5.79
CHEMBL38569 1 5.79
CHEMBL41948 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38538 EC50 = 60.0 nM 7.22
CHEMBL38486 EC50 = 420.0 nM 6.38
CHEMBL40966 EC50 = 610.0 nM 6.21
CHEMBL284782 EC50 = 680.0 nM 6.17
CHEMBL41113 EC50 = 750.0 nM 6.12
CHEMBL39596 EC50 = 1610.0 nM 5.79
CHEMBL38569 EC50 = 1610.0 nM 5.79
CHEMBL41948 EC50 = 2640.0 nM 5.58