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Assay Detail

CHEMBL650700

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Functional
Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A simplified template approach towards the synthesis of a potent beta-3 adrenoceptor agonist at the human receptor
Beeley L, Berge J, Chapman H, Dean D, Kelly J, Lowden K, Kotecha N, Morgan H, Rami H, Thompson M, Vong A, Ward R
Bioorg Med Chem Lett (1997) 7 : 219 -224
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 5.97 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62091 1 6.92
CHEMBL72396 1 6.54
CHEMBL305808 1 6.40
CHEMBL70399 1 6.25
CHEMBL302370 1 6.09
CHEMBL434 ISOPROTERENOL 4.0 1 6.00
CHEMBL70557 1 6.00
CHEMBL73770 1 5.96
CHEMBL70403 1 5.70
CHEMBL420746 CGP-12177 1 5.70
CHEMBL421489 1 5.66
CHEMBL72706 1 5.33
CHEMBL306838 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62091 EC50 = 120.0 nM 6.92
CHEMBL72396 EC50 = 290.0 nM 6.54
CHEMBL305808 EC50 = 400.0 nM 6.40
CHEMBL70399 EC50 = 560.0 nM 6.25
CHEMBL302370 EC50 = 820.0 nM 6.09
CHEMBL434 ISOPROTERENOL EC50 = 1000.0 nM 6.00
CHEMBL70557 EC50 = 1000.0 nM 6.00
CHEMBL73770 EC50 = 1100.0 nM 5.96
CHEMBL70403 EC50 = 2000.0 nM 5.70
CHEMBL420746 CGP-12177 EC50 = 2000.0 nM 5.70
CHEMBL421489 EC50 = 2200.0 nM 5.66
CHEMBL72706 EC50 = 4700.0 nM 5.33
CHEMBL306838 EC50 = 7900.0 nM 5.10