Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4051035

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

Binding
Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of Novel Indazole Derivatives as Orally Available β3-Adrenergic Receptor Agonists Lacking Off-Target-Based Cardiovascular Side Effects.
Wada Y, Nakano S, Morimoto A, Kasahara KI, Hayashi T, Takada Y, Suzuki H, Niwa-Sakai M, Ohashi S, Mori M, Hirokawa T, Shuto S.
J Med Chem (2017) 60 : 3252 -3265
PubMed 28355078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.66 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188622 1 8.77
CHEMBL4089669 1 8.41
CHEMBL4104183 1 8.19
CHEMBL3601305 1 7.89
CHEMBL3601204 1 7.85
CHEMBL4073098 1 7.75
CHEMBL4067502 1 7.75
CHEMBL3601200 1 7.68
CHEMBL4080868 1 7.37
CHEMBL3601307 1 7.18
CHEMBL4105097 1 7.16
CHEMBL434 ISOPROTERENOL 4.0 1 7.07
CHEMBL4088750 1 6.51
CHEMBL1437 NOREPINEPHRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188622 EC50 = 1.7 nM 8.77
CHEMBL4089669 EC50 = 3.9 nM 8.41
CHEMBL4104183 EC50 = 6.5 nM 8.19
CHEMBL3601305 EC50 = 13.0 nM 7.89
CHEMBL3601204 EC50 = 14.0 nM 7.85
CHEMBL4073098 EC50 = 18.0 nM 7.75
CHEMBL4067502 EC50 = 18.0 nM 7.75
CHEMBL3601200 EC50 = 21.0 nM 7.68
CHEMBL4080868 EC50 = 43.0 nM 7.37
CHEMBL3601307 EC50 = 66.0 nM 7.18
CHEMBL4105097 EC50 = 70.0 nM 7.16
CHEMBL434 ISOPROTERENOL EC50 = 86.0 nM 7.07
CHEMBL4088750 EC50 = 309.0 nM 6.51
CHEMBL1437 NOREPINEPHRINE EC50 - -