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Assay Detail

CHEMBL3603434

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

Functional
Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
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 Highly Potent and Selective Human β3-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects.
Wada Y, Shirahashi H, Iwanami T, Ogawa M, Nakano S, Morimoto A, Kasahara K, Tanaka E, Takada Y, Ohashi S, Mori M, Shuto S.
J Med Chem (2015) 58 : 6048 -6057
PubMed 26125514 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.33 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3601305 1 7.89
CHEMBL3601204 1 7.85
CHEMBL3600395 1 7.77
CHEMBL3601200 1 7.68
CHEMBL3601201 1 7.40
CHEMBL3601203 1 7.37
CHEMBL3601308 1 7.19
CHEMBL3601307 1 7.18
CHEMBL3601202 1 7.15
CHEMBL434 ISOPROTERENOL 4.0 1 7.07
CHEMBL3601310 1 6.96
CHEMBL3601306 1 6.47
CHEMBL3601309 1 -
CHEMBL1437 NOREPINEPHRINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3601305 EC50 = 13.0 nM 7.89
CHEMBL3601204 EC50 = 14.0 nM 7.85
CHEMBL3600395 EC50 = 17.0 nM 7.77
CHEMBL3601200 EC50 = 21.0 nM 7.68
CHEMBL3601201 EC50 = 40.0 nM 7.40
CHEMBL3601203 EC50 = 43.0 nM 7.37
CHEMBL3601308 EC50 = 64.0 nM 7.19
CHEMBL3601307 EC50 = 66.0 nM 7.18
CHEMBL3601202 EC50 = 71.0 nM 7.15
CHEMBL434 ISOPROTERENOL EC50 = 86.0 nM 7.07
CHEMBL3601310 EC50 = 111.0 nM 6.96
CHEMBL3601306 EC50 = 338.0 nM 6.47
CHEMBL3601309 EC50 > 10000.0 nM -
CHEMBL1437 NOREPINEPHRINE EC50 - -