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Assay Detail

CHEMBL3768478

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

Functional
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
13
Total Activities
13
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 Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Edmondson SD, Zhu C, Kar NF, Di Salvo J, Nagabukuro H, Sacre-Salem B, Dingley K, Berger R, Goble SD, Morriello G, Harper B, Moyes CR, Shen DM, Wang L, Ball R, Fitzmaurice A, Frenkl T, Gichuru LN, Ha S, Hurley AL, Jochnowitz N, Levorse D, Mistry S, Miller RR, Ormes J, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Green S, Struthers M, Weber AE.
J Med Chem (2016) 59 : 609 -623
PubMed 26709102 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 8.68 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763934 1 9.21
CHEMBL1684585 1 9.05
CHEMBL2107826 VIBEGRON 4.0 1 8.96
CHEMBL3128178 1 8.85
CHEMBL3764774 1 8.77
CHEMBL111201 1 8.70
CHEMBL3763594 1 8.66
CHEMBL3763998 1 8.59
CHEMBL3765335 1 8.57
CHEMBL3128188 1 8.43
CHEMBL3764950 1 8.41
CHEMBL3764592 1 8.37
CHEMBL3764088 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763934 EC50 = 0.62 nM 9.21
CHEMBL1684585 EC50 = 0.9 nM 9.05
CHEMBL2107826 VIBEGRON EC50 = 1.1 nM 8.96
CHEMBL3128178 EC50 = 1.4 nM 8.85
CHEMBL3764774 EC50 = 1.7 nM 8.77
CHEMBL111201 EC50 = 2.0 nM 8.70
CHEMBL3763594 EC50 = 2.2 nM 8.66
CHEMBL3763998 EC50 = 2.6 nM 8.59
CHEMBL3765335 EC50 = 2.7 nM 8.57
CHEMBL3128188 EC50 = 3.7 nM 8.43
CHEMBL3764950 EC50 = 3.9 nM 8.41
CHEMBL3764592 EC50 = 4.3 nM 8.37
CHEMBL3764088 EC50 = 4.8 nM 8.32