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Assay Detail

CHEMBL3766299

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Functional
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Canis lupus familiaris
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-3 adrenergic receptor (CHEMBL4400)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

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 4 7.58 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2107826 VIBEGRON 4.0 1 7.96
CHEMBL111201 1 7.60
CHEMBL3765335 1 7.41
CHEMBL3764088 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2107826 VIBEGRON EC50 = 11.0 nM 7.96
CHEMBL111201 EC50 = 25.0 nM 7.60
CHEMBL3765335 EC50 = 39.0 nM 7.41
CHEMBL3764088 EC50 = 47.0 nM 7.33