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Assay Detail

CHEMBL3129374

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

Functional
Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay
26
Total Activities
26
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

Design, synthesis, and evaluation of conformationally restricted acetanilides as potent and selective β3 adrenergic receptor agonists for the treatment of overactive bladder.
Moyes CR, Berger R, Goble SD, Harper B, Shen DM, Wang L, Bansal A, Brown PN, Chen AS, Dingley KH, Di Salvo J, Fitzmaurice A, Gichuru LN, Hurley AL, Jochnowitz N, Miller RR, Mistry S, Nagabukuro H, Salituro GM, Sanfiz A, Stevenson AS, Villa K, Zamlynny B, Struthers M, Weber AE, Edmondson SD.
J Med Chem (2014) 57 : 1437 -1453
PubMed 24437735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 8.80 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3128199 1 10.40
CHEMBL3128200 1 9.89
CHEMBL3128194 1 9.82
CHEMBL3128198 1 9.82
CHEMBL3128189 1 9.74
CHEMBL3128196 1 9.68
CHEMBL3128201 1 9.43
CHEMBL3128179 1 9.32
CHEMBL3128177 1 9.19
CHEMBL3128190 1 9.17
CHEMBL3128191 1 9.08
CHEMBL3128192 1 9.06
CHEMBL1684585 1 9.01
CHEMBL3128180 1 8.94
CHEMBL3128178 1 8.87
CHEMBL3128193 1 8.80
CHEMBL3128197 1 8.73
CHEMBL3128181 1 8.71
CHEMBL3128188 1 8.43
CHEMBL3128185 1 8.06
CHEMBL3128183 1 7.91
CHEMBL3128182 1 7.87
CHEMBL3128187 1 7.78
CHEMBL3128195 1 7.36
CHEMBL3128186 1 7.12
CHEMBL3128184 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3128199 EC50 = 0.04 nM 10.40
CHEMBL3128200 EC50 = 0.13 nM 9.89
CHEMBL3128194 EC50 = 0.15 nM 9.82
CHEMBL3128198 EC50 = 0.15 nM 9.82
CHEMBL3128189 EC50 = 0.18 nM 9.74
CHEMBL3128196 EC50 = 0.21 nM 9.68
CHEMBL3128201 EC50 = 0.37 nM 9.43
CHEMBL3128179 EC50 = 0.48 nM 9.32
CHEMBL3128177 EC50 = 0.64 nM 9.19
CHEMBL3128190 EC50 = 0.67 nM 9.17
CHEMBL3128191 EC50 = 0.83 nM 9.08
CHEMBL3128192 EC50 = 0.88 nM 9.06
CHEMBL1684585 EC50 = 0.98 nM 9.01
CHEMBL3128180 EC50 = 1.15 nM 8.94
CHEMBL3128178 EC50 = 1.36 nM 8.87
CHEMBL3128193 EC50 = 1.6 nM 8.80
CHEMBL3128197 EC50 = 1.86 nM 8.73
CHEMBL3128181 EC50 = 1.95 nM 8.71
CHEMBL3128188 EC50 = 3.7 nM 8.43
CHEMBL3128185 EC50 = 8.78 nM 8.06
CHEMBL3128183 EC50 = 12.4 nM 7.91
CHEMBL3128182 EC50 = 13.6 nM 7.87
CHEMBL3128187 EC50 = 16.7 nM 7.78
CHEMBL3128195 EC50 = 44.2 nM 7.36
CHEMBL3128186 EC50 = 76.7 nM 7.12
CHEMBL3128184 EC50 = 186.0 nM 6.73