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Assay Detail

CHEMBL834457

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Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
Nakajima Y, Hamashima H, Washizuka K, Tomishima Y, Ohtake H, Imamura E, Miura T, Kayakiri H, Kato M.
Bioorg Med Chem Lett (2005) 15 : 251 -254
PubMed 15603933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.52 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183129 1 9.30
CHEMBL183611 1 9.10
CHEMBL434 ISOPROTERENOL 4.0 1 9.01
CHEMBL369346 1 9.00
CHEMBL183744 1 8.96
CHEMBL183283 1 8.82
CHEMBL434524 1 8.80
CHEMBL182127 1 8.68
CHEMBL183307 1 8.60
CHEMBL425173 1 8.31
CHEMBL181115 1 8.08
CHEMBL183211 1 7.89
CHEMBL183080 1 7.66
CHEMBL183433 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183129 EC50 = 0.5 nM 9.30
CHEMBL183611 EC50 = 0.8 nM 9.10
CHEMBL434 ISOPROTERENOL EC50 = 0.97 nM 9.01
CHEMBL369346 EC50 = 1.0 nM 9.00
CHEMBL183744 EC50 = 1.1 nM 8.96
CHEMBL183283 EC50 = 1.5 nM 8.82
CHEMBL434524 EC50 = 1.6 nM 8.80
CHEMBL182127 EC50 = 2.1 nM 8.68
CHEMBL183307 EC50 = 2.5 nM 8.60
CHEMBL425173 EC50 = 4.9 nM 8.31
CHEMBL181115 EC50 = 8.3 nM 8.08
CHEMBL183211 EC50 = 13.0 nM 7.89
CHEMBL183080 EC50 = 22.0 nM 7.66
CHEMBL183433 EC50 = 74.0 nM 7.13