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Assay Detail

CHEMBL834455

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Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
12
Total Activities
12
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-1 adrenergic receptor (CHEMBL213)
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 12 8.36 10.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434 ISOPROTERENOL 4.0 1 10.08
CHEMBL369346 1 9.05
CHEMBL183283 1 8.89
CHEMBL183307 1 8.66
CHEMBL183211 1 8.52
CHEMBL434524 1 8.44
CHEMBL183611 1 8.40
CHEMBL183744 1 7.92
CHEMBL182127 1 7.82
CHEMBL183129 1 7.70
CHEMBL425173 1 7.57
CHEMBL181115 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434 ISOPROTERENOL EC50 = 0.084 nM 10.08
CHEMBL369346 EC50 = 0.9 nM 9.05
CHEMBL183283 EC50 = 1.3 nM 8.89
CHEMBL183307 EC50 = 2.2 nM 8.66
CHEMBL183211 EC50 = 3.0 nM 8.52
CHEMBL434524 EC50 = 3.6 nM 8.44
CHEMBL183611 EC50 = 4.0 nM 8.40
CHEMBL183744 EC50 = 12.0 nM 7.92
CHEMBL182127 EC50 = 15.0 nM 7.82
CHEMBL183129 EC50 = 20.0 nM 7.70
CHEMBL425173 EC50 = 27.0 nM 7.57
CHEMBL181115 EC50 = 51.0 nM 7.29