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Assay Detail

CHEMBL833517

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

Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
15
Total Activities
15
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 Expert

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
Mizuno K, Sawa M, Harada H, Tateishi H, Oue M, Tsujiuchi H, Furutani Y, Kato S.
Bioorg Med Chem Lett (2004) 14 : 5959 -5962
PubMed 15546707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.36 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185703 1 7.72
CHEMBL186135 1 7.70
CHEMBL189081 1 7.66
CHEMBL187317 1 7.58
CHEMBL361505 1 7.54
CHEMBL362136 1 7.54
CHEMBL185660 1 7.40
CHEMBL184407 1 7.36
CHEMBL186271 1 7.31
CHEMBL186676 1 7.27
CHEMBL186236 1 7.24
CHEMBL185836 1 7.18
CHEMBL187209 1 7.14
CHEMBL362763 1 7.07
CHEMBL188196 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185703 EC50 = 19.0 nM 7.72
CHEMBL186135 EC50 = 20.0 nM 7.70
CHEMBL189081 EC50 = 22.0 nM 7.66
CHEMBL187317 EC50 = 26.0 nM 7.58
CHEMBL361505 EC50 = 29.0 nM 7.54
CHEMBL362136 EC50 = 29.0 nM 7.54
CHEMBL185660 EC50 = 40.0 nM 7.40
CHEMBL184407 EC50 = 44.0 nM 7.36
CHEMBL186271 EC50 = 49.0 nM 7.31
CHEMBL186676 EC50 = 54.0 nM 7.27
CHEMBL186236 EC50 = 58.0 nM 7.24
CHEMBL185836 EC50 = 66.0 nM 7.18
CHEMBL187209 EC50 = 72.0 nM 7.14
CHEMBL362763 EC50 = 85.0 nM 7.07
CHEMBL188196 EC50 = 180.0 nM 6.75