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Assay Detail

CHEMBL840063

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

Binding
Binding inhibition constant was determined by inhibition of [125I]-iodocyanopindolol binding to Beta-1 adrenergic receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 2: SAR of the methylene derivatives.
Sawa M, Tateishi H, Mizuno K, Harada H, Oue M, Tsujiuchi H, Furutani Y, Kato S.
Bioorg Med Chem Lett (2004) 14 : 5963 -5966
PubMed 15546708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.09 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442225 1 7.47
CHEMBL184407 1 7.18
CHEMBL186247 1 7.05
CHEMBL188622 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442225 Ki = 34.0 nM 7.47
CHEMBL184407 Ki = 66.0 nM 7.18
CHEMBL186247 Ki = 89.0 nM 7.05
CHEMBL188622 Ki = 230.0 nM 6.64