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Assay Detail

CHEMBL652502

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Binding
Tested for binding affinity against cloned human beta-1 adrenergic receptor from CHO cells using [125I]iodocyanopindolol as the radioligand.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Potent, selective benzenesulfonamide agonists of the human beta 3 adrenergic receptor.
Weber AE, Mathvink RJ, Perkins L, Hutchins JE, Candelore MR, Tota L, Strader CD, Wyvratt MJ, Fisher MH.
Bioorg Med Chem Lett (1998) 8 : 1101 -1106
PubMed 9871716 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.17 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12686 1 6.85
CHEMBL12718 1 6.82
CHEMBL12769 1 6.30
CHEMBL12813 1 6.00
CHEMBL12450 1 6.00
CHEMBL13278 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12686 IC50 = 140.0 nM 6.85
CHEMBL12718 IC50 = 150.0 nM 6.82
CHEMBL12769 IC50 = 500.0 nM 6.30
CHEMBL12813 IC50 = 1000.0 nM 6.00
CHEMBL12450 IC50 = 1000.0 nM 6.00
CHEMBL13278 IC50 = 9000.0 nM 5.05