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Assay Detail

CHEMBL649966

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

Binding
Beta-1 adrenergic receptor binding affinity in CHO cells expressing cloned human receptor in the presence of 125 I-iodocyanopindolol
22
Total Activities
22
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

3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE.
Bioorg Med Chem Lett (1998) 8 : 3087 -3092
PubMed 9873681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.00 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL104193 1 6.80
CHEMBL323113 1 6.01
CHEMBL321957 1 5.70
CHEMBL106746 1 5.70
CHEMBL104061 1 5.70
CHEMBL284782 1 5.30
CHEMBL104076 1 5.16
CHEMBL104127 1 5.16
CHEMBL57486 1 5.10
CHEMBL318165 1 5.10
CHEMBL318802 1 5.00
CHEMBL64697 1 5.00
CHEMBL105968 1 5.00
CHEMBL320138 1 5.00
CHEMBL104180 1 4.70
CHEMBL320228 1 4.52
CHEMBL104981 1 4.52
CHEMBL106487 1 4.22
CHEMBL104222 1 4.22
CHEMBL104377 1 4.00
CHEMBL104551 1 4.00
CHEMBL107681 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL104193 IC50 = 160.0 nM 6.80
CHEMBL323113 IC50 = 970.0 nM 6.01
CHEMBL321957 IC50 = 2000.0 nM 5.70
CHEMBL106746 IC50 = 2000.0 nM 5.70
CHEMBL104061 IC50 = 2000.0 nM 5.70
CHEMBL284782 IC50 = 5000.0 nM 5.30
CHEMBL104076 IC50 = 7000.0 nM 5.16
CHEMBL104127 IC50 = 7000.0 nM 5.16
CHEMBL57486 IC50 = 8000.0 nM 5.10
CHEMBL318165 IC50 = 8000.0 nM 5.10
CHEMBL318802 IC50 = 10000.0 nM 5.00
CHEMBL64697 IC50 = 10000.0 nM 5.00
CHEMBL105968 IC50 = 10000.0 nM 5.00
CHEMBL320138 IC50 = 10000.0 nM 5.00
CHEMBL104180 IC50 = 20000.0 nM 4.70
CHEMBL320228 IC50 = 30000.0 nM 4.52
CHEMBL104981 IC50 = 30000.0 nM 4.52
CHEMBL106487 IC50 = 60000.0 nM 4.22
CHEMBL104222 IC50 = 60000.0 nM 4.22
CHEMBL104377 IC50 = 100000.0 nM 4.00
CHEMBL104551 IC50 = 100000.0 nM 4.00
CHEMBL107681 IC50 = 100000.0 nM 4.00