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Assay Detail

CHEMBL2015334

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

Binding
Displacement of [3H](-)-CGP-12177 from adrenergic beta1 receptor by cell based assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Cardiac Imaging of (18)F-Ligands Selective for β1-Adrenoreceptors.
Radeke HS, Purohit A, Harris TD, Hanson K, Jones R, Hu C, Yalamanchili P, Hayes M, Yu M, Guaraldi M, Kagan M, Azure M, Cdebaca M, Robinson S, Casebier D.
ACS Med Chem Lett (2011) 2 : 650 -655
PubMed 24900360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 9.14 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011218 1 10.40
CHEMBL2011227 1 10.30
CHEMBL2011226 1 10.30
CHEMBL2011216 1 10.10
CHEMBL2011215 1 10.00
CHEMBL2011224 1 10.00
CHEMBL2011213 1 9.96
CHEMBL2011235 1 9.85
CHEMBL2011214 1 9.70
CHEMBL2011217 1 9.60
CHEMBL2011225 1 9.52
CHEMBL2011228 1 9.46
CHEMBL2011222 1 9.00
CHEMBL2011219 1 8.82
CHEMBL2011223 1 8.70
CHEMBL2011221 1 8.70
CHEMBL2011234 1 8.52
CHEMBL2011236 1 8.30
CHEMBL2011230 1 8.00
CHEMBL2011233 1 8.00
CHEMBL2011232 1 7.70
CHEMBL2011220 1 7.68
CHEMBL2011229 1 7.58
CHEMBL2011231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011218 IC50 = 0.04 nM 10.40
CHEMBL2011227 IC50 = 0.05 nM 10.30
CHEMBL2011226 IC50 = 0.05 nM 10.30
CHEMBL2011216 IC50 = 0.08 nM 10.10
CHEMBL2011215 IC50 = 0.1 nM 10.00
CHEMBL2011224 IC50 = 0.1 nM 10.00
CHEMBL2011213 IC50 = 0.11 nM 9.96
CHEMBL2011235 IC50 = 0.14 nM 9.85
CHEMBL2011214 IC50 = 0.2 nM 9.70
CHEMBL2011217 IC50 = 0.25 nM 9.60
CHEMBL2011225 IC50 = 0.3 nM 9.52
CHEMBL2011228 IC50 = 0.35 nM 9.46
CHEMBL2011222 IC50 = 1.0 nM 9.00
CHEMBL2011219 IC50 = 1.5 nM 8.82
CHEMBL2011223 IC50 = 2.0 nM 8.70
CHEMBL2011221 IC50 = 2.0 nM 8.70
CHEMBL2011234 IC50 = 3.0 nM 8.52
CHEMBL2011236 IC50 = 5.0 nM 8.30
CHEMBL2011230 IC50 = 10.0 nM 8.00
CHEMBL2011233 IC50 = 10.0 nM 8.00
CHEMBL2011232 IC50 = 20.0 nM 7.70
CHEMBL2011220 IC50 = 21.0 nM 7.68
CHEMBL2011229 IC50 = 26.0 nM 7.58
CHEMBL2011231 IC50 > 100.0 nM -