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Assay Detail

CHEMBL4397555

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

Binding
Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL3440)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Hybridization of β-Adrenergic Agonists and Antagonists Confers G Protein Bias.
Stanek M, Picard LP, Schmidt MF, Kaindl JM, Hübner H, Bouvier M, Weikert D, Gmeiner P.
J Med Chem (2019) 62 : 5111 -5131
PubMed 31042379 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.21 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL324665 CARAZOLOL 2.0 1 10.05
CHEMBL3799125 1 9.68
CHEMBL3798017 (R)-Carvedilol 1 8.47
CHEMBL4593181 1 8.19
CHEMBL4451135 1 8.18
CHEMBL4435895 1 7.92
CHEMBL1160694 1 7.85
CHEMBL4513932 1 7.62
CHEMBL3800303 1 7.07
CHEMBL3797876 1 6.80
CHEMBL1160723 LEVISOPRENALINE 2.0 1 6.66
CHEMBL4470694 1 6.51
CHEMBL4436343 1 6.48
CHEMBL4450756 1 6.47
CHEMBL1263 SALMETEROL 4.0 1 6.26
CHEMBL4439238 1 6.07
CHEMBL4437939 1 5.92
CHEMBL4459109 1 5.62
CHEMBL4515498 1 5.13
CHEMBL4525632 1 -
CHEMBL4561683 1 -
CHEMBL4518727 1 -
CHEMBL4459541 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL324665 CARAZOLOL Ki = 0.09 nM 10.05
CHEMBL3799125 Ki = 0.21 nM 9.68
CHEMBL3798017 (R)-Carvedilol Ki = 3.4 nM 8.47
CHEMBL4593181 Ki = 6.5 nM 8.19
CHEMBL4451135 Ki = 6.6 nM 8.18
CHEMBL4435895 Ki = 12.0 nM 7.92
CHEMBL1160694 Ki = 14.0 nM 7.85
CHEMBL4513932 Ki = 24.0 nM 7.62
CHEMBL3800303 Ki = 85.0 nM 7.07
CHEMBL3797876 Ki = 160.0 nM 6.80
CHEMBL1160723 LEVISOPRENALINE Ki = 220.0 nM 6.66
CHEMBL4470694 Ki = 310.0 nM 6.51
CHEMBL4436343 Ki = 330.0 nM 6.48
CHEMBL4450756 Ki = 340.0 nM 6.47
CHEMBL1263 SALMETEROL Ki = 550.0 nM 6.26
CHEMBL4439238 Ki = 860.0 nM 6.07
CHEMBL4437939 Ki = 1200.0 nM 5.92
CHEMBL4459109 Ki = 2400.0 nM 5.62
CHEMBL4515498 Ki = 7400.0 nM 5.13
CHEMBL4525632 Ki > 10000.0 nM -
CHEMBL4561683 Ki > 10000.0 nM -
CHEMBL4518727 Ki > 10000.0 nM -
CHEMBL4459541 Ki > 10000.0 nM -