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Assay Detail

CHEMBL4817488

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

Binding
Displacement of 125I-cyanopindolol from human adrenergic beta2 receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β<sub>2</sub> agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Rancati F, Linney ID, Rizzi A, Delcanale M, Knight CK, Schmidt W, Pastore F, Riccardi B, Mileo V, Carnini C, Cesari N, Blackaby WP, Patacchini R, Carzaniga L.
Bioorg Med Chem Lett (2021) 41 : 127975 -127975
PubMed 33753262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 10.05 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4871517 1 10.90
CHEMBL4863525 1 10.80
CHEMBL4874819 1 10.60
CHEMBL4857743 1 10.40
CHEMBL4866806 1 10.30
CHEMBL4854418 1 10.00
CHEMBL4871702 1 10.00
CHEMBL4878138 1 9.80
CHEMBL4846536 1 9.70
CHEMBL4852629 1 9.70
CHEMBL4878395 1 9.60
CHEMBL4854091 1 9.60
CHEMBL4847910 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4871517 Ki = 0.01259 nM 10.90
CHEMBL4863525 Ki = 0.01585 nM 10.80
CHEMBL4874819 Ki = 0.02512 nM 10.60
CHEMBL4857743 Ki = 0.03981 nM 10.40
CHEMBL4866806 Ki = 0.05012 nM 10.30
CHEMBL4854418 Ki = 0.1 nM 10.00
CHEMBL4871702 Ki = 0.1 nM 10.00
CHEMBL4878138 Ki = 0.1585 nM 9.80
CHEMBL4846536 Ki = 0.1995 nM 9.70
CHEMBL4852629 Ki = 0.1995 nM 9.70
CHEMBL4878395 Ki = 0.2512 nM 9.60
CHEMBL4854091 Ki = 0.2512 nM 9.60
CHEMBL4847910 Ki = 0.5012 nM 9.30