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Assay Detail

CHEMBL3100638

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

Binding
Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β₂-adrenergic receptor.
Plazinska A, Pajak K, Rutkowska E, Jimenez L, Kozocas J, Koolpe G, Tanga M, Toll L, Wainer IW, Jozwiak K.
Bioorg Med Chem (2014) 22 : 234 -246
PubMed 24326276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.31 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 9.34
CHEMBL434 ISOPROTERENOL 4.0 1 6.72
CHEMBL3099659 1 6.38
CHEMBL3099657 1 5.57
CHEMBL3099663 1 5.12
CHEMBL3099660 1 4.70
CHEMBL3099658 1 -
CHEMBL3099664 1 -
CHEMBL3099662 1 -
CHEMBL3099661 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL Ki = 0.46 nM 9.34
CHEMBL434 ISOPROTERENOL Ki = 192.0 nM 6.72
CHEMBL3099659 Ki = 420.0 nM 6.38
CHEMBL3099657 Ki = 2670.0 nM 5.57
CHEMBL3099663 Ki = 7600.0 nM 5.12
CHEMBL3099660 Ki = 20100.0 nM 4.70
CHEMBL3099658 Ki > 100000.0 nM -
CHEMBL3099664 Ki > 100000.0 nM -
CHEMBL3099662 Ki > 100000.0 nM -
CHEMBL3099661 Ki > 100000.0 nM -