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Assay Detail

CHEMBL2445017

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

Binding
Binding affinity to N-terminal FLAG-tagged C-terminal His-10-tagged human beta2 adrenoceptor expressed in insect Sf9 cells by surface plasmon resonance analysis in presence of maltose neopentyl glycol
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
Aristotelous T, Ahn S, Shukla AK, Gawron S, Sassano MF, Kahsai AW, Wingler LM, Zhu X, Tripathi-Shukla P, Huang XP, Riley J, Besnard J, Read KD, Roth BL, Gilbert IH, Hopkins AL, Lefkowitz RJ, Navratilova I.
ACS Med Chem Lett (2013) 4 : 1005 -1010
PubMed 24454993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 6.01 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441619 1 7.41
CHEMBL2335165 1 7.14
CHEMBL236696 1 7.12
CHEMBL1892158 1 7.08
CHEMBL2441621 1 6.46
CHEMBL2441616 1 5.75
CHEMBL2441615 1 5.10
CHEMBL2441617 1 4.17
CHEMBL339069 1 3.85
CHEMBL2441618 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441619 Kd = 39.0 nM 7.41
CHEMBL2335165 Kd = 72.5 nM 7.14
CHEMBL236696 Kd = 76.5 nM 7.12
CHEMBL1892158 Kd = 84.2 nM 7.08
CHEMBL2441621 Kd = 348.3 nM 6.46
CHEMBL2441616 Kd = 1800.0 nM 5.75
CHEMBL2441615 Kd = 8000.0 nM 5.10
CHEMBL2441617 Kd = 67100.0 nM 4.17
CHEMBL339069 Kd = 141600.0 nM 3.85
CHEMBL2441618 Kd - -