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Assay Detail

CHEMBL650854

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

Binding
Binding affinity for human Beta-2 adrenergic receptor expressed in CHO cells by radioligand competition binding assays using [125I]iodocyanopindolol (ICYP)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Iodinated analogs of trimetoquinol as highly potent and selective beta 2-adrenoceptor ligands.
De Los Angeles JE, Nikulin VI, Shams G, Konkar AA, Mehta R, Feller DR, Miller DD.
J Med Chem (1996) 39 : 3701 -3711
PubMed 8809159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.14 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122757 1 9.52
CHEMBL120278 1 8.82
CHEMBL123596 1 8.81
CHEMBL121704 1 8.70
CHEMBL308351 1 8.69
CHEMBL122990 1 8.19
CHEMBL332964 1 8.11
CHEMBL122992 1 8.06
CHEMBL121964 1 7.93
CHEMBL174984 TRETOQUINOL 2.0 1 7.36
CHEMBL333438 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122757 Ki = 0.302 nM 9.52
CHEMBL120278 Ki = 1.514 nM 8.82
CHEMBL123596 Ki = 1.549 nM 8.81
CHEMBL121704 Ki = 1.995 nM 8.70
CHEMBL308351 Ki = 2.042 nM 8.69
CHEMBL122990 Ki = 6.457 nM 8.19
CHEMBL332964 Ki = 7.762 nM 8.11
CHEMBL122992 Ki = 8.71 nM 8.06
CHEMBL121964 Ki = 11.75 nM 7.93
CHEMBL174984 TRETOQUINOL Ki = 43.65 nM 7.36
CHEMBL333438 Ki = 4365.16 nM 5.36