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Assay Detail

CHEMBL652421

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

Binding
Ability to bind to human Beta-2 adrenergic receptor using membranes of stably transfected CHO cells
10
Total Activities
10
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

Carboxyl-promoted enhancement of selectivity for the 3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-3 binding selectivity
Sher PM, Mathur A, Fisher LG, Wu G, Skwish S, Michel IM, Seiler SM, Dickinson KE
Bioorg Med Chem Lett (1997) 7 : 1583 -1588
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.83 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38486 1 8.49
CHEMBL39596 1 6.95
CHEMBL38569 1 6.77
CHEMBL41113 1 6.58
CHEMBL284782 1 6.20
CHEMBL38538 1 5.65
CHEMBL290752 1 4.77
CHEMBL41948 1 4.40
CHEMBL40966 1 4.37
CHEMBL39334 1 4.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38486 Ki = 3.2 nM 8.49
CHEMBL39596 Ki = 112.0 nM 6.95
CHEMBL38569 Ki = 170.0 nM 6.77
CHEMBL41113 Ki = 260.0 nM 6.58
CHEMBL284782 Ki = 630.0 nM 6.20
CHEMBL38538 Ki = 2250.0 nM 5.65
CHEMBL290752 Ki = 17100.0 nM 4.77
CHEMBL41948 Ki = 39700.0 nM 4.40
CHEMBL40966 Ki = 42600.0 nM 4.37
CHEMBL39334 Ki = 73700.0 nM 4.13