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Assay Detail

CHEMBL1833711

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

Functional
Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.
Baker JG, Adams LA, Salchow K, Mistry SN, Middleton RJ, Hill SJ, Kellam B.
J Med Chem (2011) 54 : 6874 -6887
PubMed 21870877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 17 9.00 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27 PROPRANOLOL 4.0 1 9.62
CHEMBL1830486 1 9.56
CHEMBL1830491 1 9.53
CHEMBL266195 ALPRENOLOL 2.0 1 9.53
CHEMBL1830485 1 9.37
CHEMBL1830618 1 9.37
CHEMBL1830492 1 9.36
CHEMBL1830619 1 9.21
CHEMBL500 PINDOLOL 4.0 1 9.18
CHEMBL1830489 1 9.13
CHEMBL1830617 1 8.80
CHEMBL1830487 1 8.76
CHEMBL1830493 1 8.74
CHEMBL1830490 1 8.60
CHEMBL1830488 1 8.59
CHEMBL1830621 1 8.14
CHEMBL1830620 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27 PROPRANOLOL Kd = 0.2399 nM 9.62
CHEMBL1830486 Kd = 0.2754 nM 9.56
CHEMBL1830491 Kd = 0.2951 nM 9.53
CHEMBL266195 ALPRENOLOL Kd = 0.2951 nM 9.53
CHEMBL1830485 Kd = 0.4266 nM 9.37
CHEMBL1830618 Kd = 0.4266 nM 9.37
CHEMBL1830492 Kd = 0.4365 nM 9.36
CHEMBL1830619 Kd = 0.6166 nM 9.21
CHEMBL500 PINDOLOL Kd = 0.6607 nM 9.18
CHEMBL1830489 Kd = 0.7413 nM 9.13
CHEMBL1830617 Kd = 1.585 nM 8.80
CHEMBL1830487 Kd = 1.738 nM 8.76
CHEMBL1830493 Kd = 1.82 nM 8.74
CHEMBL1830490 Kd = 2.512 nM 8.60
CHEMBL1830488 Kd = 2.57 nM 8.59
CHEMBL1830621 Kd = 7.244 nM 8.14
CHEMBL1830620 Kd = 30.2 nM 7.52