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Assay Detail

CHEMBL5355529

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Functional
Agonist activity at human beta1-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
8
Total Activities
8
Compounds Tested
2
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-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational design, synthesis, and pharmacological evaluation of a cohort of novel beta-adrenergic receptors ligands enables an assessment of structure-activity relationships.
Tricomi J, Landini L, Nieddu V, Cavallaro U, Baker JG, Papakyriakou A, Richichi B.
Eur J Med Chem (2023) 246 : 114961 -114961
PubMed 36495629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.91 7.96
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32800 FENOTEROL 4.0 1 7.96
CHEMBL1326499 1 7.32
CHEMBL5427527 1 7.13
CHEMBL5430355 1 6.52
CHEMBL5397120 1 6.51
CHEMBL5415148 1 6.50
CHEMBL4238084 1 6.42
CHEMBL5410388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32800 FENOTEROL EC50 = 10.96 nM 7.96
CHEMBL1326499 EC50 = 47.86 nM 7.32
CHEMBL5427527 EC50 = 74.13 nM 7.13
CHEMBL5430355 EC50 = 302.0 nM 6.52
CHEMBL5397120 EC50 = 309.03 nM 6.51
CHEMBL5415148 EC50 = 316.23 nM 6.50
CHEMBL4238084 EC50 = 380.19 nM 6.42
CHEMBL5410388 pEC50 - -