Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5547468

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

Functional
Agonist activity at human recombinant adrenergic alpha-2A receptor expressed in CHO-K1 cells co-transfected with 22F-Glosensor assessed as inhibition of cAMP production measured after 30 mins incubation by Microbeta2Micro-plate counter analysis
4
Total Activities
2
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

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT<sub>2</sub> Receptor Agonist.
Varty GB, Canal CE, Mueller TA, Hartsel JA, Tyagi R, Avery K, Morgan ME, Reichelt AC, Pathare P, Stang E, Palfreyman MG, Nivorozhkin A.
J Med Chem (2024) 67 : 6144 -6188
PubMed 38593423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.21 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134 CLONIDINE 4.0 2 9.54
CHEMBL5566821 2 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134 CLONIDINE EC50 = 0.29 nM 9.54
CHEMBL134 CLONIDINE EC50 = 0.3162 nM 9.50
CHEMBL5566821 EC50 = 126.0 nM 6.90
CHEMBL5566821 EC50 = 125.89 nM 6.90