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Assay Detail

CHEMBL5547464

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

Binding
Displacement of [3H]-rauwolscine from human recombinant adrenergic alpha-2A receptor expressed in CHO-K1 cells incubated for 60 mins by spectrophotometric analysis relative to control
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 6 7.76 8.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15245 YOHIMBINE 3.0 2 8.58
CHEMBL134 CLONIDINE 4.0 2 7.59
CHEMBL5566821 2 7.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15245 YOHIMBINE Ki = 2.63 nM 8.58
CHEMBL15245 YOHIMBINE Ki = 3.0 nM 8.52
CHEMBL134 CLONIDINE Ki = 25.7 nM 7.59
CHEMBL134 CLONIDINE Ki = 26.0 nM 7.58
CHEMBL5566821 Ki = 72.0 nM 7.14
CHEMBL5566821 Ki = 72.44 nM 7.14