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Assay Detail

CHEMBL5527118

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

Binding
Binding affinity to alpha2A adrenergic receptor (unknown origin) assessed as inhibition constant
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Natural Product-Inspired Dopamine Receptor Ligands.
Dorogan M, Namballa HK, Harding WW.
J Med Chem (2024) 67 : 12463 -12484
PubMed 39038276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.61 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 1 8.70
CHEMBL1621 PALIPERIDONE 4.0 1 7.96
CHEMBL493 BROMOCRIPTINE 4.0 1 7.58
CHEMBL531 PERGOLIDE 4.0 1 7.33
CHEMBL726 FLUPHENAZINE 4.0 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 2.0 nM 8.70
CHEMBL1621 PALIPERIDONE Ki = 11.0 nM 7.96
CHEMBL493 BROMOCRIPTINE Ki = 26.0 nM 7.58
CHEMBL531 PERGOLIDE Ki = 47.0 nM 7.33
CHEMBL726 FLUPHENAZINE Ki = 314.1 nM 6.50