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Assay Detail

CHEMBL5442698

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

Functional
GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HTLA
Category GPCR beta-arrestin recruitment assay
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

EUbOPEN Chemogenomics Library - GPCR Dose-Respose
EUbOPEN
(2024)
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.36 9.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2106195 DEXMEDETOMIDINE HYDROCHLORIDE 4.0 1 9.17
CHEMBL2062257 1 8.78
CHEMBL1200791 OXYMETAZOLINE HYDROCHLORIDE 4.0 1 8.48
CHEMBL1705 CLONIDINE HYDROCHLORIDE 4.0 1 8.28
CHEMBL679 EPINEPHRINE 4.0 1 8.25
CHEMBL1200494 GUANFACINE HYDROCHLORIDE 4.0 1 7.93
CHEMBL5087452 1 7.52
CHEMBL1200329 TIZANIDINE HYDROCHLORIDE 4.0 1 7.48
CHEMBL2261346 1 6.87
CHEMBL1256876 1 6.54
CHEMBL1201087 CABERGOLINE 4.0 1 6.54
CHEMBL520992 1 6.50
CHEMBL1215 PHENYLEPHRINE 4.0 1 6.32
CHEMBL1557 DOPAMINE HYDROCHLORIDE 4.0 1 5.94
CHEMBL3143955 1 5.75
CHEMBL505308 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2106195 DEXMEDETOMIDINE HYDROCHLORIDE EC50 = 0.6747 nM 9.17
CHEMBL2062257 EC50 = 1.666 nM 8.78
CHEMBL1200791 OXYMETAZOLINE HYDROCHLORIDE EC50 = 3.29 nM 8.48
CHEMBL1705 CLONIDINE HYDROCHLORIDE EC50 = 5.259 nM 8.28
CHEMBL679 EPINEPHRINE EC50 = 5.626 nM 8.25
CHEMBL1200494 GUANFACINE HYDROCHLORIDE EC50 = 11.77 nM 7.93
CHEMBL5087452 EC50 = 30.11 nM 7.52
CHEMBL1200329 TIZANIDINE HYDROCHLORIDE EC50 = 32.91 nM 7.48
CHEMBL2261346 EC50 = 134.67 nM 6.87
CHEMBL1256876 EC50 = 291.09 nM 6.54
CHEMBL1201087 CABERGOLINE EC50 = 285.43 nM 6.54
CHEMBL520992 EC50 = 319.98 nM 6.50
CHEMBL1215 PHENYLEPHRINE EC50 = 476.65 nM 6.32
CHEMBL1557 DOPAMINE HYDROCHLORIDE EC50 = 1144.73 nM 5.94
CHEMBL3143955 EC50 = 1762.4 nM 5.75
CHEMBL505308 EC50 > 10000.0 nM -