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Assay Detail

CHEMBL858094

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

Functional
Agonist potency at Alpha-2A stably expressed in CHO cells.
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Hodson SJ, Bishop MJ, Speake JD, Navas F, Garrison DT, Bigham EC, Saussy DL, Liacos JA, Irving PE, Gobel MJ, Sherman BW.
J Med Chem (2002) 45 : 2229 -2239
PubMed 12014961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.11 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL762 OXYMETAZOLINE 4.0 1 8.48
CHEMBL70751 1 8.20
CHEMBL72768 1 7.60
CHEMBL72441 1 7.60
CHEMBL70691 2 6.70
CHEMBL306792 1 6.50
CHEMBL71001 2 5.48
CHEMBL70740 1 -
CHEMBL74114 1 -
CHEMBL544290 1 -
CHEMBL70563 1 -
CHEMBL302698 1 -
CHEMBL72724 1 -
CHEMBL71479 1 -
CHEMBL72958 NS-49 1 -
CHEMBL70634 1 -
CHEMBL74467 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL762 OXYMETAZOLINE EC50 = 3.311 nM 8.48
CHEMBL70751 EC50 = 6.31 nM 8.20
CHEMBL72768 EC50 = 25.12 nM 7.60
CHEMBL72441 EC50 = 25.12 nM 7.60
CHEMBL70691 EC50 = 199.53 nM 6.70
CHEMBL306792 EC50 = 316.23 nM 6.50
CHEMBL70691 EC50 = 446.68 nM 6.35
CHEMBL71001 EC50 = 3311.31 nM 5.48
CHEMBL70740 EC50 < 10000.0 nM -
CHEMBL74114 EC50 < 10000.0 nM -
CHEMBL544290 EC50 < 10000.0 nM -
CHEMBL70563 EC50 < 10000.0 nM -
CHEMBL302698 EC50 < 10000.0 nM -
CHEMBL71001 EC50 < 10000.0 nM -
CHEMBL72724 EC50 < 10000.0 nM -
CHEMBL71479 EC50 < 10000.0 nM -
CHEMBL72958 NS-49 EC50 < 10000.0 nM -
CHEMBL70634 EC50 < 10000.0 nM -
CHEMBL74467 EC50 < 10000.0 nM -