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Assay Detail

CHEMBL643414

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

Functional
Agonist potency at Alpha-1D adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1D adrenergic receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL223)
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 22 7.97 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72441 1 9.04
CHEMBL70751 1 8.57
CHEMBL70691 1 8.30
CHEMBL306792 1 8.04
CHEMBL72768 1 7.66
CHEMBL70692 1 7.47
CHEMBL72724 1 7.36
CHEMBL540035 1 7.29
CHEMBL70740 1 -
CHEMBL74114 1 -
CHEMBL74467 1 -
CHEMBL70973 1 -
CHEMBL70634 1 -
CHEMBL72958 NS-49 1 -
CHEMBL553276 1 -
CHEMBL71479 1 -
CHEMBL71001 1 -
CHEMBL302698 1 -
CHEMBL74071 1 -
CHEMBL70563 1 -
CHEMBL762 OXYMETAZOLINE 4.0 1 -
CHEMBL419448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72441 EC50 = 0.912 nM 9.04
CHEMBL70751 EC50 = 2.692 nM 8.57
CHEMBL70691 EC50 = 5.012 nM 8.30
CHEMBL306792 EC50 = 9.12 nM 8.04
CHEMBL72768 EC50 = 21.88 nM 7.66
CHEMBL70692 EC50 = 33.88 nM 7.47
CHEMBL72724 EC50 = 43.65 nM 7.36
CHEMBL540035 EC50 = 51.29 nM 7.29
CHEMBL70740 EC50 < 100000.0 nM -
CHEMBL74114 EC50 < 100000.0 nM -
CHEMBL74467 EC50 < 100000.0 nM -
CHEMBL70973 EC50 < 100000.0 nM -
CHEMBL70634 EC50 < 100000.0 nM -
CHEMBL72958 NS-49 EC50 < 100000.0 nM -
CHEMBL553276 EC50 < 5011.87 nM -
CHEMBL71479 EC50 < 1995.26 nM -
CHEMBL71001 EC50 < 100000.0 nM -
CHEMBL302698 EC50 < 100000.0 nM -
CHEMBL74071 EC50 < 5011.87 nM -
CHEMBL70563 EC50 < 100000.0 nM -
CHEMBL762 OXYMETAZOLINE EC50 < 25118.86 nM -
CHEMBL419448 EC50 < 100000.0 nM -