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Assay Detail

CHEMBL651231

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

Functional
Agonist potency at Alpha-1B adrenergic receptor expressed in rat-1 fibroblasts
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL232)
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 24 8.04 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72441 1 9.38
CHEMBL70751 1 9.30
CHEMBL72768 1 8.73
CHEMBL70691 1 8.44
CHEMBL72724 1 8.22
CHEMBL306792 1 8.22
CHEMBL540035 1 7.86
CHEMBL553276 1 7.21
CHEMBL70634 1 7.21
CHEMBL70692 1 7.07
CHEMBL71479 1 6.85
CHEMBL70740 1 -
CHEMBL74114 1 -
CHEMBL544290 1 -
CHEMBL74467 1 -
CHEMBL70973 1 -
CHEMBL72958 NS-49 1 -
CHEMBL71001 1 -
CHEMBL70326 1 -
CHEMBL762 OXYMETAZOLINE 4.0 1 -
CHEMBL542402 1 -
CHEMBL74071 1 -
CHEMBL419448 1 -
CHEMBL302698 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72441 EC50 = 0.4169 nM 9.38
CHEMBL70751 EC50 = 0.5012 nM 9.30
CHEMBL72768 EC50 = 1.862 nM 8.73
CHEMBL70691 EC50 = 3.631 nM 8.44
CHEMBL72724 EC50 = 6.026 nM 8.22
CHEMBL306792 EC50 = 6.026 nM 8.22
CHEMBL540035 EC50 = 13.8 nM 7.86
CHEMBL553276 EC50 = 61.66 nM 7.21
CHEMBL70634 EC50 = 61.66 nM 7.21
CHEMBL70692 EC50 = 85.11 nM 7.07
CHEMBL71479 EC50 = 141.25 nM 6.85
CHEMBL70740 EC50 < 100000.0 nM -
CHEMBL74114 EC50 < 100000.0 nM -
CHEMBL544290 EC50 < 100000.0 nM -
CHEMBL74467 EC50 < 100000.0 nM -
CHEMBL70973 EC50 < 100000.0 nM -
CHEMBL72958 NS-49 EC50 < 100000.0 nM -
CHEMBL71001 EC50 < 100000.0 nM -
CHEMBL70326 EC50 < 100000.0 nM -
CHEMBL762 OXYMETAZOLINE EC50 < 25118.86 nM -
CHEMBL542402 EC50 < 100000.0 nM -
CHEMBL74071 EC50 < 10000.0 nM -
CHEMBL419448 EC50 < 100000.0 nM -
CHEMBL302698 EC50 < 100000.0 nM -