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Assay Detail

CHEMBL641229

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

Binding
In vitro binding affinity against cloned human alpha-1B-adrenoceptor receptors expressed in rat-1 fibroblasts
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Alpha(1)-adrenoceptor activation: a comparison of 4-(anilinomethyl)imidazoles and 4-(phenoxymethyl)imidazoles to related 2-imidazolines.
Hodson SJ, Bigham EC, Garrison DT, Gobel MJ, Irving PE, Liacos JA, Navas F, Saussy DL, Sherman BW, Speake JD, Bishop MJ.
Bioorg Med Chem Lett (2002) 12 : 3449 -3452
PubMed 12419381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.81 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117248 1 6.66
CHEMBL118055 1 6.05
CHEMBL318544 1 5.77
CHEMBL13789 1 5.62
CHEMBL325745 1 5.52
CHEMBL116700 1 5.23
CHEMBL117914 1 -
CHEMBL326837 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117248 IC50 = 218.78 nM 6.66
CHEMBL118055 IC50 = 891.25 nM 6.05
CHEMBL318544 IC50 = 1698.24 nM 5.77
CHEMBL13789 IC50 = 2398.83 nM 5.62
CHEMBL325745 IC50 = 3019.95 nM 5.52
CHEMBL116700 IC50 = 5888.44 nM 5.23
CHEMBL117914 IC50 < 30199.52 nM -
CHEMBL326837 IC50 < 30199.52 nM -