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Assay Detail

CHEMBL4119595

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

ADMET
Displacement of [3H]prazosin from alpha1 adrenoceptor in C57BL/6 mouse hippocampal homogenates after 40 mins by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Mus musculus
Confidence 5 — Multiple protein complex / RNA
Curated By Intermediate

Target

Alpha-1 adrenergic receptor (CHEMBL2111452)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Evaluation of the antidepressant therapeutic potential of isocyanine and pseudoisocyanine analogues of the organic cation decynium-22.
Krause-Heuer AM, Fraser-Spears R, Dobrowolski JC, Ashford ME, Wyatt NA, Roberts MP, Gould GG, Cheah WC, Ng CKL, Bhadbhade M, Zhang B, Greguric I, Wheate NJ, Kumar N, Koek W, Callaghan PD, Daws LC, Fraser BH.
Eur J Med Chem (2017) 137 : 476 -487
PubMed 28624702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.80 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 8.74
CHEMBL4129927 1 7.22
CHEMBL4126353 1 6.46
CHEMBL4126498 1 6.24
CHEMBL4129778 1 6.15
CHEMBL4128701 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN IC50 = 1.8 nM 8.74
CHEMBL4129927 IC50 = 60.0 nM 7.22
CHEMBL4126353 IC50 = 348.0 nM 6.46
CHEMBL4126498 IC50 = 577.0 nM 6.24
CHEMBL4129778 IC50 = 711.0 nM 6.15
CHEMBL4128701 IC50 = 1066.0 nM 5.97