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Assay Detail

CHEMBL3614296

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

Binding
Displacement of [3H]prazosin from adrenergic alpha1 receptor in porcine cerebral cortex homogenates by radioligand competition binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

1,4-Disubstituted aromatic piperazines with high 5-HT2A/D2 selectivity: Quantitative structure-selectivity investigations, docking, synthesis and biological evaluation.
Möller D, Salama I, Kling RC, Hübner H, Gmeiner P.
Bioorg Med Chem (2015) 23 : 6195 -6209
PubMed 26299826 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.80 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3613877 1 9.64
CHEMBL3613878 1 9.41
CHEMBL3613876 1 8.92
CHEMBL3613873 1 8.82
CHEMBL3613874 1 8.59
CHEMBL3613880 1 8.48
CHEMBL3613879 1 8.44
CHEMBL3613875 1 8.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3613877 Ki = 0.23 nM 9.64
CHEMBL3613878 Ki = 0.39 nM 9.41
CHEMBL3613876 Ki = 1.2 nM 8.92
CHEMBL3613873 Ki = 1.5 nM 8.82
CHEMBL3613874 Ki = 2.6 nM 8.59
CHEMBL3613880 Ki = 3.3 nM 8.48
CHEMBL3613879 Ki = 3.6 nM 8.44
CHEMBL3613875 Ki = 8.4 nM 8.08