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Assay Detail

CHEMBL974466

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

Binding
Displacement of [3H]RX821002 from alpha2 adrenoceptor in human prefrontal cortex neural membrane
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Prefrontal cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel synthesis and pharmacological evaluation as alpha2-adrenoceptor ligands of O-phenylisouronium salts.
Goonan A, Kahvedzić A, Rodriguez F, Nagle PS, McCabe T, Rozas I, Erdozain AM, Meana JJ, Callado LF, Callado LF.
Bioorg Med Chem (2008) 16 : 8210 -8217
PubMed 18678494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.88 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10332 1 9.04
CHEMBL134 CLONIDINE 4.0 1 7.68
CHEMBL10316 IDAZOXAN 3.0 1 7.29
CHEMBL451179 1 7.11
CHEMBL453692 1 5.40
CHEMBL447688 1 5.35
CHEMBL452568 1 5.27
CHEMBL500626 1 5.10
CHEMBL450475 1 5.09
CHEMBL453859 1 4.98
CHEMBL453236 1 4.94
CHEMBL525985 1 4.72
CHEMBL453860 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10332 Ki = 0.912 nM 9.04
CHEMBL134 CLONIDINE Ki = 20.89 nM 7.68
CHEMBL10316 IDAZOXAN Ki = 51.29 nM 7.29
CHEMBL451179 Ki = 77.62 nM 7.11
CHEMBL453692 Ki = 3981.07 nM 5.40
CHEMBL447688 Ki = 4466.84 nM 5.35
CHEMBL452568 Ki = 5370.32 nM 5.27
CHEMBL500626 Ki = 7943.28 nM 5.10
CHEMBL450475 Ki = 8128.31 nM 5.09
CHEMBL453859 Ki = 10471.29 nM 4.98
CHEMBL453236 Ki = 11481.54 nM 4.94
CHEMBL525985 Ki = 19054.61 nM 4.72
CHEMBL453860 Ki = 32359.37 nM 4.49