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Assay Detail

CHEMBL4358956

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

Binding
Displacement of [3H]2-BFI from I2IR in Sprague-Dawley rat brain cortex incubated for 45 mins by liquid scintillation spectrometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease.
Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, de Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallàs M, Callado LF, Escolano C.
J Med Chem (2020) 63 : 3610 -3633
PubMed 32150414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.05 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10316 IDAZOXAN 3.0 1 7.17
CHEMBL4450506 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10316 IDAZOXAN Ki = 67.61 nM 7.17
CHEMBL4450506 Ki = 120.23 nM 6.92