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Assay Detail

CHEMBL1639409

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

Binding
Displacement of [125I]-alpha-Bungarotoxin from alpha7 nAChR rat cortical membranes by gamma counting
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes.
Dallanoce C, Magrone P, Matera C, Lo Presti L, De Amici M, Riganti L, Clementi F, Gotti C, De Micheli C.
Eur J Med Chem (2010) 45 : 5594 -5601
PubMed 20932609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.18 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630288 1 6.36
CHEMBL3 NICOTINE 4.0 1 6.33
CHEMBL274525 ABT-418 1 5.92
CHEMBL1630294 1 5.54
CHEMBL1630293 1 4.95
CHEMBL1630290 1 4.46
CHEMBL1630287 1 4.40
CHEMBL1630291 1 4.37
CHEMBL186295 1 4.31
CHEMBL1630289 1 -
CHEMBL1630292 1 -
CHEMBL1630295 1 -
CHEMBL185124 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630288 Ki = 440.0 nM 6.36
CHEMBL3 NICOTINE Ki = 469.0 nM 6.33
CHEMBL274525 ABT-418 Ki = 1200.0 nM 5.92
CHEMBL1630294 Ki = 2900.0 nM 5.54
CHEMBL1630293 Ki = 11300.0 nM 4.95
CHEMBL1630290 Ki = 35000.0 nM 4.46
CHEMBL1630287 Ki = 40000.0 nM 4.40
CHEMBL1630291 Ki = 43000.0 nM 4.37
CHEMBL186295 Ki = 49000.0 nM 4.31
CHEMBL1630289 Ki = 325000.0 nM -
CHEMBL1630292 Ki = 277000.0 nM -
CHEMBL1630295 Ki > 500000.0 nM -
CHEMBL185124 Ki > 50000.0 nM -