Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1028494

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

Binding
Displacement of [125I]alpha-bungarotoxin from alpha7 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
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, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes.
Tasso B, Canu Boido C, Terranova E, Gotti C, Riganti L, Clementi F, Artali R, Bombieri G, Meneghetti F, Sparatore F.
J Med Chem (2009) 52 : 4345 -4357
PubMed 19548687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 5.41 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497939 CYTISINICLINE 3.0 1 6.48
CHEMBL502295 1 6.36
CHEMBL502030 1 6.26
CHEMBL190851 1 5.91
CHEMBL502029 1 5.65
CHEMBL483804 1 5.44
CHEMBL525735 1 5.38
CHEMBL500426 1 4.89
CHEMBL497946 1 4.60
CHEMBL519673 1 4.40
CHEMBL524813 1 4.10
CHEMBL497940 1 -
CHEMBL522410 1 -
CHEMBL498277 1 -
CHEMBL499635 1 -
CHEMBL508190 1 -
CHEMBL525734 1 -
CHEMBL502374 1 -
CHEMBL526340 1 -
CHEMBL442613 1 -
CHEMBL498810 1 -
CHEMBL521152 1 -
CHEMBL483803 1 -
CHEMBL508431 1 -
CHEMBL520478 1 -
CHEMBL484148 1 -
CHEMBL499636 1 -
CHEMBL526554 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497939 CYTISINICLINE Ki = 331.0 nM 6.48
CHEMBL502295 Ki = 433.0 nM 6.36
CHEMBL502030 Ki = 550.0 nM 6.26
CHEMBL190851 Ki = 1240.0 nM 5.91
CHEMBL502029 Ki = 2250.0 nM 5.65
CHEMBL483804 Ki = 3600.0 nM 5.44
CHEMBL525735 Ki = 4200.0 nM 5.38
CHEMBL500426 Ki = 13000.0 nM 4.89
CHEMBL497946 Ki = 25000.0 nM 4.60
CHEMBL519673 Ki = 39700.0 nM 4.40
CHEMBL524813 Ki = 78700.0 nM 4.10
CHEMBL497940 Ki > 100000.0 nM -
CHEMBL522410 Ki > 100000.0 nM -
CHEMBL498277 Ki > 100000.0 nM -
CHEMBL499635 Ki > 100000.0 nM -
CHEMBL508190 Ki > 50000.0 nM -
CHEMBL525734 Ki > 50000.0 nM -
CHEMBL502374 Ki > 50000.0 nM -
CHEMBL526340 Ki > 50000.0 nM -
CHEMBL442613 Ki > 50000.0 nM -
CHEMBL498810 Ki > 50000.0 nM -
CHEMBL521152 Ki > 50000.0 nM -
CHEMBL483803 Ki > 50000.0 nM -
CHEMBL508431 Ki > 50000.0 nM -
CHEMBL520478 Ki > 50000.0 nM -
CHEMBL484148 Ki > 50000.0 nM -
CHEMBL499636 Ki - -
CHEMBL526554 Ki - -