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

CHEMBL2182411

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

Binding
Displacement of [3H]nicotine human alpha4beta2 nAChR in SH-EP1 cell membranes
ChEMBL ↗
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-EP1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of (2S,3R)-N-[2-(pyridin-3-ylmethyl)-1-azabicyclo[2.2.2]oct-3-yl]benzo[b]furan-2-carboxamide (TC-5619), a selective α7 nicotinic acetylcholine receptor agonist, for the treatment of cognitive disorders.
Mazurov AA, Kombo DC, Hauser TA, Miao L, Dull G, Genus JF, Fedorov NB, Benson L, Sidach S, Xiao Y, Hammond PS, James JW, Miller CH, Yohannes D.
J Med Chem (2012) 55 : 9793 -9809
PubMed 23126648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 71 6.10 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 8.70
CHEMBL105374 — — 1 8.54
CHEMBL1789658 — — 1 7.50
CHEMBL2179857 — — 1 6.85
CHEMBL194082 — — 1 6.80
CHEMBL2179862 — — 1 6.70
CHEMBL2179874 — — 1 6.70
CHEMBL2179853 — — 1 6.70
CHEMBL2179843 — — 1 6.52
CHEMBL2180257 — — 1 6.48
CHEMBL2179872 — — 1 6.40
CHEMBL2180250 — — 1 6.40
CHEMBL2179856 — — 1 6.40
CHEMBL2179881 — — 1 6.30
CHEMBL2179866 — — 1 6.30
CHEMBL2179858 — — 1 6.30
CHEMBL2179841 — — 1 6.30
CHEMBL2179852 — — 1 6.30
CHEMBL2179860 — — 1 6.30
CHEMBL2179849 — — 1 6.22
CHEMBL2179859 — — 1 6.22
CHEMBL2179878 — — 1 6.22
CHEMBL2180251 — — 1 6.21
CHEMBL2179839 — — 1 6.16
CHEMBL2180253 — — 1 6.13
CHEMBL2180260 — — 1 6.12
CHEMBL2179882 — — 1 6.08
CHEMBL2179871 — — 1 6.05
CHEMBL2179850 — — 1 6.05
CHEMBL2179838 — — 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 2.0 nM 8.70
CHEMBL105374 — Ki = 2.9 nM 8.54
CHEMBL1789658 — Ki = 32.0 nM 7.50
CHEMBL2179857 — Ki = 140.0 nM 6.85
CHEMBL194082 — Ki = 157.0 nM 6.80
CHEMBL2179862 — Ki = 200.0 nM 6.70
CHEMBL2179874 — Ki = 200.0 nM 6.70
CHEMBL2179853 — Ki = 200.0 nM 6.70
CHEMBL2179843 — Ki = 300.0 nM 6.52
CHEMBL2180257 — Ki = 330.0 nM 6.48
CHEMBL2179872 — Ki = 400.0 nM 6.40
CHEMBL2180250 — Ki = 400.0 nM 6.40
CHEMBL2179856 — Ki = 400.0 nM 6.40
CHEMBL2179852 — Ki = 500.0 nM 6.30
CHEMBL2179866 — Ki = 500.0 nM 6.30
CHEMBL2179858 — Ki = 500.0 nM 6.30
CHEMBL2179841 — Ki = 500.0 nM 6.30
CHEMBL2179881 — Ki = 500.0 nM 6.30
CHEMBL2179860 — Ki = 500.0 nM 6.30
CHEMBL2179849 — Ki = 600.0 nM 6.22
CHEMBL2179859 — Ki = 600.0 nM 6.22
CHEMBL2179878 — Ki = 600.0 nM 6.22
CHEMBL2180251 — Ki = 620.0 nM 6.21
CHEMBL2179839 — Ki = 700.0 nM 6.16
CHEMBL2180253 — Ki = 740.0 nM 6.13
CHEMBL2180260 — Ki = 760.0 nM 6.12
CHEMBL2179882 — Ki = 830.0 nM 6.08
CHEMBL2179871 — Ki = 900.0 nM 6.05
CHEMBL2179850 — Ki = 900.0 nM 6.05
CHEMBL2179838 — Ki = 900.0 nM 6.05
CHEMBL2179875 — Ki = 900.0 nM 6.05
CHEMBL2179844 — Ki = 900.0 nM 6.05
CHEMBL1258005 — Ki = 900.0 nM 6.05
CHEMBL2180259 — Ki = 980.0 nM 6.01
CHEMBL2179873 — Ki = 1000.0 nM 6.00
CHEMBL2179879 — Ki = 1000.0 nM 6.00
CHEMBL2180258 — Ki = 1000.0 nM 6.00
CHEMBL2180256 — Ki = 1100.0 nM 5.96
CHEMBL2179846 — Ki = 1100.0 nM 5.96
CHEMBL2179848 — Ki = 1200.0 nM 5.92
CHEMBL2179840 — Ki = 1200.0 nM 5.92
CHEMBL2180265 — Ki = 1200.0 nM 5.92
CHEMBL2179880 — Ki = 1200.0 nM 5.92
CHEMBL2179837 — Ki = 1300.0 nM 5.89
CHEMBL2180261 — Ki = 1300.0 nM 5.89
CHEMBL2180255 — Ki = 1300.0 nM 5.89
CHEMBL2180254 — Ki = 1300.0 nM 5.89
CHEMBL2151441 — Ki = 1300.0 nM 5.89
CHEMBL2179877 — Ki = 1300.0 nM 5.89
CHEMBL2179864 — Ki = 1400.0 nM 5.85