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Assay Detail

CHEMBL5136914

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

Binding
Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR expressed in SH-SY5Y cells membrane assessed as inhibition constant preincubated for 5 mins followed by overnight incubation with [125I]alpha-bungarotoxin by beta liquid scintilation analysis
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
Bavo F, Pallavicini M, Pucci S, Appiani R, Giraudo A, Eaton B, Lucero L, Gotti C, Moretti M, Whiteaker P, Bolchi C.
J Med Chem (2022) 65 : 10079 -10097
PubMed 35834819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 6.43 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178473 1 7.64
CHEMBL5192210 1 7.47
CHEMBL5177606 1 7.43
CHEMBL5202770 1 7.23
CHEMBL5201239 1 7.14
CHEMBL5176690 1 7.10
CHEMBL5190813 1 7.03
CHEMBL1257065 STILONIUM IODIDE 2.0 1 6.98
CHEMBL5200914 1 6.96
CHEMBL5174508 1 6.95
CHEMBL5197631 1 6.93
CHEMBL5176101 1 6.79
CHEMBL5176544 1 6.65
CHEMBL5182114 1 6.61
CHEMBL5193899 1 6.59
CHEMBL5170445 1 6.55
CHEMBL5191958 1 6.51
CHEMBL5193143 1 6.25
CHEMBL5171118 1 6.21
CHEMBL5181363 1 6.20
CHEMBL5182514 1 5.95
CHEMBL5173112 1 5.80
CHEMBL5195695 1 5.61
CHEMBL5186396 1 5.48
CHEMBL5184266 1 5.41
CHEMBL5176875 1 5.23
CHEMBL5205894 1 5.00
CHEMBL5208202 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178473 Ki = 23.0 nM 7.64
CHEMBL5192210 Ki = 34.0 nM 7.47
CHEMBL5177606 Ki = 37.0 nM 7.43
CHEMBL5202770 Ki = 59.0 nM 7.23
CHEMBL5201239 Ki = 73.0 nM 7.14
CHEMBL5176690 Ki = 79.0 nM 7.10
CHEMBL5190813 Ki = 94.0 nM 7.03
CHEMBL1257065 STILONIUM IODIDE Ki = 104.0 nM 6.98
CHEMBL5200914 Ki = 110.0 nM 6.96
CHEMBL5174508 Ki = 112.0 nM 6.95
CHEMBL5197631 Ki = 117.0 nM 6.93
CHEMBL5176101 Ki = 163.0 nM 6.79
CHEMBL5176544 Ki = 222.0 nM 6.65
CHEMBL5182114 Ki = 248.0 nM 6.61
CHEMBL5193899 Ki = 259.0 nM 6.59
CHEMBL5170445 Ki = 284.0 nM 6.55
CHEMBL5191958 Ki = 306.0 nM 6.51
CHEMBL5193143 Ki = 567.0 nM 6.25
CHEMBL5171118 Ki = 613.0 nM 6.21
CHEMBL5181363 Ki = 635.0 nM 6.20
CHEMBL5182514 Ki = 1123.0 nM 5.95
CHEMBL5173112 Ki = 1600.0 nM 5.80
CHEMBL5195695 Ki = 2430.0 nM 5.61
CHEMBL5186396 Ki = 3300.0 nM 5.48
CHEMBL5184266 Ki = 3900.0 nM 5.41
CHEMBL5176875 Ki = 5900.0 nM 5.23
CHEMBL5205894 Ki = 10000.0 nM 5.00
CHEMBL5208202 Ki = 50000.0 nM 4.30