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Assay Detail

CHEMBL828969

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

Binding
Inhibition of [3H]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha-1-beta-1-delta-gamma of electroplax
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Coe JW, Vetelino MG, Bashore CG, Wirtz MC, Brooks PR, Arnold EP, Lebel LA, Fox CB, Sands SB, Davis TI, Schulz DW, Rollema H, Tingley FD, O'Neill BT.
Bioorg Med Chem Lett (2005) 15 : 2974 -2979
PubMed 15908213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.83 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL497939 CYTISINICLINE 3.0 1 6.60
CHEMBL191174 1 6.47
CHEMBL365965 1 5.52
CHEMBL373359 1 5.35
CHEMBL3 NICOTINE 4.0 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL497939 CYTISINICLINE Ki = 250.0 nM 6.60
CHEMBL191174 Ki = 340.0 nM 6.47
CHEMBL365965 Ki = 3000.0 nM 5.52
CHEMBL373359 Ki = 4500.0 nM 5.35
CHEMBL3 NICOTINE Ki = 6300.0 nM 5.20