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Assay Detail

CHEMBL748020

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

Binding
Binding affinity against Nicotinic Acetylcholine Receptor was determined by measuring the displacement of [3H]cytisine from a preparation of whole rat brain.
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor (CHEMBL2094110)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.
Abreo MA, Lin NH, Garvey DS, Gunn DE, Hettinger AM, Wasicak JT, Pavlik PA, Martin YC, Donnelly-roberts DL, Anderson DJ, Sullivan JP, Williams M, Arneric SP, Holladay MW.
J Med Chem (1996) 39 : 817 -825
PubMed 8632405 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 9.49 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.37
CHEMBL262769 1 10.30
CHEMBL59986 1 10.28
CHEMBL440195 1 9.85
CHEMBL84149 2 9.82
CHEMBL293435 1 9.35
CHEMBL3 NICOTINE 4.0 1 9.00
CHEMBL168780 1 8.46
CHEMBL354602 1 7.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.043 nM 10.37
CHEMBL262769 Ki = 0.05 nM 10.30
CHEMBL59986 Ki = 0.052 nM 10.28
CHEMBL440195 Ki = 0.14 nM 9.85
CHEMBL84149 Ki = 0.15 nM 9.82
CHEMBL84149 Ki = 0.16 nM 9.80
CHEMBL293435 Ki = 0.45 nM 9.35
CHEMBL3 NICOTINE Ki = 1.0 nM 9.00
CHEMBL168780 Ki = 3.5 nM 8.46
CHEMBL354602 Ki = 19.7 nM 7.71