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Assay Detail

CHEMBL748017

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

Binding
Displacement of [3H](-)-cytisine from rat brain nicotinic acetylcholine receptors (nAChR)
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and structure-activity relationships of 2-(R) and (S) pyrrolidine-modified analogs of the cholinergic channel activator, ABT-418
Lin N, He Y, Arneric SP, Sullivan JP
Bioorg Med Chem Lett (1995) 5 : 1141 -1146
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.32 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274525 ABT-418 1 8.52
CHEMBL268750 1 8.13
CHEMBL14743 1 7.72
CHEMBL274979 2 7.15
CHEMBL275173 1 6.81
CHEMBL14839 1 6.02
CHEMBL14554 1 5.77
CHEMBL15244 1 5.22
CHEMBL14537 1 5.18
CHEMBL2079554 1 5.09
CHEMBL15212 1 4.96
CHEMBL277559 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274525 ABT-418 Ki = 3.0 nM 8.52
CHEMBL268750 Ki = 7.4 nM 8.13
CHEMBL14743 Ki = 19.0 nM 7.72
CHEMBL274979 Ki = 71.0 nM 7.15
CHEMBL275173 Ki = 155.0 nM 6.81
CHEMBL274979 Ki = 166.0 nM 6.78
CHEMBL14839 Ki = 946.0 nM 6.02
CHEMBL14554 Ki = 1683.0 nM 5.77
CHEMBL15244 Ki = 6036.0 nM 5.22
CHEMBL14537 Ki = 6646.0 nM 5.18
CHEMBL2079554 Ki = 8136.0 nM 5.09
CHEMBL15212 Ki = 10883.0 nM 4.96
CHEMBL277559 Ki = 16946.0 nM 4.77