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Assay Detail

CHEMBL1912299

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

Binding
Displacement of [3H]-epibatidine from Bulinus truncatus N-terminal FLAG-tagged AChBP F149L mutant expressed in HEK293 cells after 2 hrs by liquid scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bulinus truncatus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Docking studies of benzylidene anabaseine interactions with α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): application to the design of related α7 selective ligands.
Kombo DC, Mazurov A, Tallapragada K, Hammond PS, Chewning J, Hauser TA, Vasquez-Valdivieso M, Yohannes D, Talley TT, Taylor P, Caldwell WS.
Eur J Med Chem (2011) 46 : 5625 -5635
PubMed 21986237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.35 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1162395 1 7.66
CHEMBL1163383 1 7.48
CHEMBL134713 GTS-21 2.0 1 7.23
CHEMBL1165604 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1162395 Kd = 22.0 nM 7.66
CHEMBL1163383 Kd = 33.0 nM 7.48
CHEMBL134713 GTS-21 Kd = 59.0 nM 7.23
CHEMBL1165604 Kd = 93.0 nM 7.03