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Assay Detail

CHEMBL961849

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Binding
Activity at human alpha4beta2 nAChR expressed in Xenopus oocytes assessed as inhibition of acetylcholine-evoked current
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Oocyte
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Use of acetylcholine binding protein in the search for novel alpha7 nicotinic receptor ligands. In silico docking, pharmacological screening, and X-ray analysis.
Ulens C, Akdemir A, Jongejan A, van Elk R, Bertrand S, Perrakis A, Leurs R, Smit AB, Sixma TK, Bertrand D, de Esch IJ.
J Med Chem (2009) 52 : 2372 -2383
PubMed 19331415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 2 - -
IC50 2 6.51 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490843 2 6.68
CHEMBL491861 2 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490843 IC50 = 210.0 nM 6.68
CHEMBL491861 IC50 = 460.0 nM 6.34
CHEMBL490843 Activity - -
CHEMBL491861 Activity - -