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Assay Detail

CHEMBL4026902

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

Binding
Displacement of [3H]cytisine from alpha4beta2 nAChR expressed in human recombinant SH-SY5Y cell membranes after 120 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Based Design and Discovery of New M2 Receptor Agonists.
Fish I, Stößel A, Eitel K, Valant C, Albold S, Huebner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P.
J Med Chem (2017) 60 : 9239 -9250
PubMed 29094937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.33 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 8.82
CHEMBL4083241 1 8.80
CHEMBL4099673 1 6.70
CHEMBL4060823 1 5.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 1.5 nM 8.82
CHEMBL4083241 Ki = 1.6 nM 8.80
CHEMBL4099673 Ki = 200.0 nM 6.70
CHEMBL4060823 Ki = 9700.0 nM 5.01