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Assay Detail

CHEMBL2446010

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

Binding
Binding affinity to alpha4beta2 nAChR (unknown origin)
5
Total Activities
5
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

Design, synthesis and binding affinity of acetylcholine carbamoyl analogues.
Bolchi C, Valoti E, Binda M, Fasoli F, Ferrara R, Fumagalli L, Gotti C, Matucci R, Vistoli G, Pallavicini M.
Bioorg Med Chem Lett (2013) 23 : 6481 -6485
PubMed 24128660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.68 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2441748 1 7.70
CHEMBL1472561 1 7.64
CHEMBL965 CARBAMOYLCHOLINE 4.0 1 6.12
CHEMBL2441749 2-(DIMETHYLAMINO)ETHYL DIMETHYLCARBAMATE 1 5.24
CHEMBL1482 BETHANECHOL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2441748 Ki = 20.0 nM 7.70
CHEMBL1472561 Ki = 23.0 nM 7.64
CHEMBL965 CARBAMOYLCHOLINE Ki = 750.0 nM 6.12
CHEMBL2441749 2-(DIMETHYLAMINO)ETHYL DIMETHYLCARBAMATE Ki = 5700.0 nM 5.24
CHEMBL1482 BETHANECHOL Ki - -