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Assay Detail

CHEMBL4119544

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

Binding
Displacement of [3H]NMS from recombinant human muscarinic M1 receptor expressed in CHOK1 cell membranes after 120 mins by scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments.
Del Bello F, Bonifazi A, Giorgioni G, Petrelli R, Quaglia W, Altomare A, Falcicchio A, Matucci R, Vistoli G, Piergentili A.
Eur J Med Chem (2017) 137 : 327 -337
PubMed 28609709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.16 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2078942 1 8.90
CHEMBL4128341 1 8.34
CHEMBL4129580 1 8.05
CHEMBL2078987 1 7.45
CHEMBL4126071 1 7.38
CHEMBL1734 SOLIFENACIN 4.0 1 7.29
CHEMBL4126290 1 7.26
CHEMBL4127373 1 7.17
CHEMBL4127428 1 6.92
CHEMBL4129723 1 6.79
CHEMBL4130037 1 6.72
CHEMBL4128497 1 6.71
CHEMBL4128667 1 6.42
CHEMBL4128764 1 6.18
CHEMBL4129382 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2078942 Ki = 1.259 nM 8.90
CHEMBL4128341 Ki = 4.571 nM 8.34
CHEMBL4129580 Ki = 8.913 nM 8.05
CHEMBL2078987 Ki = 35.48 nM 7.45
CHEMBL4126071 Ki = 41.69 nM 7.38
CHEMBL1734 SOLIFENACIN Ki = 51.29 nM 7.29
CHEMBL4126290 Ki = 54.95 nM 7.26
CHEMBL4127373 Ki = 67.61 nM 7.17
CHEMBL4127428 Ki = 120.23 nM 6.92
CHEMBL4129723 Ki = 162.18 nM 6.79
CHEMBL4130037 Ki = 190.55 nM 6.72
CHEMBL4128497 Ki = 194.98 nM 6.71
CHEMBL4128667 Ki = 380.19 nM 6.42
CHEMBL4128764 Ki = 660.69 nM 6.18
CHEMBL4129382 Ki = 1698.24 nM 5.77