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Assay Detail

CHEMBL982068

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

Binding
Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
Minarini A, Marucci G, Bellucci C, Giorgi G, Tumiatti V, Bolognesi ML, Matera R, Rosini M, Melchiorre C.
Bioorg Med Chem (2008) 16 : 7311 -7320
PubMed 18595721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.27 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2021477 1 7.40
CHEMBL2021479 1 7.39
CHEMBL2021476 1 7.35
CHEMBL9967 PIRENZEPINE 2.0 1 7.32
CHEMBL2021478 1 7.31
CHEMBL265256 TRIPITRAMINE 1 6.83
CHEMBL478227 1 -
CHEMBL478226 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2021477 Ki = 39.81 nM 7.40
CHEMBL2021479 Ki = 40.74 nM 7.39
CHEMBL2021476 Ki = 44.67 nM 7.35
CHEMBL9967 PIRENZEPINE Ki = 47.86 nM 7.32
CHEMBL2021478 Ki = 48.98 nM 7.31
CHEMBL265256 TRIPITRAMINE Ki = 147.91 nM 6.83
CHEMBL478227 Ki > 10000.0 nM -
CHEMBL478226 Ki > 10000.0 nM -