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Assay Detail

CHEMBL745065

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

Binding
Inhibition of binding of [3H]N-methylscopolamine to Muscarinic acetylcholine receptor M4 in NG 108-15 cell homogenates
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NG 108-15
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M4 (CHEMBL317)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-DAMP
Melchiorre C, Minarini A, Spampinato S, Tumiatti V
Bioorg Med Chem Lett (1995) 5 : 785 -790
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.58 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76897 4-DAMP 1 9.29
CHEMBL27673 METHOCTRAMINE 1 7.58
CHEMBL165220 1 7.50
CHEMBL9967 PIRENZEPINE 2.0 1 7.46
CHEMBL163901 1 7.40
CHEMBL194216 SPIROTRAMINE 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76897 4-DAMP Ki = 0.5129 nM 9.29
CHEMBL27673 METHOCTRAMINE Ki = 26.3 nM 7.58
CHEMBL165220 Ki = 31.62 nM 7.50
CHEMBL9967 PIRENZEPINE Ki = 34.67 nM 7.46
CHEMBL163901 Ki = 39.81 nM 7.40
CHEMBL194216 SPIROTRAMINE Ki = 537.03 nM 6.27