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Assay Detail

CHEMBL743970

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

Binding
Inhibition of binding of [3H]N-methylscopolamine to muscarinic receptor (M3) in rat submaxillary gland homogenates
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL320)
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 6.64 8.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76897 4-DAMP 1 8.94
CHEMBL9967 PIRENZEPINE 2.0 1 6.76
CHEMBL165220 1 6.52
CHEMBL194216 SPIROTRAMINE 1 6.01
CHEMBL27673 METHOCTRAMINE 1 5.96
CHEMBL163901 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76897 4-DAMP Ki = 1.148 nM 8.94
CHEMBL9967 PIRENZEPINE Ki = 173.78 nM 6.76
CHEMBL165220 Ki = 302.0 nM 6.52
CHEMBL194216 SPIROTRAMINE Ki = 977.24 nM 6.01
CHEMBL27673 METHOCTRAMINE Ki = 1096.48 nM 5.96
CHEMBL163901 Ki = 2137.96 nM 5.67