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Assay Detail

CHEMBL749024

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

Binding
Inhibition of binding of [3H]pirenzepine to muscarinic receptor (M1) in rat cortex homogenates
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
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 8.03 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76897 4-DAMP 1 9.23
CHEMBL165220 1 8.30
CHEMBL9967 PIRENZEPINE 2.0 1 8.19
CHEMBL194216 SPIROTRAMINE 1 7.88
CHEMBL27673 METHOCTRAMINE 1 7.43
CHEMBL163901 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76897 4-DAMP Ki = 0.5888 nM 9.23
CHEMBL165220 Ki = 5.012 nM 8.30
CHEMBL9967 PIRENZEPINE Ki = 6.457 nM 8.19
CHEMBL194216 SPIROTRAMINE Ki = 13.18 nM 7.88
CHEMBL27673 METHOCTRAMINE Ki = 37.15 nM 7.43
CHEMBL163901 Ki = 75.86 nM 7.12