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Assay Detail

CHEMBL744272

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

Binding
Binding affinity for rat cortex Muscarinic acetylcholine receptor M1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL276)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Bolognesi ML, Minarini A, Budriesi R, Cacciaguerra S, Chiarini A, Spampinato S, Tumiatti V, Melchiorre C.
J Med Chem (1998) 41 : 4150 -4160
PubMed 9767650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.89 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131865 1 9.30
CHEMBL1202003 1 9.02
CHEMBL265256 TRIPITRAMINE 1 8.45
CHEMBL112244 1 8.36
CHEMBL1202000 1 7.90
CHEMBL1202001 1 7.84
CHEMBL1202004 1 7.83
CHEMBL1202002 1 7.60
CHEMBL27673 METHOCTRAMINE 1 7.38
CHEMBL407678 1 7.30
CHEMBL134692 1 7.20
CHEMBL335115 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131865 Ki = 0.5012 nM 9.30
CHEMBL1202003 Ki = 0.955 nM 9.02
CHEMBL265256 TRIPITRAMINE Ki = 3.548 nM 8.45
CHEMBL112244 Ki = 4.365 nM 8.36
CHEMBL1202000 Ki = 12.59 nM 7.90
CHEMBL1202001 Ki = 14.45 nM 7.84
CHEMBL1202004 Ki = 14.79 nM 7.83
CHEMBL1202002 Ki = 25.12 nM 7.60
CHEMBL27673 METHOCTRAMINE Ki = 41.69 nM 7.38
CHEMBL407678 Ki = 50.12 nM 7.30
CHEMBL134692 Ki = 63.1 nM 7.20
CHEMBL335115 Ki = 316.23 nM 6.50