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Assay Detail

CHEMBL745529

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Binding
Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
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 M4 (CHEMBL317)
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 7.61 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131865 1 8.84
CHEMBL1202004 1 8.55
CHEMBL265256 TRIPITRAMINE 1 7.94
CHEMBL112244 1 7.80
CHEMBL335115 1 7.70
CHEMBL27673 METHOCTRAMINE 1 7.49
CHEMBL1202001 1 7.44
CHEMBL1202000 1 7.40
CHEMBL1202003 1 7.38
CHEMBL134692 1 7.20
CHEMBL1202002 1 6.80
CHEMBL407678 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131865 Ki = 1.445 nM 8.84
CHEMBL1202004 Ki = 2.818 nM 8.55
CHEMBL265256 TRIPITRAMINE Ki = 11.48 nM 7.94
CHEMBL112244 Ki = 15.85 nM 7.80
CHEMBL335115 Ki = 19.95 nM 7.70
CHEMBL27673 METHOCTRAMINE Ki = 32.36 nM 7.49
CHEMBL1202001 Ki = 36.31 nM 7.44
CHEMBL1202000 Ki = 39.81 nM 7.40
CHEMBL1202003 Ki = 41.69 nM 7.38
CHEMBL134692 Ki = 63.1 nM 7.20
CHEMBL1202002 Ki = 158.49 nM 6.80
CHEMBL407678 Ki = 158.49 nM 6.80