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Assay Detail

CHEMBL752165

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

Binding
Binding affinity against Muscarinic acetylcholine receptor using [3H]-OXO-M as the radioligand.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.
Wu ES, Kover A, Semus SF.
J Med Chem (1998) 41 : 4181 -4185
PubMed 9784090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.55 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92421 1 9.70
CHEMBL334387 1 9.40
CHEMBL335503 1 9.10
CHEMBL134860 1 8.70
CHEMBL337509 1 8.70
CHEMBL134937 1 8.43
CHEMBL335496 1 8.40
CHEMBL40121 1 8.17
CHEMBL14 CARBACHOL 4.0 1 8.05
CHEMBL134830 1 7.85
CHEMBL448736 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92421 Ki = 0.2 nM 9.70
CHEMBL334387 Ki = 0.4 nM 9.40
CHEMBL335503 Ki = 0.8 nM 9.10
CHEMBL134860 Ki = 2.0 nM 8.70
CHEMBL337509 Ki = 2.0 nM 8.70
CHEMBL134937 Ki = 3.7 nM 8.43
CHEMBL335496 Ki = 4.0 nM 8.40
CHEMBL40121 Ki = 6.7 nM 8.17
CHEMBL14 CARBACHOL Ki = 9.0 nM 8.05
CHEMBL134830 Ki = 14.0 nM 7.85
CHEMBL448736 Ki = 30.0 nM 7.52