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Assay Detail

CHEMBL742765

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

Binding
Binding affinity against Muscarinic acetylcholine receptor M1 sites of rat
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.
Agoston GE, Wu JH, Izenwasser S, George C, Katz J, Kline RH, Newman AH.
J Med Chem (1997) 40 : 4329 -4339
PubMed 9435902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.65 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317757 DIFLUOROBENZTROPINE 1 8.05
CHEMBL3084641 1 7.54
CHEMBL417249 1 6.90
CHEMBL440272 1 6.87
CHEMBL12227 1 6.87
CHEMBL11776 1 6.81
CHEMBL3084927 1 6.62
CHEMBL11493 1 6.60
CHEMBL2308105 1 6.32
CHEMBL11768 1 6.21
CHEMBL12375 1 6.11
CHEMBL135982 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 9.0 nM 8.05
CHEMBL3084641 Ki = 29.1 nM 7.54
CHEMBL417249 Ki = 126.0 nM 6.90
CHEMBL440272 Ki = 136.0 nM 6.87
CHEMBL12227 Ki = 136.0 nM 6.87
CHEMBL11776 Ki = 156.0 nM 6.81
CHEMBL3084927 Ki = 238.0 nM 6.62
CHEMBL11493 Ki = 251.0 nM 6.60
CHEMBL2308105 Ki = 483.0 nM 6.32
CHEMBL11768 Ki = 611.0 nM 6.21
CHEMBL12375 Ki = 773.0 nM 6.11
CHEMBL135982 Ki = 12300.0 nM 4.91