Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL839537

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

Binding
Inhibition of [3H]QNB binding to muscarinic receptor of rat cortex
20
Total Activities
20
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

Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
Zhou J, Kläss T, Johnson KM, Giberson KM, Kozikowski AP.
Bioorg Med Chem Lett (2005) 15 : 2461 -2465
PubMed 15863297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 5.28 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371816 1 5.97
CHEMBL195146 1 5.67
CHEMBL194329 1 5.56
CHEMBL2113081 1 5.55
CHEMBL2113083 1 5.47
CHEMBL195475 1 5.39
CHEMBL195138 1 5.15
CHEMBL194439 1 5.15
CHEMBL194024 1 4.92
CHEMBL193806 1 4.87
CHEMBL365519 1 4.86
CHEMBL371679 1 4.82
CHEMBL371349 1 -
CHEMBL195404 1 -
CHEMBL195181 1 -
CHEMBL195709 1 -
CHEMBL371344 1 -
CHEMBL334027 1 -
CHEMBL363189 1 -
CHEMBL191985 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371816 Ki = 1060.0 nM 5.97
CHEMBL195146 Ki = 2140.0 nM 5.67
CHEMBL194329 Ki = 2740.0 nM 5.56
CHEMBL2113081 Ki = 2830.0 nM 5.55
CHEMBL2113083 Ki = 3400.0 nM 5.47
CHEMBL195475 Ki = 4060.0 nM 5.39
CHEMBL195138 Ki = 7060.0 nM 5.15
CHEMBL194439 Ki = 7090.0 nM 5.15
CHEMBL194024 Ki = 11900.0 nM 4.92
CHEMBL193806 Ki = 13500.0 nM 4.87
CHEMBL365519 Ki = 13900.0 nM 4.86
CHEMBL371679 Ki = 15100.0 nM 4.82
CHEMBL371349 Ki > 10000.0 nM -
CHEMBL195404 Ki > 10000.0 nM -
CHEMBL195181 Ki > 10000.0 nM -
CHEMBL195709 Ki > 10000.0 nM -
CHEMBL371344 Ki > 10000.0 nM -
CHEMBL334027 Ki > 10000.0 nM -
CHEMBL363189 Ki > 10000.0 nM -
CHEMBL191985 Ki > 10000.0 nM -