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Assay Detail

CHEMBL932205

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

Binding
Displacement of [3H]N-methyl Scopolamine from human cloned muscarinic M4 receptor expressed in CHO cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a fluorescent muscarinic antagonist.
Jones LH, Randall A, Napier C, Trevethick M, Sreckovic S, Watson J.
Bioorg Med Chem Lett (2008) 18 : 825 -827
PubMed 18042383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.66 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1382 TOLTERODINE 4.0 1 8.51
CHEMBL271108 1 8.20
CHEMBL257431 1 6.99
CHEMBL257643 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1382 TOLTERODINE Ki = 3.1 nM 8.51
CHEMBL271108 Ki = 6.3 nM 8.20
CHEMBL257431 Ki = 103.0 nM 6.99
CHEMBL257643 Ki = 121.0 nM 6.92