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Assay Detail

CHEMBL891646

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

Binding
Displacement of 1-[N-methyl- 3H]scopolamine from human muscarinic M2 receptor expressed in Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.
Sonda S, Katayama K, Fujio M, Sakashita H, Inaba K, Asano K, Akira T.
Bioorg Med Chem Lett (2007) 17 : 925 -931
PubMed 17188867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.12 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234440 1 9.92
CHEMBL394137 1 9.18
CHEMBL234258 1 8.74
CHEMBL391977 1 8.72
CHEMBL234439 1 8.70
CHEMBL394254 1 8.62
CHEMBL392186 1 8.29
CHEMBL435353 1 8.22
CHEMBL234438 1 8.21
CHEMBL233201 1 8.14
CHEMBL1231 OXYBUTYNIN 4.0 1 8.09
CHEMBL394255 1 8.06
CHEMBL234257 1 7.92
CHEMBL233202 1 7.92
CHEMBL233200 1 7.39
CHEMBL233198 1 7.36
CHEMBL234253 1 7.32
CHEMBL233199 1 7.31
CHEMBL234254 1 7.31
CHEMBL234252 1 7.05
CHEMBL234260 1 -
CHEMBL429620 1 -
CHEMBL435158 1 -
CHEMBL234255 1 -
CHEMBL234256 1 -
CHEMBL392045 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234440 Ki = 0.12 nM 9.92
CHEMBL394137 Ki = 0.66 nM 9.18
CHEMBL234258 Ki = 1.8 nM 8.74
CHEMBL391977 Ki = 1.9 nM 8.72
CHEMBL234439 Ki = 2.0 nM 8.70
CHEMBL394254 Ki = 2.4 nM 8.62
CHEMBL392186 Ki = 5.1 nM 8.29
CHEMBL435353 Ki = 6.0 nM 8.22
CHEMBL234438 Ki = 6.2 nM 8.21
CHEMBL233201 Ki = 7.2 nM 8.14
CHEMBL1231 OXYBUTYNIN Ki = 8.1 nM 8.09
CHEMBL394255 Ki = 8.8 nM 8.06
CHEMBL234257 Ki = 12.0 nM 7.92
CHEMBL233202 Ki = 12.0 nM 7.92
CHEMBL233200 Ki = 41.0 nM 7.39
CHEMBL233198 Ki = 44.0 nM 7.36
CHEMBL234253 Ki = 48.0 nM 7.32
CHEMBL233199 Ki = 49.0 nM 7.31
CHEMBL234254 Ki = 49.0 nM 7.31
CHEMBL234252 Ki = 90.0 nM 7.05
CHEMBL234260 Ki - -
CHEMBL429620 Ki - -
CHEMBL435158 Ki - -
CHEMBL234255 Ki - -
CHEMBL234256 Ki - -
CHEMBL392045 Ki - -