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Assay Detail

CHEMBL1048032

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

Binding
Displacement of [3H]NMS from human cloned muscarinic M2 receptor expressed in CHO cells by scintillation counting
17
Total Activities
17
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 Intermediate

Target

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

Publication

Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.
Scapecchi S, Nesi M, Matucci R, Bellucci C, Buccioni M, Dei S, Guandalini L, Manetti D, Martelli C, Martini E, Marucci G, Orlandi F, Romanelli MN, Teodori E, Cirilli R.
J Med Chem (2010) 53 : 201 -207
PubMed 19928767 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.51 9.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376897 METHSCOPOLAMINE 4.0 1 9.75
CHEMBL569307 1 8.63
CHEMBL571121 1 8.34
CHEMBL583051 1 8.17
CHEMBL569760 1 7.99
CHEMBL583027 1 7.87
CHEMBL569712 1 7.76
CHEMBL568870 1 7.70
CHEMBL576663 1 7.53
CHEMBL569729 1 7.50
CHEMBL571341 1 7.22
CHEMBL571123 1 7.19
CHEMBL568775 1 7.06
CHEMBL576707 1 6.85
CHEMBL569212 1 6.44
CHEMBL569089 1 6.12
CHEMBL569953 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376897 METHSCOPOLAMINE Ki = 0.1778 nM 9.75
CHEMBL569307 Ki = 2.344 nM 8.63
CHEMBL571121 Ki = 4.571 nM 8.34
CHEMBL583051 Ki = 6.761 nM 8.17
CHEMBL569760 Ki = 10.23 nM 7.99
CHEMBL583027 Ki = 13.49 nM 7.87
CHEMBL569712 Ki = 17.38 nM 7.76
CHEMBL568870 Ki = 19.95 nM 7.70
CHEMBL576663 Ki = 29.51 nM 7.53
CHEMBL569729 Ki = 31.62 nM 7.50
CHEMBL571341 Ki = 60.26 nM 7.22
CHEMBL571123 Ki = 64.57 nM 7.19
CHEMBL568775 Ki = 87.1 nM 7.06
CHEMBL576707 Ki = 141.25 nM 6.85
CHEMBL569212 Ki = 363.08 nM 6.44
CHEMBL569089 Ki = 758.58 nM 6.12
CHEMBL569953 Ki = 3235.94 nM 5.49