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Assay Detail

CHEMBL995215

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

Functional
Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.
Jin J, Wang Y, Shi D, Wang F, Davis RS, Jin Q, Fu W, Foley JJ, Webb EF, Dehaas CJ, Berlanga M, Burman M, Sarau HM, Morrow DM, Rao P, Kallal LA, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Busch-Petersen J.
J Med Chem (2008) 51 : 4866 -4869
PubMed 18680280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 9.17 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540396 1 9.70
CHEMBL540359 1 9.00
CHEMBL539887 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540396 Kd = 0.1995 nM 9.70
CHEMBL540359 Kd = 1.0 nM 9.00
CHEMBL539887 Kd = 1.585 nM 8.80