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

CHEMBL1024869

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

Functional
Antagonist activity at cloned muscarinic M1 receptor expressed in CHO cells assessed as acetylcholine-induced change in cytosolic calcium concentration by FLIPR assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
Jin J, Budzik B, Wang Y, Shi D, Wang F, Xie H, Wan Z, Zhu C, Foley JJ, Webb EF, Berlanga M, Burman M, Sarau HM, Morrow DM, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Lainé DI.
J Med Chem (2008) 51 : 5915 -5918
PubMed 18798607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 8.67 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492437 1 9.00
CHEMBL493266 1 9.00
CHEMBL555476 1 8.70
CHEMBL521523 1 8.60
CHEMBL493265 1 8.60
CHEMBL493465 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492437 Kd = 1.0 nM 9.00
CHEMBL493266 Kd = 1.0 nM 9.00
CHEMBL555476 Kd = 1.995 nM 8.70
CHEMBL521523 Kd = 2.512 nM 8.60
CHEMBL493265 Kd = 2.512 nM 8.60
CHEMBL493465 Kd = 7.943 nM 8.10