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Assay Detail

CHEMBL747774

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

Binding
Evaluated for its binding affinity at human muscarinic receptor m2 by displacement of [3H]NMS binding using membranes from transfected chinese hamster ovarian cell
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type ovarian
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Identification and characterization of m4 selective muscarinic antagonists.
Augelli-Szafran CE, Jaen JC, Moreland DW, Nelson CB, Penvose-Yi JR, Schwarz RD.
Bioorg Med Chem Lett (1998) 8 : 1991 -1996
PubMed 9873472 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.66 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277642 HIMBACINE 1 7.76
CHEMBL1092 TRIHEXYPHENIDYL HYDROCHLORIDE 4.0 1 7.73
CHEMBL294726 1 5.94
CHEMBL61700 1 5.78
CHEMBL61412 1 5.72
CHEMBL62247 1 5.59
CHEMBL62251 1 5.58
CHEMBL301041 1 5.57
CHEMBL300987 1 5.52
CHEMBL59898 1 5.46
CHEMBL60142 1 5.34
CHEMBL61774 1 5.33
CHEMBL61494 1 5.11
CHEMBL58228 1 5.03
CHEMBL303758 1 5.02
CHEMBL59939 1 4.88
CHEMBL59347 1 4.83
CHEMBL304036 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277642 HIMBACINE IC50 = 17.5 nM 7.76
CHEMBL1092 TRIHEXYPHENIDYL HYDROCHLORIDE IC50 = 18.6 nM 7.73
CHEMBL294726 IC50 = 1151.5 nM 5.94
CHEMBL61700 IC50 = 1646.0 nM 5.78
CHEMBL61412 IC50 = 1905.1 nM 5.72
CHEMBL62247 IC50 = 2565.0 nM 5.59
CHEMBL62251 IC50 = 2643.0 nM 5.58
CHEMBL301041 IC50 = 2680.7 nM 5.57
CHEMBL300987 IC50 = 3002.9 nM 5.52
CHEMBL59898 IC50 = 3440.7 nM 5.46
CHEMBL60142 IC50 = 4563.5 nM 5.34
CHEMBL61774 IC50 = 4662.4 nM 5.33
CHEMBL61494 IC50 = 7703.7 nM 5.11
CHEMBL58228 IC50 = 9341.4 nM 5.03
CHEMBL303758 IC50 = 9524.7 nM 5.02
CHEMBL59939 IC50 = 13138.0 nM 4.88
CHEMBL59347 IC50 = 14677.7 nM 4.83
CHEMBL304036 IC50 < 1000.0 nM -