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Assay Detail

CHEMBL4816282

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Functional
Agonist activity at muscarinic M3 receptor (unknown origin) expressed in CHO cells
7
Total Activities
7
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 M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.
Watanabe H, Ishida K, Yamamoto M, Nakako T, Horiguchi M, Isobe Y.
Bioorg Med Chem Lett (2021) 40 : 127911 -127911
PubMed 33691168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.18 6.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4748915 1 6.19
CHEMBL845 N-DESMETHYLCLOZAPINE 1 6.17
CHEMBL42 CLOZAPINE 4.0 1 -
CHEMBL4852403 1 -
CHEMBL4873426 1 -
CHEMBL4849385 1 -
CHEMBL4856628 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4748915 EC50 = 640.0 nM 6.19
CHEMBL845 N-DESMETHYLCLOZAPINE EC50 = 670.0 nM 6.17
CHEMBL42 CLOZAPINE EC50 > 10000.0 nM -
CHEMBL4852403 EC50 > 10000.0 nM -
CHEMBL4873426 EC50 > 10000.0 nM -
CHEMBL4849385 EC50 > 10000.0 nM -
CHEMBL4856628 EC50 > 10000.0 nM -