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Assay Detail

CHEMBL983583

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Functional
Agonist activity at muscarinic M2 receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.
Bridges TM, Brady AE, Kennedy JP, Daniels RN, Miller NR, Kim K, Breininger ML, Gentry PR, Brogan JT, Jones CK, Conn PJ, Lindsley CW.
Bioorg Med Chem Lett (2008) 18 : 5439 -5442
PubMed 18805692 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 7.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL491209 1 7.92
CHEMBL514689 1 -
CHEMBL522460 1 -
CHEMBL491818 1 -
CHEMBL489576 1 -
CHEMBL521914 1 -
CHEMBL490797 1 -
CHEMBL522451 1 -
CHEMBL490598 1 -
CHEMBL491208 1 -
CHEMBL478034 1 -
CHEMBL515489 1 -
CHEMBL477821 1 -
CHEMBL518747 1 -
CHEMBL478662 1 -
CHEMBL490597 1 -
CHEMBL523657 1 -
CHEMBL476990 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL491209 EC50 = 11.9 nM 7.92
CHEMBL514689 EC50 > 50000.0 nM -
CHEMBL522460 EC50 > 50000.0 nM -
CHEMBL491818 EC50 > 50000.0 nM -
CHEMBL489576 EC50 > 50000.0 nM -
CHEMBL521914 EC50 > 50000.0 nM -
CHEMBL490797 EC50 > 50000.0 nM -
CHEMBL522451 EC50 > 50000.0 nM -
CHEMBL490598 EC50 > 50000.0 nM -
CHEMBL491208 EC50 > 50000.0 nM -
CHEMBL478034 EC50 > 50000.0 nM -
CHEMBL515489 EC50 > 50000.0 nM -
CHEMBL477821 EC50 > 50000.0 nM -
CHEMBL518747 EC50 > 50000.0 nM -
CHEMBL478662 EC50 > 50000.0 nM -
CHEMBL490597 EC50 > 50000.0 nM -
CHEMBL523657 EC50 > 50000.0 nM -
CHEMBL476990 EC50 > 50000.0 nM -