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Assay Detail

CHEMBL744152

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

Binding
Inhibition of [3H]NMS (N-[3H]methylscopolamine) binding to Muscarinic acetylcholine receptor (mAChR)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL2094109)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.
Leader H, Wolfe AD, Chiang PK, Gordon RK.
J Med Chem (2002) 45 : 902 -910
PubMed 11831902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.62 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 8.62
CHEMBL26505 APROFENE 2.0 1 7.29
CHEMBL171501 1 5.58
CHEMBL443499 1 5.33
CHEMBL422905 1 5.09
CHEMBL352808 1 4.54
CHEMBL173955 1 4.38
CHEMBL172729 1 4.12
CHEMBL1115 PYRIDOSTIGMINE 4.0 1 -
CHEMBL173710 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 2.4 nM 8.62
CHEMBL26505 APROFENE Ki = 51.0 nM 7.29
CHEMBL171501 Ki = 2600.0 nM 5.58
CHEMBL443499 Ki = 4700.0 nM 5.33
CHEMBL422905 Ki = 8100.01 nM 5.09
CHEMBL352808 Ki = 29000.0 nM 4.54
CHEMBL173955 Ki = 42000.1 nM 4.38
CHEMBL172729 Ki = 75000.1 nM 4.12
CHEMBL1115 PYRIDOSTIGMINE Ki > 100000.0 nM -
CHEMBL173710 Ki > 100000.0 nM -