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Assay Detail

CHEMBL747248

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

Binding
Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the Muscarinic acetylcholine receptor M1 subtypes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL2672)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
Leader H, Smejkal RM, Payne CS, Padilla FN, Doctor BP, Gordon RK, Chiang PK.
J Med Chem (1989) 32 : 1522 -1528
PubMed 2738887 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.92 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 8.62
CHEMBL36583 1 7.58
CHEMBL26505 APROFENE 2.0 1 7.29
CHEMBL37372 1 7.00
CHEMBL416974 1 6.82
CHEMBL39342 1 5.68
CHEMBL288482 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 2.4 nM 8.62
CHEMBL36583 Ki = 26.0 nM 7.58
CHEMBL26505 APROFENE Ki = 51.0 nM 7.29
CHEMBL37372 Ki = 100.0 nM 7.00
CHEMBL416974 Ki = 150.0 nM 6.82
CHEMBL39342 Ki = 2100.0 nM 5.68
CHEMBL288482 Ki = 3400.0 nM 5.47