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Assay Detail

CHEMBL752313

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

Binding
Inhibition of [3H]OXO-M binding against muscarinic acetylcholine receptor in rat brain membranes
12
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues.
Triggle DJ, Kwon YW, Abraham P, Pitner JB, Mascarella SW, Carroll FI.
J Med Chem (1991) 34 : 3164 -3171
PubMed 1956033 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.05 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 9.34
CHEMBL14 CARBACHOL 4.0 1 7.88
CHEMBL550 PILOCARPINE 4.0 1 7.08
CHEMBL326453 1 6.95
CHEMBL111529 2 5.94
CHEMBL607175 1 5.71
CHEMBL2113669 2 5.38
CHEMBL325322 3 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 0.459 nM 9.34
CHEMBL14 CARBACHOL Ki = 13.1 nM 7.88
CHEMBL550 PILOCARPINE Ki = 82.9 nM 7.08
CHEMBL326453 Ki = 113.0 nM 6.95
CHEMBL111529 Ki = 1150.0 nM 5.94
CHEMBL607175 Ki = 1950.0 nM 5.71
CHEMBL2113669 Ki = 4150.0 nM 5.38
CHEMBL111529 Ki = 6550.0 nM 5.18
CHEMBL325322 Ki = 7820.0 nM 5.11
CHEMBL325322 Ki = 10400.0 nM 4.98
CHEMBL2113669 Ki = 23300.0 nM 4.63
CHEMBL325322 Ki = 33900.0 nM 4.47