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Assay Detail

CHEMBL748438

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

Binding
Binding affinity for muscarinic receptor site in rat hippocampus was determined using competitive radioligand binding assays employing [3H]OXO-M
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Isoarecolones and arecolones: selective central nicotinic agonists that cross the blood-brain barrier
Ward JS, Merritt L, Bymaster FP, Calligaro DO
Bioorg Med Chem Lett (1994) 4 : 573 -578
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.66 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7303 ARECOLINE -1.0 1 7.40
CHEMBL152775 1 5.86
CHEMBL154329 1 5.78
CHEMBL152310 1 5.72
CHEMBL346802 ARECOLON 1 5.71
CHEMBL346466 1 5.61
CHEMBL154385 1 5.57
CHEMBL153298 1 5.56
CHEMBL152530 1 5.46
CHEMBL156793 1 5.43
CHEMBL157267 1 5.36
CHEMBL152050 1 5.36
CHEMBL265553 1 5.27
CHEMBL154941 1 5.20
CHEMBL351805 1 -
CHEMBL3 NICOTINE 4.0 1 -
CHEMBL439821 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7303 ARECOLINE Ki = 40.0 nM 7.40
CHEMBL152775 Ki = 1385.0 nM 5.86
CHEMBL154329 Ki = 1650.0 nM 5.78
CHEMBL152310 Ki = 1885.0 nM 5.72
CHEMBL346802 ARECOLON Ki = 1950.0 nM 5.71
CHEMBL346466 Ki = 2450.0 nM 5.61
CHEMBL154385 Ki = 2690.0 nM 5.57
CHEMBL153298 Ki = 2730.0 nM 5.56
CHEMBL152530 Ki = 3500.0 nM 5.46
CHEMBL156793 Ki = 3750.0 nM 5.43
CHEMBL157267 Ki = 4380.0 nM 5.36
CHEMBL152050 Ki = 4345.0 nM 5.36
CHEMBL265553 Ki = 5425.0 nM 5.27
CHEMBL154941 Ki = 6250.0 nM 5.20
CHEMBL351805 Ki > 5000.0 nM -
CHEMBL3 NICOTINE Ki > 5000.0 nM -
CHEMBL439821 Ki > 5000.0 nM -