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Assay Detail

CHEMBL743978

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

Binding
Displacement of [3H]QNB from rat ileum Muscarinic acetylcholine receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Ileum
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis of some 3-(1-azabicyclo[2.2.2]octyl) 3-amino-2-hydroxy-2-phenylpropionates: profile of antimuscarinic efficacy and selectivity.
Audia VH, McPherson DW, Weitzberg M, Rzeszotarski WJ, Sturm B, Kachur JF, Abreu M, Kaiser C.
J Med Chem (1990) 33 : 307 -310
PubMed 2296026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.09 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517712 ATROPINE 4.0 1 9.35
CHEMBL2115342 1 8.22
CHEMBL1202960 1 6.80
CHEMBL1202955 1 6.71
CHEMBL1202954 1 5.79
CHEMBL1202958 1 5.62
CHEMBL557216 1 5.40
CHEMBL320755 1 5.28
CHEMBL1202956 1 5.08
CHEMBL1202957 1 5.04
CHEMBL1202959 1 4.91
CHEMBL1202961 1 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517712 ATROPINE Ki = 0.45 nM 9.35
CHEMBL2115342 Ki = 6.0 nM 8.22
CHEMBL1202960 Ki = 158.0 nM 6.80
CHEMBL1202955 Ki = 195.0 nM 6.71
CHEMBL1202954 Ki = 1620.0 nM 5.79
CHEMBL1202958 Ki = 2380.0 nM 5.62
CHEMBL557216 Ki = 3980.0 nM 5.40
CHEMBL320755 Ki = 5240.0 nM 5.28
CHEMBL1202956 Ki = 8280.0 nM 5.08
CHEMBL1202957 Ki = 9190.0 nM 5.04
CHEMBL1202959 Ki = 12230.0 nM 4.91
CHEMBL1202961 Ki = 12600.0 nM 4.90