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Assay Detail

CHEMBL748442

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

Binding
Inhibition of radioligand [3H]NMS binding to muscarinic receptor of rat brain
11
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A marked change of receptor affinity of the 2-methyl-5-(3-hydroxyphenyl)morphans upon attachment of an (E)-8-benzylidene moiety: synthesis and evaluation of a new class of sigma receptor ligands.
Bertha CM, Mattson MV, Flippen-Anderson JL, Rothman RB, Xu H, Cha XY, Becketts K, Rice KC.
J Med Chem (1994) 37 : 3163 -3170
PubMed 7932540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 4.94 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111686 1 7.41
CHEMBL2111684 1 5.13
CHEMBL109124 1 4.94
CHEMBL110319 1 4.84
CHEMBL109160 1 4.83
CHEMBL2008608 1 4.73
CHEMBL322329 1 4.63
CHEMBL38791 2 4.60
CHEMBL3350264 1 4.58
CHEMBL2111685 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111686 Ki = 39.1 nM 7.41
CHEMBL2111684 Ki = 7400.0 nM 5.13
CHEMBL109124 Ki = 11600.0 nM 4.94
CHEMBL110319 Ki = 14400.0 nM 4.84
CHEMBL109160 Ki = 14700.0 nM 4.83
CHEMBL2008608 Ki = 18600.0 nM 4.73
CHEMBL322329 Ki = 23300.0 nM 4.63
CHEMBL38791 Ki = 25300.0 nM 4.60
CHEMBL3350264 Ki = 26000.0 nM 4.58
CHEMBL38791 Ki = 46400.0 nM 4.33
CHEMBL2111685 Ki = 50300.0 nM 4.30