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Assay Detail

CHEMBL752168

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

Binding
Binding affinity against Muscarinic acetylcholine receptors using [3H]oxotremorine-M as radioligand in rat cortex
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Muscarinic analgesics with potent and selective effects on the gastrointestinal tract: potential application for the treatment of irritable bowel syndrome.
Mitch CH, Brown TJ, Bymaster FP, Calligaro DO, Dieckman D, Merrit L, Peters SC, Quimby SJ, Shannon HE, Shipley LA, Ward JS, Hansen K, Olesen PH, Sauerberg P, Sheardown MJ, Swedberg MD, Suzdak P, Greenwood B.
J Med Chem (1997) 40 : 538 -546
PubMed 9046345 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 8.84 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL150450 1 9.62
CHEMBL436075 1 9.48
CHEMBL153723 1 9.44
CHEMBL136807 VEDACLIDINE 2.0 1 9.40
CHEMBL150293 1 9.38
CHEMBL153478 1 9.36
CHEMBL343731 1 9.35
CHEMBL115648 1 9.30
CHEMBL517712 ATROPINE 4.0 1 9.05
CHEMBL357279 1 9.04
CHEMBL318403 1 9.00
CHEMBL101054 1 8.85
CHEMBL153150 1 8.52
CHEMBL153031 1 8.46
CHEMBL332700 1 8.40
CHEMBL150501 1 8.02
CHEMBL152892 1 8.00
CHEMBL152919 1 7.75
CHEMBL154923 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL150450 Ki = 0.24 nM 9.62
CHEMBL436075 Ki = 0.33 nM 9.48
CHEMBL153723 Ki = 0.36 nM 9.44
CHEMBL136807 VEDACLIDINE Ki = 0.4 nM 9.40
CHEMBL150293 Ki = 0.42 nM 9.38
CHEMBL153478 Ki = 0.44 nM 9.36
CHEMBL343731 Ki = 0.45 nM 9.35
CHEMBL115648 Ki = 0.5 nM 9.30
CHEMBL517712 ATROPINE Ki = 0.9 nM 9.05
CHEMBL357279 Ki = 0.91 nM 9.04
CHEMBL318403 Ki = 1.0 nM 9.00
CHEMBL101054 Ki = 1.4 nM 8.85
CHEMBL153150 Ki = 3.0 nM 8.52
CHEMBL153031 Ki = 3.5 nM 8.46
CHEMBL332700 Ki = 4.0 nM 8.40
CHEMBL150501 Ki = 9.6 nM 8.02
CHEMBL152892 Ki = 10.0 nM 8.00
CHEMBL152919 Ki = 18.0 nM 7.75
CHEMBL154923 Ki = 25.0 nM 7.60