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Assay Detail

CHEMBL748441

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

Binding
Inhibition of [3H]pirenzepine binding to muscarinic receptor in rat cortical homogenates
14
Total Activities
14
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

Muscarinic antagonist activity of 3-(5-alkoxy-oxazol-2-yl)-1,2,5,6-tetrahydropyridines.
Mitch CH, Bymaster FP, Calligaro DO, Quimby SJ, Schoepp DD, Wong DT, Shannon HE
Bioorg Med Chem Lett (1994) 4 : 1721 -1724
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.22 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569713 SCOPOLAMINE 4.0 1 10.10
CHEMBL295365 1 9.10
CHEMBL300424 1 9.10
CHEMBL45694 1 8.82
CHEMBL49915 1 8.70
CHEMBL298030 1 8.00
CHEMBL48342 1 7.96
CHEMBL297794 1 7.80
CHEMBL47178 1 7.66
CHEMBL46324 1 7.60
CHEMBL296552 1 7.52
CHEMBL47331 1 7.48
CHEMBL49139 1 7.05
CHEMBL297896 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569713 SCOPOLAMINE Ki = 0.08 nM 10.10
CHEMBL295365 Ki = 0.8 nM 9.10
CHEMBL300424 Ki = 0.8 nM 9.10
CHEMBL45694 Ki = 1.5 nM 8.82
CHEMBL49915 Ki = 2.0 nM 8.70
CHEMBL298030 Ki = 10.0 nM 8.00
CHEMBL48342 Ki = 11.0 nM 7.96
CHEMBL297794 Ki = 16.0 nM 7.80
CHEMBL47178 Ki = 22.0 nM 7.66
CHEMBL46324 Ki = 25.0 nM 7.60
CHEMBL296552 Ki = 30.0 nM 7.52
CHEMBL47331 Ki = 33.0 nM 7.48
CHEMBL49139 Ki = 90.0 nM 7.05
CHEMBL297896 Ki > 1000.0 nM -