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Assay Detail

CHEMBL744920

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

Binding
Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M1 expressed in CHO cell membranes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.
Daly JW, Gupta TH, Padgett WL, Pei XF.
J Med Chem (2000) 43 : 2514 -2522
PubMed 10891110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.88 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64000 1 8.34
CHEMBL7303 ARECOLINE -1.0 1 7.85
CHEMBL7634 OXOTREMORINE 1 7.77
CHEMBL315428 1 7.54
CHEMBL12587 MUSCARINE 1 7.25
CHEMBL84113 1 6.92
CHEMBL14 CARBACHOL 4.0 1 6.77
CHEMBL310558 1 6.72
CHEMBL440138 1 6.64
CHEMBL85190 1 6.57
CHEMBL313738 1 6.35
CHEMBL82754 1 6.01
CHEMBL314493 1 6.00
CHEMBL294273 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64000 Ki = 4.6 nM 8.34
CHEMBL7303 ARECOLINE Ki = 14.0 nM 7.85
CHEMBL7634 OXOTREMORINE Ki = 17.0 nM 7.77
CHEMBL315428 Ki = 29.0 nM 7.54
CHEMBL12587 MUSCARINE Ki = 56.0 nM 7.25
CHEMBL84113 Ki = 120.0 nM 6.92
CHEMBL14 CARBACHOL Ki = 170.0 nM 6.77
CHEMBL310558 Ki = 190.0 nM 6.72
CHEMBL440138 Ki = 230.0 nM 6.64
CHEMBL85190 Ki = 270.0 nM 6.57
CHEMBL313738 Ki = 450.0 nM 6.35
CHEMBL82754 Ki = 970.0 nM 6.01
CHEMBL314493 Ki = 1000.0 nM 6.00
CHEMBL294273 Ki = 2300.0 nM 5.64