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Assay Detail

CHEMBL749864

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

Binding
Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 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 M4 (CHEMBL1821)
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 6.36 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64000 1 7.48
CHEMBL314493 1 7.38
CHEMBL315428 1 7.32
CHEMBL7634 OXOTREMORINE 1 6.80
CHEMBL84113 1 6.72
CHEMBL313738 1 6.52
CHEMBL85190 1 6.39
CHEMBL310558 1 6.18
CHEMBL82754 1 6.08
CHEMBL440138 1 6.02
CHEMBL12587 MUSCARINE 1 5.85
CHEMBL7303 ARECOLINE -1.0 1 5.62
CHEMBL14 CARBACHOL 4.0 1 5.58
CHEMBL294273 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64000 Ki = 33.0 nM 7.48
CHEMBL314493 Ki = 42.0 nM 7.38
CHEMBL315428 Ki = 48.0 nM 7.32
CHEMBL7634 OXOTREMORINE Ki = 160.0 nM 6.80
CHEMBL84113 Ki = 190.0 nM 6.72
CHEMBL313738 Ki = 300.0 nM 6.52
CHEMBL85190 Ki = 410.0 nM 6.39
CHEMBL310558 Ki = 660.0 nM 6.18
CHEMBL82754 Ki = 840.0 nM 6.08
CHEMBL440138 Ki = 960.0 nM 6.02
CHEMBL12587 MUSCARINE Ki = 1400.0 nM 5.85
CHEMBL7303 ARECOLINE Ki = 2400.0 nM 5.62
CHEMBL14 CARBACHOL Ki = 2600.0 nM 5.58
CHEMBL294273 Ki = 8300.0 nM 5.08