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Assay Detail

CHEMBL741873

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Binding
The binding affinity was measured as inhibition of binding of [3H]- oxotremorine-M to muscarinic acetylcholine receptor in rat cerebral cortical membranes.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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 27 6.25 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64000 1 8.70
CHEMBL14 CARBACHOL 4.0 1 7.92
CHEMBL7634 OXOTREMORINE 1 7.89
CHEMBL12587 MUSCARINE 1 7.85
CHEMBL310558 1 7.52
CHEMBL7303 ARECOLINE -1.0 1 7.51
CHEMBL315630 1 6.80
CHEMBL315428 1 6.37
CHEMBL84113 1 6.19
CHEMBL314493 1 6.14
CHEMBL313738 1 6.07
CHEMBL85190 1 6.07
CHEMBL294273 1 6.07
CHEMBL316443 1 5.92
CHEMBL315749 1 5.85
CHEMBL440138 1 5.82
CHEMBL313002 1 5.77
CHEMBL314875 1 5.77
CHEMBL82754 1 5.72
CHEMBL82451 1 5.66
CHEMBL82225 1 5.57
CHEMBL408847 1 5.55
CHEMBL82260 1 5.37
CHEMBL82704 1 5.29
CHEMBL314212 1 5.25
CHEMBL312158 1 5.14
CHEMBL85299 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64000 Ki = 2.0 nM 8.70
CHEMBL14 CARBACHOL Ki = 12.0 nM 7.92
CHEMBL7634 OXOTREMORINE Ki = 13.0 nM 7.89
CHEMBL12587 MUSCARINE Ki = 14.0 nM 7.85
CHEMBL310558 Ki = 30.0 nM 7.52
CHEMBL7303 ARECOLINE Ki = 31.0 nM 7.51
CHEMBL315630 Ki = 160.0 nM 6.80
CHEMBL315428 Ki = 430.0 nM 6.37
CHEMBL84113 Ki = 650.0 nM 6.19
CHEMBL314493 Ki = 720.0 nM 6.14
CHEMBL313738 Ki = 860.0 nM 6.07
CHEMBL85190 Ki = 860.0 nM 6.07
CHEMBL294273 Ki = 860.0 nM 6.07
CHEMBL316443 Ki = 1200.0 nM 5.92
CHEMBL315749 Ki = 1400.0 nM 5.85
CHEMBL440138 Ki = 1500.0 nM 5.82
CHEMBL313002 Ki = 1700.0 nM 5.77
CHEMBL314875 Ki = 1700.0 nM 5.77
CHEMBL82754 Ki = 1900.0 nM 5.72
CHEMBL82451 Ki = 2200.0 nM 5.66
CHEMBL82225 Ki = 2700.0 nM 5.57
CHEMBL408847 Ki = 2800.0 nM 5.55
CHEMBL82260 Ki = 4300.0 nM 5.37
CHEMBL82704 Ki = 5100.0 nM 5.29
CHEMBL314212 Ki = 5600.0 nM 5.25
CHEMBL312158 Ki = 7300.0 nM 5.14
CHEMBL85299 Ki = 14000.0 nM 4.85