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Assay Detail

CHEMBL771610

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

Functional
In vitro inhibition of twitch height in electrically stimulated rabbit vas deferens
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Vas deferens
Confidence 1 — Organism
Curated By Expert

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Novel functional M1 selective muscarinic agonists. Synthesis and structure-activity relationships of 3-(1,2,5-thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines .
Sauerberg P, Olesen PH, Nielsen S, Treppendahl S, Sheardown MJ, Honoré T, Mitch CH, Ward JS, Pike AJ, Bymaster FP.
J Med Chem (1992) 35 : 2274 -2283
PubMed 1613751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.03 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308608 1 8.52
CHEMBL420007 1 8.52
CHEMBL306395 1 8.15
CHEMBL76161 1 8.05
CHEMBL74358 1 7.66
CHEMBL74301 1 7.58
CHEMBL75704 1 7.37
CHEMBL308744 1 7.33
CHEMBL76296 1 7.32
CHEMBL73338 1 6.97
CHEMBL72908 1 6.44
CHEMBL14 CARBACHOL 4.0 1 6.34
CHEMBL307645 1 6.27
CHEMBL7303 ARECOLINE -1.0 1 6.26
CHEMBL74300 1 6.18
CHEMBL308168 1 5.52
CHEMBL74786 1 5.00
CHEMBL75552 1 -
CHEMBL76107 1 -
CHEMBL309093 1 -
CHEMBL308381 1 -
CHEMBL73149 1 -
CHEMBL306941 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308608 IC50 = 3.0 nM 8.52
CHEMBL420007 IC50 = 3.0 nM 8.52
CHEMBL306395 IC50 = 7.0 nM 8.15
CHEMBL76161 IC50 = 9.0 nM 8.05
CHEMBL74358 IC50 = 22.0 nM 7.66
CHEMBL74301 IC50 = 26.0 nM 7.58
CHEMBL75704 IC50 = 43.0 nM 7.37
CHEMBL308744 IC50 = 47.0 nM 7.33
CHEMBL76296 IC50 = 48.0 nM 7.32
CHEMBL73338 IC50 = 108.0 nM 6.97
CHEMBL72908 IC50 = 364.0 nM 6.44
CHEMBL14 CARBACHOL IC50 = 460.0 nM 6.34
CHEMBL307645 IC50 = 537.0 nM 6.27
CHEMBL7303 ARECOLINE IC50 = 545.0 nM 6.26
CHEMBL74300 IC50 = 659.0 nM 6.18
CHEMBL308168 IC50 = 3000.0 nM 5.52
CHEMBL74786 IC50 = 10000.0 nM 5.00
CHEMBL75552 IC50 = 0.004 nM -
CHEMBL76107 IC50 = 0.006 nM -
CHEMBL309093 IC50 = 0.001 nM -
CHEMBL308381 IC50 = 0.002 nM -
CHEMBL73149 IC50 = 0.008 nM -
CHEMBL306941 IC50 = 0.003 nM -