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Assay Detail

CHEMBL772346

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

Functional
Compound was evaluated for the inhibition of the twitch response in the electrically stimulated rabbit vas deferens
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP
Sauerberg P, Olesen PH, Suzdak PD, Sheardown MJ, Mitch CH, Sawyer BD, Shannon HE
Bioorg Med Chem Lett (1992) 2 : 809 -814
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.78 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21536 XANOMELINE 4.0 1 11.00
CHEMBL101054 1 7.82
CHEMBL7303 ARECOLINE -1.0 1 6.26
CHEMBL74300 1 6.18
CHEMBL74786 1 5.00
CHEMBL168581 1 4.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21536 XANOMELINE IC50 = 0.01 nM 11.00
CHEMBL101054 IC50 = 15.0 nM 7.82
CHEMBL7303 ARECOLINE IC50 = 545.0 nM 6.26
CHEMBL74300 IC50 = 659.0 nM 6.18
CHEMBL74786 IC50 = 10000.0 nM 5.00
CHEMBL168581 IC50 = 39000.0 nM 4.41