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Assay Detail

CHEMBL3124177

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Binding
Agonist activity at muscarinic M1 receptor in New Zealand rabbit vas deferens assessed as stimulation of electrically-induced response
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Vas deferens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Bis(ammonio)alkane-type agonists of muscarinic acetylcholine receptors: synthesis, in vitro functional characterization, and in vivo evaluation of their analgesic activity.
Matera C, Flammini L, Quadri M, Vivo V, Ballabeni V, Holzgrabe U, Mohr K, De Amici M, Barocelli E, Bertoni S, Dallanoce C.
Eur J Med Chem (2014) 75 : 222 -232
PubMed 24534538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 7.74 9.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3121473 1 9.87
CHEMBL3121479 1 8.19
CHEMBL3120178 1 8.06
CHEMBL3121480 1 8.00
CHEMBL3121475 1 7.98
CHEMBL3121476 1 7.79
CHEMBL3121478 1 7.66
CHEMBL3121477 1 7.41
CHEMBL74300 1 6.43
CHEMBL3121474 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3121473 EC50 = 0.1349 nM 9.87
CHEMBL3121479 EC50 = 6.457 nM 8.19
CHEMBL3120178 EC50 = 8.71 nM 8.06
CHEMBL3121480 EC50 = 10.0 nM 8.00
CHEMBL3121475 EC50 = 10.47 nM 7.98
CHEMBL3121476 EC50 = 16.22 nM 7.79
CHEMBL3121478 EC50 = 21.88 nM 7.66
CHEMBL3121477 EC50 = 38.9 nM 7.41
CHEMBL74300 EC50 = 371.54 nM 6.43
CHEMBL3121474 EC50 = 912.01 nM 6.04