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Assay Detail

CHEMBL861935

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

Functional
Potency at muscarinic receptor M1 in rabbit vas deferens
16
Total Activities
7
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Vas deferens
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors.
Disingrini T, Muth M, Dallanoce C, Barocelli E, Bertoni S, Kellershohn K, Mohr K, De Amici M, Holzgrabe U.
J Med Chem (2006) 49 : 366 -372
PubMed 16392821 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
pKb 7 - -
Intrinsic activity 7 - -
EC50 2 4.75 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL380572 3 5.05
CHEMBL199636 3 4.44
CHEMBL382846 2 -
CHEMBL381913 2 -
CHEMBL201016 2 -
CHEMBL197604 2 -
CHEMBL382659 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL380572 EC50 = 8912.51 nM 5.05
CHEMBL199636 EC50 = 36307.81 nM 4.44
CHEMBL380572 pKb - -
CHEMBL382846 pKb = 5.6 -
CHEMBL381913 pKb = 6.77 -
CHEMBL201016 pKb = 5.75 -
CHEMBL199636 pKb - -
CHEMBL197604 pKb = 5.33 -
CHEMBL382846 Intrinsic activity = - -
CHEMBL381913 Intrinsic activity = 0.28 -
CHEMBL201016 Intrinsic activity = - -
CHEMBL197604 Intrinsic activity = - -
CHEMBL199636 Intrinsic activity = 0.94 -
CHEMBL380572 Intrinsic activity = 0.99 -
CHEMBL382659 pKb = 6.2 -
CHEMBL382659 Intrinsic activity = - -