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Assay Detail

CHEMBL873446

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

Binding
In vitro inhibition of [3H]Oxo-Mas binding to M1 and M4 receptors in rat brain homogenate.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Muscarinic agonists with antipsychotic-like activity: structure-activity relationships of 1,2,5-thiadiazole analogues with functional dopamine antagonist activity.
Sauerberg P, Jeppesen L, Olesen PH, Rasmussen T, Swedberg MD, Sheardown MJ, Fink-Jensen A, Thomsen C, Thøgersen H, Rimvall K, Ward JS, Calligaro DO, DeLapp NW, Bymaster FP, Shannon HE.
J Med Chem (1998) 41 : 4378 -4384
PubMed 9784113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.61 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139316 1 9.33
CHEMBL344872 1 9.30
CHEMBL137804 1 9.28
CHEMBL336449 1 9.19
CHEMBL134579 1 9.19
CHEMBL137490 1 8.89
CHEMBL137537 1 8.89
CHEMBL343502 1 8.85
CHEMBL136807 VEDACLIDINE 2.0 1 8.66
CHEMBL343155 1 8.64
CHEMBL139075 1 8.60
CHEMBL344624 1 8.54
CHEMBL336227 1 8.48
CHEMBL139054 1 8.44
CHEMBL136194 1 8.38
CHEMBL7634 OXOTREMORINE 1 8.30
CHEMBL344669 1 8.21
CHEMBL343731 1 8.00
CHEMBL137292 1 7.88
CHEMBL550 PILOCARPINE 4.0 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139316 IC50 = 0.47 nM 9.33
CHEMBL344872 IC50 = 0.5 nM 9.30
CHEMBL137804 IC50 = 0.53 nM 9.28
CHEMBL336449 IC50 = 0.65 nM 9.19
CHEMBL134579 IC50 = 0.64 nM 9.19
CHEMBL137490 IC50 = 1.3 nM 8.89
CHEMBL137537 IC50 = 1.3 nM 8.89
CHEMBL343502 IC50 = 1.4 nM 8.85
CHEMBL136807 VEDACLIDINE IC50 = 2.2 nM 8.66
CHEMBL343155 IC50 = 2.3 nM 8.64
CHEMBL139075 IC50 = 2.5 nM 8.60
CHEMBL344624 IC50 = 2.9 nM 8.54
CHEMBL336227 IC50 = 3.3 nM 8.48
CHEMBL139054 IC50 = 3.6 nM 8.44
CHEMBL136194 IC50 = 4.2 nM 8.38
CHEMBL7634 OXOTREMORINE IC50 = 5.0 nM 8.30
CHEMBL344669 IC50 = 6.1 nM 8.21
CHEMBL343731 IC50 = 9.9 nM 8.00
CHEMBL137292 IC50 = 13.3 nM 7.88
CHEMBL550 PILOCARPINE IC50 = 67.0 nM 7.17