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Assay Detail

CHEMBL746423

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Binding
Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type A9L
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL3733)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
Messer WS, Abuh YF, Liu Y, Periyasamy S, Ngur DO, Edgar MA, El-Assadi AA, Sbeih S, Dunbar PG, Roknich S, Rho T, Fang Z, Ojo B, Zhang H, Huzl JJ, Nagy PI.
J Med Chem (1997) 40 : 1230 -1246
PubMed 9111297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 4.91 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7634 OXOTREMORINE 1 6.57
CHEMBL23957 OXOTREMORINE METHIODIDE 1 6.16
CHEMBL277014 1 5.27
CHEMBL21536 XANOMELINE 4.0 1 5.24
CHEMBL550 PILOCARPINE 4.0 1 5.16
CHEMBL12378 1 4.92
CHEMBL416736 1 4.92
CHEMBL281411 1 4.85
CHEMBL7303 ARECOLINE -1.0 1 4.57
CHEMBL542065 1 4.48
CHEMBL14 CARBACHOL 4.0 1 4.40
CHEMBL553602 1 4.39
CHEMBL541398 1 4.36
CHEMBL542064 1 4.30
CHEMBL543030 1 4.10
CHEMBL542561 1 -
CHEMBL538467 1 -
CHEMBL557795 1 -
CHEMBL538224 1 -
CHEMBL542559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7634 OXOTREMORINE EC50 = 270.0 nM 6.57
CHEMBL23957 OXOTREMORINE METHIODIDE EC50 = 700.0 nM 6.16
CHEMBL277014 EC50 = 5400.0 nM 5.27
CHEMBL21536 XANOMELINE EC50 = 5700.0 nM 5.24
CHEMBL550 PILOCARPINE EC50 = 6900.0 nM 5.16
CHEMBL12378 EC50 = 12000.0 nM 4.92
CHEMBL416736 EC50 = 12000.0 nM 4.92
CHEMBL281411 EC50 = 14000.0 nM 4.85
CHEMBL7303 ARECOLINE EC50 = 27000.0 nM 4.57
CHEMBL542065 EC50 = 33000.0 nM 4.48
CHEMBL14 CARBACHOL EC50 = 40000.0 nM 4.40
CHEMBL553602 EC50 = 41000.0 nM 4.39
CHEMBL541398 EC50 = 44000.0 nM 4.36
CHEMBL542064 EC50 = 50000.0 nM 4.30
CHEMBL543030 EC50 = 80000.0 nM 4.10
CHEMBL542561 EC50 = 300000.0 nM -
CHEMBL538467 EC50 = 200000.0 nM -
CHEMBL557795 EC50 = 116000.0 nM -
CHEMBL538224 EC50 = 160000.0 nM -
CHEMBL542559 EC50 = 560000.0 nM -