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Assay Detail

CHEMBL684492

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Functional
Agonist activity at muscarinic acetylcholine receptor in isolated guinea pig ileum.
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL2094109)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships.
Sauerberg P, Kindtler JW, Nielsen L, Sheardown MJ, Honoré T.
J Med Chem (1991) 34 : 687 -692
PubMed 1995893 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 6.54 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL346030 1 7.50
CHEMBL7303 ARECOLINE -1.0 1 7.14
CHEMBL351934 1 7.00
CHEMBL161007 1 6.89
CHEMBL349025 1 6.82
CHEMBL159273 1 6.70
CHEMBL355824 1 6.50
CHEMBL422538 1 6.38
CHEMBL349066 1 6.21
CHEMBL162134 1 6.14
CHEMBL350949 1 6.00
CHEMBL161748 1 5.89
CHEMBL161670 1 5.84
CHEMBL161189 1 -
CHEMBL161364 1 -
CHEMBL349844 1 -
CHEMBL159651 1 -
CHEMBL161419 1 -
CHEMBL159311 1 -
CHEMBL159841 1 -
CHEMBL159935 1 -
CHEMBL159708 1 -
CHEMBL262517 1 -
CHEMBL161088 1 -
CHEMBL422710 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL346030 EC50 = 32.0 nM 7.50
CHEMBL7303 ARECOLINE EC50 = 73.0 nM 7.14
CHEMBL351934 EC50 = 100.0 nM 7.00
CHEMBL161007 EC50 = 130.0 nM 6.89
CHEMBL349025 EC50 = 150.0 nM 6.82
CHEMBL159273 EC50 = 200.0 nM 6.70
CHEMBL355824 EC50 = 320.0 nM 6.50
CHEMBL422538 EC50 = 420.0 nM 6.38
CHEMBL349066 EC50 = 620.0 nM 6.21
CHEMBL162134 EC50 = 720.0 nM 6.14
CHEMBL350949 EC50 = 1000.0 nM 6.00
CHEMBL161748 EC50 = 1280.0 nM 5.89
CHEMBL161670 EC50 = 1460.0 nM 5.84
CHEMBL161189 EC50 > 30000.0 nM -
CHEMBL161364 EC50 > 30000.0 nM -
CHEMBL349844 EC50 > 30000.0 nM -
CHEMBL159651 EC50 > 30000.0 nM -
CHEMBL161419 EC50 > 30000.0 nM -
CHEMBL159311 EC50 > 30000.0 nM -
CHEMBL159841 EC50 > 30000.0 nM -
CHEMBL159935 EC50 > 30000.0 nM -
CHEMBL159708 EC50 > 30000.0 nM -
CHEMBL262517 EC50 > 30000.0 nM -
CHEMBL161088 EC50 > 30000.0 nM -
CHEMBL422710 EC50 > 30000.0 nM -