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Assay Detail

CHEMBL747415

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

Binding
In vitro binding affinity to muscarinic acetylcholine receptor site in rat brain assayed using [3H]oxotremorine-M as the radioligand.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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
IC50 27 7.11 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL351934 1 8.20
CHEMBL350949 1 8.11
CHEMBL159273 1 7.96
CHEMBL355824 1 7.92
CHEMBL346030 1 7.91
CHEMBL349025 1 7.85
CHEMBL161007 1 7.55
CHEMBL349066 1 7.43
CHEMBL422538 1 7.36
CHEMBL159628 1 7.23
CHEMBL161670 1 7.22
CHEMBL7303 ARECOLINE -1.0 1 7.11
CHEMBL159841 1 7.11
CHEMBL161088 1 7.06
CHEMBL161364 1 6.99
CHEMBL161748 1 6.97
CHEMBL159708 1 6.84
CHEMBL162134 1 6.84
CHEMBL159651 1 6.74
CHEMBL159935 1 6.74
CHEMBL159839 1 6.72
CHEMBL262517 1 6.54
CHEMBL422710 1 6.17
CHEMBL161189 1 6.16
CHEMBL161419 1 6.02
CHEMBL349844 1 6.02
CHEMBL159311 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL351934 IC50 = 6.3 nM 8.20
CHEMBL350949 IC50 = 7.8 nM 8.11
CHEMBL159273 IC50 = 11.0 nM 7.96
CHEMBL355824 IC50 = 12.1 nM 7.92
CHEMBL346030 IC50 = 12.3 nM 7.91
CHEMBL349025 IC50 = 14.1 nM 7.85
CHEMBL161007 IC50 = 28.3 nM 7.55
CHEMBL349066 IC50 = 36.9 nM 7.43
CHEMBL422538 IC50 = 43.5 nM 7.36
CHEMBL159628 IC50 = 58.5 nM 7.23
CHEMBL161670 IC50 = 59.9 nM 7.22
CHEMBL7303 ARECOLINE IC50 = 77.0 nM 7.11
CHEMBL159841 IC50 = 78.0 nM 7.11
CHEMBL161088 IC50 = 86.2 nM 7.06
CHEMBL161364 IC50 = 102.0 nM 6.99
CHEMBL161748 IC50 = 107.0 nM 6.97
CHEMBL159708 IC50 = 145.0 nM 6.84
CHEMBL162134 IC50 = 144.0 nM 6.84
CHEMBL159651 IC50 = 181.0 nM 6.74
CHEMBL159935 IC50 = 182.0 nM 6.74
CHEMBL159839 IC50 = 191.0 nM 6.72
CHEMBL262517 IC50 = 286.0 nM 6.54
CHEMBL422710 IC50 = 681.0 nM 6.17
CHEMBL161189 IC50 = 685.0 nM 6.16
CHEMBL161419 IC50 = 954.0 nM 6.02
CHEMBL349844 IC50 = 955.0 nM 6.02
CHEMBL159311 IC50 > 850.0 nM -