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Assay Detail

CHEMBL4329314

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

Binding
Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel multitarget-directed ligands targeting acetylcholinesterase and σ<sub>1</sub> receptors as lead compounds for treatment of Alzheimer's disease: Synthesis, evaluation, and structural characterization of their complexes with acetylcholinesterase.
Lalut J, Santoni G, Karila D, Lecoutey C, Davis A, Nachon F, Silman I, Sussman J, Weik M, Maurice T, Dallemagne P, Rochais C.
Eur J Med Chem (2019) 162 : 234 -248
PubMed 30447434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.41 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85251 1 8.03
CHEMBL3417009 1 8.02
CHEMBL4562793 1 7.60
CHEMBL4444843 1 7.43
CHEMBL4529710 1 7.43
CHEMBL4537101 1 7.39
CHEMBL4567394 1 7.30
CHEMBL4454706 1 7.29
CHEMBL4526050 1 6.82
CHEMBL4585990 1 6.77
CHEMBL54 HALOPERIDOL 4.0 1 -
CHEMBL4540355 1 -
CHEMBL502 DONEPEZIL 4.0 1 -
CHEMBL4559904 1 -
CHEMBL4541090 1 -
CHEMBL4583738 1 -
CHEMBL4578844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85251 Ki = 9.33 nM 8.03
CHEMBL3417009 Ki = 9.5 nM 8.02
CHEMBL4562793 Ki = 25.0 nM 7.60
CHEMBL4444843 Ki = 37.5 nM 7.43
CHEMBL4529710 Ki = 37.5 nM 7.43
CHEMBL4537101 Ki = 40.9 nM 7.39
CHEMBL4567394 Ki = 49.6 nM 7.30
CHEMBL4454706 Ki = 51.0 nM 7.29
CHEMBL4526050 Ki = 150.0 nM 6.82
CHEMBL4585990 Ki = 169.0 nM 6.77
CHEMBL54 HALOPERIDOL Ki - -
CHEMBL4540355 Ki - -
CHEMBL502 DONEPEZIL Ki - -
CHEMBL4559904 Ki - -
CHEMBL4541090 Ki - -
CHEMBL4583738 Ki - -
CHEMBL4578844 Ki - -