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Assay Detail

CHEMBL4821057

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

Binding
Binding affinity to 5-HT6 receptor (unknown origin)
9
Total Activities
9
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 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
Gao L, Hao C, Chen J, Ma R, Zheng L, Wu Q, Liu X, Liu BF, Zhang G, Chen Y, Jin J.
Bioorg Med Chem Lett (2021) 40 : 127909 -127909
PubMed 33705900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.13 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3883955 1 9.30
CHEMBL4289498 1 8.25
CHEMBL4865907 1 7.03
CHEMBL4846866 1 6.91
CHEMBL4867978 1 6.85
CHEMBL4861311 1 6.83
CHEMBL2387229 1 6.64
CHEMBL1112 ARIPIPRAZOLE 4.0 1 6.50
CHEMBL85 RISPERIDONE 4.0 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3883955 Ki = 0.5 nM 9.30
CHEMBL4289498 Ki = 5.6 nM 8.25
CHEMBL4865907 Ki = 93.3 nM 7.03
CHEMBL4846866 Ki = 122.7 nM 6.91
CHEMBL4867978 Ki = 141.0 nM 6.85
CHEMBL4861311 Ki = 149.2 nM 6.83
CHEMBL2387229 Ki = 228.4 nM 6.64
CHEMBL1112 ARIPIPRAZOLE Ki = 318.0 nM 6.50
CHEMBL85 RISPERIDONE Ki = 1329.2 nM 5.88