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Assay Detail

CHEMBL4844509

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

Binding
Displacement of [3H]-LSD from human 5HT6R expressed in CHO-K1 cell membranes incubated for 1 hr by scintillation counter method
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-(phenylsulfonyl)-1H-indole-based multifunctional ligands targeting cholinesterases and 5-HT<sub>6</sub> receptor with anti-aggregation properties against amyloid-beta and tau.
Wichur T, Pasieka A, Godyń J, Panek D, Góral I, Latacz G, Honkisz-Orzechowska E, Bucki A, Siwek A, Głuch-Lutwin M, Knez D, Brazzolotto X, Gobec S, Kołaczkowski M, Sabate R, Malawska B, Więckowska A.
Eur J Med Chem (2021) 225 : 113783 -113783
PubMed 34461507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.47 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4852099 1 10.00
CHEMBL93240 METITEPINE 2.0 1 9.52
CHEMBL4863218 1 9.00
CHEMBL4854972 1 8.77
CHEMBL4864206 1 8.70
CHEMBL4851595 1 8.70
CHEMBL4847532 1 8.70
CHEMBL4878383 1 8.52
CHEMBL4878361 1 8.52
CHEMBL4874513 1 8.46
CHEMBL4868597 1 8.46
CHEMBL4848231 1 8.15
CHEMBL4850488 1 8.10
CHEMBL4866788 1 8.10
CHEMBL4877482 1 8.07
CHEMBL4850051 1 8.00
CHEMBL4847373 1 7.96
CHEMBL4871964 1 7.92
CHEMBL4850546 1 7.89
CHEMBL4845823 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4852099 Ki = 0.1 nM 10.00
CHEMBL93240 METITEPINE Ki = 0.3 nM 9.52
CHEMBL4863218 Ki = 1.0 nM 9.00
CHEMBL4854972 Ki = 1.7 nM 8.77
CHEMBL4864206 Ki = 2.0 nM 8.70
CHEMBL4851595 Ki = 2.0 nM 8.70
CHEMBL4847532 Ki = 2.0 nM 8.70
CHEMBL4878383 Ki = 3.0 nM 8.52
CHEMBL4878361 Ki = 3.0 nM 8.52
CHEMBL4874513 Ki = 3.5 nM 8.46
CHEMBL4868597 Ki = 3.5 nM 8.46
CHEMBL4848231 Ki = 7.0 nM 8.15
CHEMBL4850488 Ki = 8.0 nM 8.10
CHEMBL4866788 Ki = 8.0 nM 8.10
CHEMBL4877482 Ki = 8.6 nM 8.07
CHEMBL4850051 Ki = 10.0 nM 8.00
CHEMBL4847373 Ki = 11.0 nM 7.96
CHEMBL4871964 Ki = 12.0 nM 7.92
CHEMBL4850546 Ki = 13.0 nM 7.89
CHEMBL4845823 Ki = 15.0 nM 7.82