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Assay Detail

CHEMBL5164094

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

Binding
Displacement of [3H]-LSD from human 5-HT6R stably expressed in HEK293 cells by radioligand binding assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Overcoming undesirable hERG affinity by incorporating fluorine atoms: A case of MAO-B inhibitors derived from 1 H-pyrrolo-[3,2-c]quinolines.
Grychowska K, Olejarz-Maciej A, Blicharz K, Pietruś W, Karcz T, Kurczab R, Koczurkiewicz P, Doroz-Płonka A, Latacz G, Keeri AR, Piska K, Satała G, Pęgiel J, Trybała W, Jastrzębska-Więsek M, Bojarski AJ, Lamaty F, Partyka A, Walczak M, Krawczyk M, Malikowska-Racia N, Popik P, Zajdel P.
Eur J Med Chem (2022) 236 : 114329 -114329
PubMed 35397400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.96 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4125735 1 8.52
CHEMBL5183690 1 7.14
CHEMBL5188859 1 6.46
CHEMBL5197407 1 6.16
CHEMBL5174789 1 6.13
CHEMBL5209131 1 6.10
CHEMBL5187034 1 6.08
CHEMBL5173511 1 6.00
CHEMBL5201892 1 5.91
CHEMBL5175763 1 5.87
CHEMBL5177167 1 5.87
CHEMBL5178803 1 5.77
CHEMBL5193046 1 5.76
CHEMBL5181534 1 5.65
CHEMBL5199814 1 5.52
CHEMBL5200705 1 5.42
CHEMBL5206513 1 4.48
CHEMBL5187539 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4125735 Ki = 3.0 nM 8.52
CHEMBL5183690 Ki = 73.0 nM 7.14
CHEMBL5188859 Ki = 350.0 nM 6.46
CHEMBL5197407 Ki = 696.0 nM 6.16
CHEMBL5174789 Ki = 740.0 nM 6.13
CHEMBL5209131 Ki = 799.0 nM 6.10
CHEMBL5187034 Ki = 838.0 nM 6.08
CHEMBL5173511 Ki = 992.0 nM 6.00
CHEMBL5201892 Ki = 1227.0 nM 5.91
CHEMBL5175763 Ki = 1362.0 nM 5.87
CHEMBL5177167 Ki = 1338.0 nM 5.87
CHEMBL5178803 Ki = 1713.0 nM 5.77
CHEMBL5193046 Ki = 1742.0 nM 5.76
CHEMBL5181534 Ki = 2243.0 nM 5.65
CHEMBL5199814 Ki = 3024.0 nM 5.52
CHEMBL5200705 Ki = 3827.0 nM 5.42
CHEMBL5206513 Ki = 33060.0 nM 4.48
CHEMBL5187539 Ki = 40300.0 nM 4.39