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Assay Detail

CHEMBL854532

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

Binding
Binding affinity to human 5HT6 receptor 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 Expert

Target

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

Publication

Binding of sulfonyl-containing arylalkylamines at human 5-HT6 serotonin receptors.
Sikazwe D, Bondarev ML, Dukat M, Rangisetty JB, Roth BL, Glennon RA.
J Med Chem (2006) 49 : 5217 -5225
PubMed 16913710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.21 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL212995 1 8.92
CHEMBL211577 1 8.16
CHEMBL378892 1 7.82
CHEMBL378656 1 7.77
CHEMBL212063 1 7.68
CHEMBL213589 1 7.43
CHEMBL434365 1 7.42
CHEMBL212227 1 7.42
CHEMBL209383 1 7.30
CHEMBL212178 1 7.28
CHEMBL213586 1 7.21
CHEMBL415046 1 7.16
CHEMBL426332 1 7.07
CHEMBL211688 1 6.94
CHEMBL378179 1 6.64
CHEMBL209909 1 6.54
CHEMBL378618 1 5.55
CHEMBL209893 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL212995 Ki = 1.2 nM 8.92
CHEMBL211577 Ki = 6.9 nM 8.16
CHEMBL378892 Ki = 15.0 nM 7.82
CHEMBL378656 Ki = 17.0 nM 7.77
CHEMBL212063 Ki = 21.0 nM 7.68
CHEMBL213589 Ki = 37.0 nM 7.43
CHEMBL434365 Ki = 38.0 nM 7.42
CHEMBL212227 Ki = 38.0 nM 7.42
CHEMBL209383 Ki = 50.0 nM 7.30
CHEMBL212178 Ki = 52.0 nM 7.28
CHEMBL213586 Ki = 62.0 nM 7.21
CHEMBL415046 Ki = 70.0 nM 7.16
CHEMBL426332 Ki = 85.0 nM 7.07
CHEMBL211688 Ki = 115.0 nM 6.94
CHEMBL378179 Ki = 230.0 nM 6.64
CHEMBL209909 Ki = 290.0 nM 6.54
CHEMBL378618 Ki = 2840.0 nM 5.55
CHEMBL209893 Ki = 4000.0 nM 5.40