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Assay Detail

CHEMBL829676

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

Binding
Binding affinity against cloned human 5-hydroxytryptamine 6 receptor expressed in HeLa cells using [3H]LSD
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
Cole DC, Ellingboe JW, Lennox WJ, Mazandarani H, Smith DL, Stock JR, Zhang G, Zhou P, Schechter LE.
Bioorg Med Chem Lett (2005) 15 : 379 -383
PubMed 15603958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 8.08 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362487 1 9.40
CHEMBL180606 1 9.00
CHEMBL359876 1 9.00
CHEMBL361180 1 9.00
CHEMBL179277 1 9.00
CHEMBL444015 1 8.70
CHEMBL178385 1 8.70
CHEMBL179592 1 8.70
CHEMBL444878 1 8.70
CHEMBL361189 1 8.62
CHEMBL178870 1 8.52
CHEMBL360234 1 8.52
CHEMBL361572 1 8.52
CHEMBL181066 1 8.52
CHEMBL178234 1 8.52
CHEMBL182000 1 8.40
CHEMBL182099 1 8.30
CHEMBL180765 1 8.30
CHEMBL178767 1 8.15
CHEMBL281937 1 8.00
CHEMBL180221 1 8.00
CHEMBL180066 1 8.00
CHEMBL180826 1 7.92
CHEMBL180823 1 7.85
CHEMBL359460 1 7.75
CHEMBL178193 1 7.72
CHEMBL362220 1 7.70
CHEMBL178869 1 7.70
CHEMBL179173 1 7.57
CHEMBL178123 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362487 Ki = 0.4 nM 9.40
CHEMBL180606 Ki = 1.0 nM 9.00
CHEMBL359876 Ki = 1.0 nM 9.00
CHEMBL361180 Ki = 1.0 nM 9.00
CHEMBL179277 Ki = 1.0 nM 9.00
CHEMBL444015 Ki = 2.0 nM 8.70
CHEMBL178385 Ki = 2.0 nM 8.70
CHEMBL179592 Ki = 2.0 nM 8.70
CHEMBL444878 Ki = 2.0 nM 8.70
CHEMBL361189 Ki = 2.4 nM 8.62
CHEMBL178870 Ki = 3.0 nM 8.52
CHEMBL178234 Ki = 3.0 nM 8.52
CHEMBL181066 Ki = 3.0 nM 8.52
CHEMBL361572 Ki = 3.0 nM 8.52
CHEMBL360234 Ki = 3.0 nM 8.52
CHEMBL182000 Ki = 4.0 nM 8.40
CHEMBL182099 Ki = 5.0 nM 8.30
CHEMBL180765 Ki = 5.0 nM 8.30
CHEMBL178767 Ki = 7.0 nM 8.15
CHEMBL281937 Ki = 10.0 nM 8.00
CHEMBL180066 Ki = 10.0 nM 8.00
CHEMBL180221 Ki = 10.0 nM 8.00
CHEMBL180826 Ki = 12.0 nM 7.92
CHEMBL180823 Ki = 14.0 nM 7.85
CHEMBL359460 Ki = 18.0 nM 7.75
CHEMBL178193 Ki = 19.0 nM 7.72
CHEMBL362220 Ki = 20.0 nM 7.70
CHEMBL178869 Ki = 20.0 nM 7.70
CHEMBL179173 Ki = 27.0 nM 7.57
CHEMBL178123 Ki = 29.0 nM 7.54
CHEMBL362177 Ki = 31.0 nM 7.51
CHEMBL181425 Ki = 50.0 nM 7.30
CHEMBL181938 Ki = 54.0 nM 7.27
CHEMBL179232 Ki = 77.0 nM 7.11
CHEMBL26655 Ki = 98.0 nM 7.01
CHEMBL410710 Ki = 99.0 nM 7.00
CHEMBL359604 Ki = 118.0 nM 6.93
CHEMBL360475 Ki = 246.0 nM 6.61