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Assay Detail

CHEMBL618094

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

Binding
Binding affinity as displacement of [3H]5-HT binding to 5-hydroxytryptamine 6 receptor in HeLa cells.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HeLa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.
Russell MG, Baker RJ, Barden L, Beer MS, Bristow L, Broughton HB, Knowles M, McAllister G, Patel S, Castro JL.
J Med Chem (2001) 44 : 3881 -3895
PubMed 11689074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.53 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329329 1 8.89
CHEMBL92139 1 8.82
CHEMBL76237 1 8.64
CHEMBL125745 1 8.62
CHEMBL93868 1 8.54
CHEMBL126340 1 8.52
CHEMBL127411 1 8.14
CHEMBL127636 1 8.10
CHEMBL339741 1 8.08
CHEMBL75010 1 8.01
CHEMBL129614 1 7.96
CHEMBL126374 1 7.92
CHEMBL72574 1 7.77
CHEMBL112024 1 7.72
CHEMBL317535 1 7.70
CHEMBL316881 1 7.60
CHEMBL76466 1 7.58
CHEMBL127089 1 7.48
CHEMBL339337 1 7.40
CHEMBL127975 1 7.36
CHEMBL127732 1 7.35
CHEMBL263700 1 7.27
CHEMBL124971 1 7.20
CHEMBL7143 1 7.05
CHEMBL338290 1 6.89
CHEMBL124382 1 6.58
CHEMBL341495 1 6.50
CHEMBL126263 1 6.46
CHEMBL126420 1 6.43
CHEMBL338380 1 6.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329329 Ki = 1.3 nM 8.89
CHEMBL92139 Ki = 1.5 nM 8.82
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL125745 Ki = 2.4 nM 8.62
CHEMBL93868 Ki = 2.9 nM 8.54
CHEMBL126340 Ki = 3.0 nM 8.52
CHEMBL127411 Ki = 7.2 nM 8.14
CHEMBL127636 Ki = 7.9 nM 8.10
CHEMBL339741 Ki = 8.3 nM 8.08
CHEMBL75010 Ki = 9.8 nM 8.01
CHEMBL129614 Ki = 11.0 nM 7.96
CHEMBL126374 Ki = 12.0 nM 7.92
CHEMBL72574 Ki = 17.0 nM 7.77
CHEMBL112024 Ki = 19.0 nM 7.72
CHEMBL317535 Ki = 20.0 nM 7.70
CHEMBL316881 Ki = 25.0 nM 7.60
CHEMBL76466 Ki = 26.0 nM 7.58
CHEMBL127089 Ki = 33.0 nM 7.48
CHEMBL339337 Ki = 40.0 nM 7.40
CHEMBL127975 Ki = 44.0 nM 7.36
CHEMBL127732 Ki = 45.0 nM 7.35
CHEMBL263700 Ki = 54.0 nM 7.27
CHEMBL124971 Ki = 63.0 nM 7.20
CHEMBL7143 Ki = 89.0 nM 7.05
CHEMBL338290 Ki = 130.0 nM 6.89
CHEMBL124382 Ki = 260.0 nM 6.58
CHEMBL341495 Ki = 320.0 nM 6.50
CHEMBL126263 Ki = 350.0 nM 6.46
CHEMBL126420 Ki = 370.0 nM 6.43
CHEMBL338380 Ki = 490.0 nM 6.31
CHEMBL127232 Ki = 620.0 nM 6.21
CHEMBL339913 Ki = 1700.0 nM 5.77