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Assay Detail

CHEMBL830434

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

Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HeLa cells
ChEMBL ↗
49
Total Activities
49
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

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Cole DC, Lennox WJ, Lombardi S, Ellingboe JW, Bernotas RC, Tawa GJ, Mazandarani H, Smith DL, Zhang G, Coupet J, Schechter LE.
J Med Chem (2005) 48 : 353 -356
PubMed 15658848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 8.47 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL609994 — — 1 9.52
CHEMBL606556 — — 1 9.40
CHEMBL606559 — — 1 9.40
CHEMBL609995 — — 1 9.00
CHEMBL609992 — — 1 9.00
CHEMBL606547 — — 1 9.00
CHEMBL606557 — — 1 9.00
CHEMBL610254 — — 1 9.00
CHEMBL606558 — — 1 9.00
CHEMBL606548 — — 1 9.00
CHEMBL606636 — — 1 9.00
CHEMBL609741 — — 1 9.00
CHEMBL610253 — — 1 9.00
CHEMBL609996 — — 1 9.00
CHEMBL2113386 — — 1 9.00
CHEMBL606546 — — 1 9.00
CHEMBL606817 — — 1 9.00
CHEMBL606638 — — 1 9.00
CHEMBL606637 — — 1 9.00
CHEMBL610256 — — 1 8.70
CHEMBL606639 — — 1 8.70
CHEMBL606549 — — 1 8.52
CHEMBL610257 — — 1 8.52
CHEMBL606704 — — 1 8.52
CHEMBL609743 — — 1 8.52
CHEMBL609742 — — 1 8.52
CHEMBL609737 — — 1 8.40
CHEMBL609738 — — 1 8.40
CHEMBL609740 — — 1 8.40
CHEMBL606703 — — 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL609994 — Ki = 0.3 nM 9.52
CHEMBL606556 — Ki = 0.4 nM 9.40
CHEMBL606559 — Ki = 0.4 nM 9.40
CHEMBL606638 — Ki = 1.0 nM 9.00
CHEMBL609992 — Ki = 1.0 nM 9.00
CHEMBL606547 — Ki = 1.0 nM 9.00
CHEMBL606557 — Ki = 1.0 nM 9.00
CHEMBL609995 — Ki = 1.0 nM 9.00
CHEMBL610254 — Ki = 1.0 nM 9.00
CHEMBL606558 — Ki = 1.0 nM 9.00
CHEMBL606548 — Ki = 1.0 nM 9.00
CHEMBL606636 — Ki = 1.0 nM 9.00
CHEMBL606637 — Ki = 1.0 nM 9.00
CHEMBL609741 — Ki = 1.0 nM 9.00
CHEMBL610253 — Ki = 1.0 nM 9.00
CHEMBL609996 — Ki = 1.0 nM 9.00
CHEMBL2113386 — Ki = 1.0 nM 9.00
CHEMBL606546 — Ki = 1.0 nM 9.00
CHEMBL606817 — Ki = 1.0 nM 9.00
CHEMBL606639 — Ki = 2.0 nM 8.70
CHEMBL610256 — Ki = 2.0 nM 8.70
CHEMBL609742 — Ki = 3.0 nM 8.52
CHEMBL609743 — Ki = 3.0 nM 8.52
CHEMBL610257 — Ki = 3.0 nM 8.52
CHEMBL606549 — Ki = 3.0 nM 8.52
CHEMBL606704 — Ki = 3.0 nM 8.52
CHEMBL609737 — Ki = 4.0 nM 8.40
CHEMBL609738 — Ki = 4.0 nM 8.40
CHEMBL609740 — Ki = 4.0 nM 8.40
CHEMBL606703 — Ki = 4.0 nM 8.40
CHEMBL609991 — Ki = 4.0 nM 8.40
CHEMBL609993 — Ki = 5.0 nM 8.30
CHEMBL609739 — Ki = 5.0 nM 8.30
CHEMBL606818 — Ki = 7.0 nM 8.15
CHEMBL606816 — Ki = 8.0 nM 8.10
CHEMBL606705 — Ki = 8.0 nM 8.10
CHEMBL610259 — Ki = 9.0 nM 8.05
CHEMBL610255 — Ki = 9.0 nM 8.05
CHEMBL606815 — Ki = 10.0 nM 8.00
CHEMBL606764 — Ki = 11.0 nM 7.96
CHEMBL606765 — Ki = 12.0 nM 7.92
CHEMBL606706 — Ki = 16.0 nM 7.80
CHEMBL606763 — Ki = 22.0 nM 7.66
CHEMBL610258 — Ki = 24.0 nM 7.62
CHEMBL606766 — Ki = 34.0 nM 7.47
CHEMBL609736 — Ki = 35.0 nM 7.46
CHEMBL606868 — Ki = 36.0 nM 7.44
CHEMBL606870 — Ki = 57.0 nM 7.24
CHEMBL606871 — Ki = 131.0 nM 6.88