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Assay Detail

CHEMBL927702

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

Binding
Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells
36
Total Activities
36
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 Intermediate

Target

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

Publication

Discovery of 3-aryl-3-methyl-1H-quinoline-2,4-diones as a new class of selective 5-HT6 receptor antagonists.
Seong CM, Park WK, Park CM, Kong JY, Park NS.
Bioorg Med Chem Lett (2008) 18 : 738 -743
PubMed 18053713 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.16 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23038 1 9.00
CHEMBL431298 1 9.00
CHEMBL95136 1 8.85
CHEMBL76237 1 8.64
CHEMBL329383 1 8.52
CHEMBL401970 1 8.04
CHEMBL253708 1 7.91
CHEMBL253095 1 7.55
CHEMBL404352 1 7.52
CHEMBL254298 1 7.26
CHEMBL433461 1 7.26
CHEMBL251857 1 7.13
CHEMBL253718 1 7.11
CHEMBL253096 1 7.08
CHEMBL253502 1 6.83
CHEMBL253709 1 6.81
CHEMBL252673 1 6.71
CHEMBL401969 1 6.59
CHEMBL254330 1 6.53
CHEMBL403843 1 6.52
CHEMBL252902 1 6.46
CHEMBL402810 1 6.46
CHEMBL46071 1 6.29
CHEMBL251861 1 6.15
CHEMBL404552 1 6.14
CHEMBL252496 1 6.06
CHEMBL254331 1 6.05
CHEMBL253061 1 6.02
CHEMBL404538 1 -
CHEMBL253097 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23038 Ki = 1.0 nM 9.00
CHEMBL431298 Ki = 1.0 nM 9.00
CHEMBL95136 Ki = 1.4 nM 8.85
CHEMBL76237 Ki = 2.3 nM 8.64
CHEMBL329383 Ki = 3.0 nM 8.52
CHEMBL401970 Ki = 9.2 nM 8.04
CHEMBL253708 Ki = 12.3 nM 7.91
CHEMBL253095 Ki = 28.3 nM 7.55
CHEMBL404352 Ki = 30.1 nM 7.52
CHEMBL433461 Ki = 55.0 nM 7.26
CHEMBL254298 Ki = 54.7 nM 7.26
CHEMBL251857 Ki = 73.2 nM 7.13
CHEMBL253718 Ki = 77.5 nM 7.11
CHEMBL253096 Ki = 82.4 nM 7.08
CHEMBL253502 Ki = 147.0 nM 6.83
CHEMBL253709 Ki = 156.0 nM 6.81
CHEMBL252673 Ki = 196.9 nM 6.71
CHEMBL401969 Ki = 257.0 nM 6.59
CHEMBL254330 Ki = 293.0 nM 6.53
CHEMBL403843 Ki = 304.0 nM 6.52
CHEMBL252902 Ki = 346.0 nM 6.46
CHEMBL402810 Ki = 344.6 nM 6.46
CHEMBL46071 Ki = 512.0 nM 6.29
CHEMBL251861 Ki = 715.0 nM 6.15
CHEMBL404552 Ki = 728.0 nM 6.14
CHEMBL252496 Ki = 877.0 nM 6.06
CHEMBL254331 Ki = 893.0 nM 6.05
CHEMBL253061 Ki = 952.0 nM 6.02
CHEMBL404538 Ki > 1000.0 nM -
CHEMBL253097 Ki > 1000.0 nM -
CHEMBL253513 Ki > 1000.0 nM -
CHEMBL402292 Ki > 1000.0 nM -
CHEMBL402380 Ki > 1000.0 nM -
CHEMBL253271 Ki > 1000.0 nM -
CHEMBL253281 Ki > 1000.0 nM -
CHEMBL401707 Ki > 1000.0 nM -