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Assay Detail

CHEMBL839441

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

Binding
Binding affinity against h5-HT6 receptor transiently expressed in HEK293 cells
16
Total Activities
16
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

Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Abate C, Kolanos R, Dukat M, Setola V, Roth BL, Glennon RA.
Bioorg Med Chem Lett (2005) 15 : 3510 -3513
PubMed 15990303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.53 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187865 1 9.52
CHEMBL373107 1 8.77
CHEMBL76237 1 8.70
CHEMBL93868 1 8.40
CHEMBL188144 1 8.22
CHEMBL188864 1 8.11
CHEMBL554369 1 8.04
CHEMBL361892 1 8.00
CHEMBL433765 1 7.54
CHEMBL186621 1 7.50
CHEMBL188285 1 7.34
CHEMBL539589 1 7.22
CHEMBL539587 1 6.26
CHEMBL539327 1 6.19
CHEMBL534703 1 5.62
CHEMBL554985 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187865 Ki = 0.3 nM 9.52
CHEMBL373107 Ki = 1.7 nM 8.77
CHEMBL76237 Ki = 2.0 nM 8.70
CHEMBL93868 Ki = 4.0 nM 8.40
CHEMBL188144 Ki = 6.0 nM 8.22
CHEMBL188864 Ki = 7.8 nM 8.11
CHEMBL554369 Ki = 9.1 nM 8.04
CHEMBL361892 Ki = 9.9 nM 8.00
CHEMBL433765 Ki = 29.0 nM 7.54
CHEMBL186621 Ki = 32.0 nM 7.50
CHEMBL188285 Ki = 46.0 nM 7.34
CHEMBL539589 Ki = 60.0 nM 7.22
CHEMBL539587 Ki = 550.0 nM 6.26
CHEMBL539327 Ki = 640.0 nM 6.19
CHEMBL534703 Ki = 2400.0 nM 5.62
CHEMBL554985 Ki = 8750.0 nM 5.06