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Assay Detail

CHEMBL618118

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

Binding
Binding affinity towards human 5-hydroxytryptamine 6 receptor was evaluated using [3H]-LSD as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
Glennon RA.
J Med Chem (2003) 46 : 2795 -2812
PubMed 12825922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.68 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 9.40
CHEMBL42 CLOZAPINE 4.0 1 8.02
CHEMBL6437 MIANSERIN 4.0 1 7.26
CHEMBL39 SEROTONIN 3.0 1 7.19
CHEMBL13816 1 6.40
CHEMBL18840 1 6.14
CHEMBL267930 SPIPERONE 2.0 1 5.80
CHEMBL96729 1 5.58
CHEMBL51 KETANSERIN 3.0 1 5.55
CHEMBL18772 QUIPAZINE 2.0 1 5.44
CHEMBL56 8-OH-DPAT 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE Ki = 0.4 nM 9.40
CHEMBL42 CLOZAPINE Ki = 9.5 nM 8.02
CHEMBL6437 MIANSERIN Ki = 55.0 nM 7.26
CHEMBL39 SEROTONIN Ki = 65.0 nM 7.19
CHEMBL13816 Ki = 400.0 nM 6.40
CHEMBL18840 Ki = 720.0 nM 6.14
CHEMBL267930 SPIPERONE Ki = 1595.0 nM 5.80
CHEMBL96729 Ki = 2600.0 nM 5.58
CHEMBL51 KETANSERIN Ki = 2800.0 nM 5.55
CHEMBL18772 QUIPAZINE Ki = 3600.0 nM 5.44
CHEMBL56 8-OH-DPAT Ki > 10000.0 nM -