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Assay Detail

CHEMBL3706364

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

Binding
Radioligand Binding Assay: For binding analysis vs. the human receptor, samples were incubated in 50 mM Tris-HCl, pH 7.5, 5 mM MgCl2, 1 mM EDTA (4% DMSO final) with 10 nM [N-methyl-3H]-LSD (Perkin Elmer), 2.5 ng of human 5-HT6 receptor membranes (Millipore) and 50 ug SPA beads (PVT-PEI-WGA, GE Healthcare) per well in a final volume of 0.2 mL. For binding analysis vs. the rat receptor, samples were incubated in the same buffer with 3.5 nM [N-methyl-3H]-LSD, 50 ug of rat 5-HT6 receptor membranes (Perkin Elmer) and 0.4 mg SPA beads (PVT-PEI-WGA Type B, GE Healthcare) per well also in a final volume of 0.2 mL. Binding reactions were performed in PicoPlate96 microtiter plates (Perkin Elmer) by consecutively adding 50 uL of each competing compound or buffer, SPA beads, radioligand and 5-HT6 receptor membranes. After an overnight incubation at room temperature on a Nutator mixer, plates were centrifuged for 15 min at 1,500 rpm, followed by incubation in the dark for 10 min.
ChEMBL ↗
216
Total Activities
201
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 216 8.36 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3692995 — — 1 10.30
CHEMBL3692882 — — 1 10.08
CHEMBL3692990 — — 1 10.00
CHEMBL3692968 — — 1 9.96
CHEMBL3692993 — — 1 9.96
CHEMBL3696966 — — 1 9.96
CHEMBL3692867 — — 1 9.92
CHEMBL3692910 — — 2 9.89
CHEMBL3692974 — — 1 9.89
CHEMBL3692894 — — 3 9.82
CHEMBL3692988 — — 1 9.80
CHEMBL3692989 — — 1 9.80
CHEMBL3692863 — — 1 9.77
CHEMBL3692997 — — 1 9.77
CHEMBL3692975 — — 1 9.72
CHEMBL3692971 — — 1 9.72
CHEMBL3692864 — — 1 9.70
CHEMBL3692973 — — 1 9.70
CHEMBL3692866 — — 1 9.66
CHEMBL3696953 — — 1 9.66
CHEMBL3692996 — — 1 9.64
CHEMBL3696956 — — 1 9.64
CHEMBL3692901 — — 1 9.60
CHEMBL3692942 — — 1 9.59
CHEMBL3692992 — — 1 9.57
CHEMBL3692994 — — 1 9.55
CHEMBL3693000 — — 1 9.55
CHEMBL3696954 — — 1 9.52
CHEMBL3692969 — — 1 9.49
CHEMBL3692985 — — 1 9.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3692995 — Ki = 0.05 nM 10.30
CHEMBL3692882 — Ki = 0.083 nM 10.08
CHEMBL3692990 — Ki = 0.1 nM 10.00
CHEMBL3692968 — Ki = 0.11 nM 9.96
CHEMBL3692993 — Ki = 0.11 nM 9.96
CHEMBL3696966 — Ki = 0.11 nM 9.96
CHEMBL3692867 — Ki = 0.12 nM 9.92
CHEMBL3692910 — Ki = 0.13 nM 9.89
CHEMBL3692974 — Ki = 0.13 nM 9.89
CHEMBL3692910 — Ki = 0.13 nM 9.89
CHEMBL3692894 — Ki = 0.15 nM 9.82
CHEMBL3692988 — Ki = 0.16 nM 9.80
CHEMBL3692989 — Ki = 0.16 nM 9.80
CHEMBL3692863 — Ki = 0.17 nM 9.77
CHEMBL3692997 — Ki = 0.17 nM 9.77
CHEMBL3692971 — Ki = 0.19 nM 9.72
CHEMBL3692975 — Ki = 0.19 nM 9.72
CHEMBL3692973 — Ki = 0.2 nM 9.70
CHEMBL3692864 — Ki = 0.2 nM 9.70
CHEMBL3696953 — Ki = 0.22 nM 9.66
CHEMBL3692866 — Ki = 0.22 nM 9.66
CHEMBL3692996 — Ki = 0.23 nM 9.64
CHEMBL3696956 — Ki = 0.23 nM 9.64
CHEMBL3692901 — Ki = 0.25 nM 9.60
CHEMBL3692942 — Ki = 0.26 nM 9.59
CHEMBL3692992 — Ki = 0.27 nM 9.57
CHEMBL3693000 — Ki = 0.28 nM 9.55
CHEMBL3692994 — Ki = 0.28 nM 9.55
CHEMBL3696954 — Ki = 0.3 nM 9.52
CHEMBL3692969 — Ki = 0.32 nM 9.49
CHEMBL3692985 — Ki = 0.32 nM 9.49
CHEMBL3692991 — Ki = 0.33 nM 9.48
CHEMBL3696967 — Ki = 0.33 nM 9.48
CHEMBL3692984 — Ki = 0.35 nM 9.46
CHEMBL3692859 — Ki = 0.35 nM 9.46
CHEMBL3692894 — Ki = 0.35 nM 9.46
CHEMBL3692986 — Ki = 0.36 nM 9.44
CHEMBL3692999 — Ki = 0.39 nM 9.41
CHEMBL3692860 — Ki = 0.39 nM 9.41
CHEMBL3696962 — Ki = 0.4 nM 9.40
CHEMBL3639918 — Ki = 0.4 nM 9.40
CHEMBL3692986 — Ki = 0.41 nM 9.39
CHEMBL3692856 — Ki = 0.42 nM 9.38
CHEMBL3692858 — Ki = 0.48 nM 9.32
CHEMBL3692966 — Ki = 0.48 nM 9.32
CHEMBL3692970 — Ki = 0.49 nM 9.31
CHEMBL3692986 — Ki = 0.49 nM 9.31
CHEMBL3696952 — Ki = 0.5 nM 9.30
CHEMBL3692857 — Ki = 0.55 nM 9.26
CHEMBL3692943 — Ki = 0.55 nM 9.26