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Assay Detail

CHEMBL1038009

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

Functional
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles.
Ivachtchenko AV, Frolov EB, Mitkin OD, Tkachenko SE, Okun IM, Khvat AV.
Bioorg Med Chem Lett (2010) 20 : 78 -82
PubMed 19945877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.88 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL605405 1 7.06
CHEMBL592752 MARITUPIRDINE 2.0 1 6.80
CHEMBL592271 1 6.75
CHEMBL605081 1 6.56
CHEMBL591569 1 6.26
CHEMBL589147 1 6.18
CHEMBL589148 1 6.16
CHEMBL601902 1 6.04
CHEMBL589388 1 6.01
CHEMBL592753 1 6.01
CHEMBL591570 1 6.00
CHEMBL589389 1 5.98
CHEMBL589149 1 5.95
CHEMBL589390 LATREPIRDINE 3.0 1 5.94
CHEMBL589386 1 5.84
CHEMBL592516 1 5.82
CHEMBL601304 1 5.78
CHEMBL591801 1 5.76
CHEMBL604669 1 5.70
CHEMBL603049 1 5.64
CHEMBL589150 1 5.63
CHEMBL591568 1 5.59
CHEMBL592514 1 5.55
CHEMBL604668 1 5.53
CHEMBL592751 1 5.43
CHEMBL606036 1 5.39
CHEMBL592515 1 5.25
CHEMBL599913 1 5.24
CHEMBL591803 1 4.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL605405 IC50 = 87.0 nM 7.06
CHEMBL592752 MARITUPIRDINE IC50 = 158.0 nM 6.80
CHEMBL592271 IC50 = 180.0 nM 6.75
CHEMBL605081 IC50 = 276.0 nM 6.56
CHEMBL591569 IC50 = 550.0 nM 6.26
CHEMBL589147 IC50 = 666.0 nM 6.18
CHEMBL589148 IC50 = 692.0 nM 6.16
CHEMBL601902 IC50 = 910.0 nM 6.04
CHEMBL589388 IC50 = 974.0 nM 6.01
CHEMBL592753 IC50 = 977.0 nM 6.01
CHEMBL591570 IC50 = 1000.0 nM 6.00
CHEMBL589389 IC50 = 1050.0 nM 5.98
CHEMBL589149 IC50 = 1130.0 nM 5.95
CHEMBL589390 LATREPIRDINE IC50 = 1160.0 nM 5.94
CHEMBL589386 IC50 = 1440.0 nM 5.84
CHEMBL592516 IC50 = 1500.0 nM 5.82
CHEMBL601304 IC50 = 1680.0 nM 5.78
CHEMBL591801 IC50 = 1750.0 nM 5.76
CHEMBL604669 IC50 = 1980.0 nM 5.70
CHEMBL603049 IC50 = 2270.0 nM 5.64
CHEMBL589150 IC50 = 2350.0 nM 5.63
CHEMBL591568 IC50 = 2580.0 nM 5.59
CHEMBL592514 IC50 = 2810.0 nM 5.55
CHEMBL604668 IC50 = 2950.0 nM 5.53
CHEMBL592751 IC50 = 3720.0 nM 5.43
CHEMBL606036 IC50 = 4070.0 nM 5.39
CHEMBL592515 IC50 = 5580.0 nM 5.25
CHEMBL599913 IC50 = 5730.0 nM 5.24
CHEMBL591803 IC50 = 20700.0 nM 4.68