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Assay Detail

CHEMBL1953152

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

Functional
Antagonist activity at human 5HT6 receptor expressed in human astrocytoma cells assessed as inhibition of cAMP production
18
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.
Tripathy R, McHugh RJ, Bacon ER, Salvino JM, Morton GC, Aimone LD, Huang Z, Mathiasen JR, DiCamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Qian J, Angeles TS, Connors T, Spais C, Holskin B, Duzic E, Schaffhauser H, Rossé GC.
Bioorg Med Chem Lett (2012) 22 : 1421 -1426
PubMed 22226656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.92 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1949928 2 8.22
CHEMBL1949764 1 7.57
CHEMBL1949763 1 7.48
CHEMBL1949930 2 7.35
CHEMBL1949927 2 7.20
CHEMBL1949773 2 7.02
CHEMBL1949761 1 6.88
CHEMBL1949762 1 6.87
CHEMBL1949760 1 6.75
CHEMBL1949765 1 6.64
CHEMBL1949772 1 6.61
CHEMBL1949767 1 6.55
CHEMBL1949768 1 6.51
CHEMBL1949766 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1949928 IC50 = 6.0 nM 8.22
CHEMBL1949764 IC50 = 27.0 nM 7.57
CHEMBL1949763 IC50 = 33.0 nM 7.48
CHEMBL1949928 IC50 = 40.0 nM 7.40
CHEMBL1949930 IC50 = 45.0 nM 7.35
CHEMBL1949927 IC50 = 63.0 nM 7.20
CHEMBL1949930 IC50 = 67.0 nM 7.17
CHEMBL1949773 IC50 = 96.0 nM 7.02
CHEMBL1949761 IC50 = 133.0 nM 6.88
CHEMBL1949762 IC50 = 135.0 nM 6.87
CHEMBL1949760 IC50 = 179.0 nM 6.75
CHEMBL1949765 IC50 = 227.0 nM 6.64
CHEMBL1949772 IC50 = 245.0 nM 6.61
CHEMBL1949767 IC50 = 281.0 nM 6.55
CHEMBL1949768 IC50 = 306.0 nM 6.51
CHEMBL1949766 IC50 = 357.0 nM 6.45
CHEMBL1949927 IC50 = 790.0 nM 6.10
CHEMBL1949773 IC50 = 1363.0 nM 5.87