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Assay Detail

CHEMBL1936932

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

Functional
Antagonist activity at human recombinant 5-HT6 receptor expressed human astrocytoma cells assessed as inhibition of 5-HT-induced cAMP accumulation after 1 hr preincubation by HTRF assay
10
Total Activities
10
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

Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
Sundar BG, Bailey TR, Dunn DD, Bacon ER, Salvino JM, Morton GC, Aimone LD, Zeqi H, Mathiasen JR, Dicamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Brown R, Qian J, Angeles T, Connors T, Spais C, Holskin B, Galinis D, Duzic E, Schaffhauser H, Rosse GC.
Bioorg Med Chem Lett (2012) 22 : 120 -123
PubMed 22153937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.77 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1935590 1 8.44
CHEMBL1935599 1 8.17
CHEMBL1935589 1 8.07
CHEMBL1935601 1 8.01
CHEMBL1935594 1 7.93
CHEMBL1935592 1 7.68
CHEMBL1935600 1 7.50
CHEMBL1935593 1 7.47
CHEMBL1935597 1 7.27
CHEMBL1935595 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1935590 IC50 = 3.6 nM 8.44
CHEMBL1935599 IC50 = 6.8 nM 8.17
CHEMBL1935589 IC50 = 8.5 nM 8.07
CHEMBL1935601 IC50 = 9.8 nM 8.01
CHEMBL1935594 IC50 = 11.7 nM 7.93
CHEMBL1935592 IC50 = 21.0 nM 7.68
CHEMBL1935600 IC50 = 32.0 nM 7.50
CHEMBL1935593 IC50 = 34.0 nM 7.47
CHEMBL1935597 IC50 = 54.0 nM 7.27
CHEMBL1935595 IC50 = 68.6 nM 7.16