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Assay Detail

CHEMBL3240451

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

Binding
Displacement of [3H]-LSD from human recombinant 5-HT6 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.
Handzlik J, Bojarski AJ, Satała G, Kubacka M, Sadek B, Ashoor A, Siwek A, Więcek M, Kucwaj K, Filipek B, Kieć-Kononowicz K.
Eur J Med Chem (2014) 78 : 324 -339
PubMed 24691057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.47 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 8.15
CHEMBL3233677 1 6.50
CHEMBL3233676 1 6.40
CHEMBL3233675 1 5.75
CHEMBL3233672 1 5.71
CHEMBL3233671 1 5.60
CHEMBL3233678 1 5.54
CHEMBL3233670 1 5.53
CHEMBL3233402 1 5.51
CHEMBL2079256 1 5.45
CHEMBL3233401 1 5.38
CHEMBL3233668 1 5.36
CHEMBL3233673 1 5.13
CHEMBL3233674 1 5.09
CHEMBL3233669 1 5.07
CHEMBL3233665 1 5.02
CHEMBL3233679 1 4.97
CHEMBL3233667 1 4.83
CHEMBL1916746 1 4.69
CHEMBL3233666 1 4.59
CHEMBL1916745 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Ki = 7.0 nM 8.15
CHEMBL3233677 Ki = 314.0 nM 6.50
CHEMBL3233676 Ki = 395.0 nM 6.40
CHEMBL3233675 Ki = 1762.0 nM 5.75
CHEMBL3233672 Ki = 1945.0 nM 5.71
CHEMBL3233671 Ki = 2506.0 nM 5.60
CHEMBL3233678 Ki = 2879.0 nM 5.54
CHEMBL3233670 Ki = 2926.0 nM 5.53
CHEMBL3233402 Ki = 3071.0 nM 5.51
CHEMBL2079256 Ki = 3567.0 nM 5.45
CHEMBL3233401 Ki = 4139.0 nM 5.38
CHEMBL3233668 Ki = 4368.0 nM 5.36
CHEMBL3233673 Ki = 7469.0 nM 5.13
CHEMBL3233674 Ki = 8104.0 nM 5.09
CHEMBL3233669 Ki = 8611.0 nM 5.07
CHEMBL3233665 Ki = 9600.0 nM 5.02
CHEMBL3233679 Ki = 10790.0 nM 4.97
CHEMBL3233667 Ki = 14650.0 nM 4.83
CHEMBL1916746 Ki = 20410.0 nM 4.69
CHEMBL3233666 Ki = 25520.0 nM 4.59
CHEMBL1916745 Ki = 29070.0 nM 4.54