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Assay Detail

CHEMBL3744654

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

Binding
Displacement of [3H]-5-carboxyamidotryptamine from human serotonin 5-HT7B receptor expressed in HEK293 cells after 1 hr by microplate reader based assay
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 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7receptor antagonists and their psychotropic properties
Zajdel P, Canale V, Partyka A, Marciniec K, Kurczab R, Sataa G, Siwek A, Jastrzebska-Wiesek M, Wesoowska A, Kos T, Popik P, Bojarski AJ
Medchemcomm (2015) 6 : 1272 -1277
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.79 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3740055 1 8.22
CHEMBL3740801 1 8.15
CHEMBL2159466 1 8.15
CHEMBL3740913 1 8.15
CHEMBL3739680 1 8.15
CHEMBL3739582 1 8.10
CHEMBL3740235 1 8.10
CHEMBL3742251 1 8.10
CHEMBL3741445 1 8.05
CHEMBL3740054 1 8.05
CHEMBL2159309 1 7.92
CHEMBL3739745 1 7.72
CHEMBL3741281 1 7.72
CHEMBL3739561 1 7.68
CHEMBL3742257 1 7.62
CHEMBL3741657 1 7.55
CHEMBL3740302 1 7.44
CHEMBL3741279 1 7.38
CHEMBL3740209 1 7.36
CHEMBL3740691 1 7.31
CHEMBL3740624 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3740055 Ki = 6.0 nM 8.22
CHEMBL3740801 Ki = 7.0 nM 8.15
CHEMBL2159466 Ki = 7.0 nM 8.15
CHEMBL3740913 Ki = 7.0 nM 8.15
CHEMBL3739680 Ki = 7.0 nM 8.15
CHEMBL3739582 Ki = 8.0 nM 8.10
CHEMBL3740235 Ki = 8.0 nM 8.10
CHEMBL3742251 Ki = 8.0 nM 8.10
CHEMBL3741445 Ki = 9.0 nM 8.05
CHEMBL3740054 Ki = 9.0 nM 8.05
CHEMBL2159309 Ki = 12.0 nM 7.92
CHEMBL3739745 Ki = 19.0 nM 7.72
CHEMBL3741281 Ki = 19.0 nM 7.72
CHEMBL3739561 Ki = 21.0 nM 7.68
CHEMBL3742257 Ki = 24.0 nM 7.62
CHEMBL3741657 Ki = 28.0 nM 7.55
CHEMBL3740302 Ki = 36.0 nM 7.44
CHEMBL3741279 Ki = 42.0 nM 7.38
CHEMBL3740209 Ki = 44.0 nM 7.36
CHEMBL3740691 Ki = 49.0 nM 7.31
CHEMBL3740624 Ki = 200.0 nM 6.70