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Assay Detail

CHEMBL3373147

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

Binding
Displacement of [3H]HT from human 5-HT7 receptor expressed in CHO cells by liquid scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT₂B and 5-HT₇ receptor antagonists. Part 2.
Moritomo A, Yamada H, Watanabe T, Itahana H, Koga Y, Akuzawa S, Okada M.
Bioorg Med Chem (2014) 22 : 4323 -4337
PubMed 24916029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.65 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3310714 1 8.64
CHEMBL3310713 1 8.40
CHEMBL3310113 1 8.39
CHEMBL3310122 1 8.39
CHEMBL3310123 1 8.37
CHEMBL3310111 1 7.85
CHEMBL3139188 1 7.75
CHEMBL3310112 1 7.54
CHEMBL3310115 1 7.48
CHEMBL3310117 1 7.39
CHEMBL3310109 1 7.39
CHEMBL3310120 1 7.37
CHEMBL3310118 1 7.30
CHEMBL3310121 1 7.24
CHEMBL3310116 1 7.06
CHEMBL3310114 1 6.80
CHEMBL3310119 1 6.75
CHEMBL3310110 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3310714 Ki = 2.3 nM 8.64
CHEMBL3310713 Ki = 4.0 nM 8.40
CHEMBL3310113 Ki = 4.1 nM 8.39
CHEMBL3310122 Ki = 4.1 nM 8.39
CHEMBL3310123 Ki = 4.3 nM 8.37
CHEMBL3310111 Ki = 14.0 nM 7.85
CHEMBL3139188 Ki = 18.0 nM 7.75
CHEMBL3310112 Ki = 29.0 nM 7.54
CHEMBL3310115 Ki = 33.0 nM 7.48
CHEMBL3310117 Ki = 41.0 nM 7.39
CHEMBL3310109 Ki = 41.0 nM 7.39
CHEMBL3310120 Ki = 43.0 nM 7.37
CHEMBL3310118 Ki = 50.0 nM 7.30
CHEMBL3310121 Ki = 57.0 nM 7.24
CHEMBL3310116 Ki = 87.0 nM 7.06
CHEMBL3310114 Ki = 160.0 nM 6.80
CHEMBL3310119 Ki = 180.0 nM 6.75
CHEMBL3310110 Ki > 1000.0 nM -