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Assay Detail

CHEMBL2443393

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

Binding
Displacement of [3H]5-CT from human 5HT7A receptor expressed in HEK293 cells after 60 mins
6
Total Activities
6
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

Novel highly potent serotonin 5-HT7 receptor ligands: structural modifications to improve pharmacokinetic properties.
Lacivita E, Di Pilato P, Stama ML, Colabufo NA, Berardi F, Perrone R, De Filippis B, Laviola G, Adriani W, Niso M, Leopoldo M.
Bioorg Med Chem Lett (2013) 23 : 6083 -6086
PubMed 24100077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.78 7.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2442996 1 7.95
CHEMBL2442995 1 7.90
CHEMBL2442994 1 7.82
CHEMBL2442999 1 7.75
CHEMBL2442997 1 7.63
CHEMBL2442998 1 7.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2442996 Ki = 11.2 nM 7.95
CHEMBL2442995 Ki = 12.7 nM 7.90
CHEMBL2442994 Ki = 15.2 nM 7.82
CHEMBL2442999 Ki = 18.0 nM 7.75
CHEMBL2442997 Ki = 23.5 nM 7.63
CHEMBL2442998 Ki = 23.8 nM 7.62