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Assay Detail

CHEMBL888165

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

Binding
Displacement of [3H]LSD from rat recombinant 5HT7 receptor expressed in HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3223)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Bivalent ligand approach on 4-[2-(3-methoxyphenyl)ethyl]-1-(2-methoxyphenyl)piperazine: synthesis and binding affinities for 5-HT(7) and 5-HT(1A) receptors.
Leopoldo M, Lacivita E, Colabufo NA, Niso M, Berardi F, Perrone R.
Bioorg Med Chem (2007) 15 : 5316 -5321
PubMed 17517509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.37 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 1 9.29
CHEMBL238808 1 7.60
CHEMBL239656 1 7.54
CHEMBL395444 1 7.43
CHEMBL239231 1 7.39
CHEMBL396396 1 7.37
CHEMBL396844 1 7.37
CHEMBL396349 1 6.92
CHEMBL240729 1 6.59
CHEMBL239530 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 Ki = 0.51 nM 9.29
CHEMBL238808 Ki = 25.0 nM 7.60
CHEMBL239656 Ki = 28.5 nM 7.54
CHEMBL395444 Ki = 37.0 nM 7.43
CHEMBL239231 Ki = 41.1 nM 7.39
CHEMBL396396 Ki = 43.0 nM 7.37
CHEMBL396844 Ki = 42.6 nM 7.37
CHEMBL396349 Ki = 120.0 nM 6.92
CHEMBL240729 Ki = 258.0 nM 6.59
CHEMBL239530 Ki = 573.0 nM 6.24