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Assay Detail

CHEMBL959382

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

Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHOK1 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis of new serotonin 5-HT7 receptor ligands. Determinants of 5-HT7/5-HT1A receptor selectivity.
Medina RA, Sallander J, Benhamú B, Porras E, Campillo M, Pardo L, López-Rodríguez ML.
J Med Chem (2009) 52 : 2384 -2392
PubMed 19326916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.06 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445334 1 8.15
CHEMBL394080 1 7.50
CHEMBL489028 1 7.33
CHEMBL489029 1 7.20
CHEMBL522417 1 7.20
CHEMBL523121 1 7.17
CHEMBL506875 1 7.16
CHEMBL490645 1 7.16
CHEMBL395933 1 7.13
CHEMBL12259 UCM-5600 1 7.05
CHEMBL455210 1 6.98
CHEMBL393492 1 6.80
CHEMBL489448 1 6.80
CHEMBL489255 1 6.71
CHEMBL521973 1 6.69
CHEMBL490644 1 6.60
CHEMBL489256 1 6.46
CHEMBL521574 1 -
CHEMBL489447 1 -
CHEMBL489249 1 -
CHEMBL240774 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445334 Ki = 7.0 nM 8.15
CHEMBL394080 Ki = 32.0 nM 7.50
CHEMBL489028 Ki = 47.0 nM 7.33
CHEMBL489029 Ki = 63.0 nM 7.20
CHEMBL522417 Ki = 63.0 nM 7.20
CHEMBL523121 Ki = 68.0 nM 7.17
CHEMBL506875 Ki = 69.0 nM 7.16
CHEMBL490645 Ki = 69.0 nM 7.16
CHEMBL395933 Ki = 74.0 nM 7.13
CHEMBL12259 UCM-5600 Ki = 89.0 nM 7.05
CHEMBL455210 Ki = 105.0 nM 6.98
CHEMBL393492 Ki = 158.0 nM 6.80
CHEMBL489448 Ki = 160.0 nM 6.80
CHEMBL489255 Ki = 193.0 nM 6.71
CHEMBL521973 Ki = 203.0 nM 6.69
CHEMBL490644 Ki = 250.0 nM 6.60
CHEMBL489256 Ki = 350.0 nM 6.46
CHEMBL521574 Ki > 1000.0 nM -
CHEMBL489447 Ki > 1000.0 nM -
CHEMBL489249 Ki > 1000.0 nM -
CHEMBL240774 Ki > 1000.0 nM -