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Assay Detail

CHEMBL619052

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Binding
Binding affinity towards 5-hydroxytryptamine 7 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

First pharmacophoric hypothesis for 5-HT7 antagonism.
López-Rodríguez ML, Porras E, Benhamú B, Ramos JA, Morcillo MJ, Lavandera JL.
Bioorg Med Chem Lett (2000) 10 : 1097 -1100
PubMed 10843226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.90 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428892 1 9.00
CHEMBL12624 SB-258741 1 8.50
CHEMBL19215 METERGOLINE 2.0 1 8.20
CHEMBL12314 MESULERGINE 2.0 1 8.10
CHEMBL274384 1 8.00
CHEMBL1065 METHYSERGIDE 4.0 1 7.90
CHEMBL42 CLOZAPINE 4.0 1 7.90
CHEMBL267777 RITANSERIN 2.0 1 7.80
CHEMBL267930 SPIPERONE 2.0 1 7.70
CHEMBL516 CYPROHEPTADINE 4.0 1 7.30
CHEMBL6066838 1 7.20
CHEMBL6437 MIANSERIN 4.0 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428892 Ki = 1.0 nM 9.00
CHEMBL12624 SB-258741 Ki = 3.162 nM 8.50
CHEMBL19215 METERGOLINE Ki = 6.31 nM 8.20
CHEMBL12314 MESULERGINE Ki = 7.943 nM 8.10
CHEMBL274384 Ki = 10.0 nM 8.00
CHEMBL1065 METHYSERGIDE Ki = 12.59 nM 7.90
CHEMBL42 CLOZAPINE Ki = 12.59 nM 7.90
CHEMBL267777 RITANSERIN Ki = 15.85 nM 7.80
CHEMBL267930 SPIPERONE Ki = 19.95 nM 7.70
CHEMBL516 CYPROHEPTADINE Ki = 50.12 nM 7.30
CHEMBL6066838 Ki = 63.1 nM 7.20
CHEMBL6437 MIANSERIN Ki = 63.1 nM 7.20