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Assay Detail

CHEMBL1006687

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

Binding
Displacement of [3H]8-OHDPAT from 5HT1A receptor in rat hippocampus
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Specific targeting of peripheral serotonin 5-HT(3) receptors. Synthesis, biological investigation, and structure-activity relationships.
Morelli E, Gemma S, Budriesi R, Campiani G, Novellino E, Fattorusso C, Catalanotti B, Coccone SS, Ros S, Borrelli G, Persico M, Fiorini I, Nacci V, Ioan P, Chiarini A, Hamon M, Cagnotto A, Mennini T, Fracasso C, Colovic M, Caccia S, Butini S.
J Med Chem (2009) 52 : 3548 -3562
PubMed 19425598 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.83 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.80
CHEMBL341474 1 6.86
CHEMBL511555 1 6.35
CHEMBL466462 1 6.32
CHEMBL18772 QUIPAZINE 2.0 1 5.80
CHEMBL523716 1 -
CHEMBL468498 1 -
CHEMBL136978 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN Ki = 1.6 nM 8.80
CHEMBL341474 Ki = 138.0 nM 6.86
CHEMBL511555 Ki = 446.0 nM 6.35
CHEMBL466462 Ki = 480.0 nM 6.32
CHEMBL18772 QUIPAZINE Ki = 1584.0 nM 5.80
CHEMBL523716 Ki > 10000.0 nM -
CHEMBL468498 Ki > 10000.0 nM -
CHEMBL136978 Ki > 10000.0 nM -