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Assay Detail

CHEMBL615589

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

Binding
Displacement of [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor of rat hippocampal membranes
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.
el Ahmad Y, Laurent E, Maillet P, Talab A, Teste JF, Dokhan R, Tran G, Ollivier R.
J Med Chem (1997) 40 : 952 -960
PubMed 9083484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.37 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL354210 2 9.40
CHEMBL56 8-OH-DPAT 1 9.30
CHEMBL368061 3 9.30
CHEMBL177031 3 8.40
CHEMBL49 BUSPIRONE 4.0 1 8.15
CHEMBL366388 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL354210 Ki = 0.4 nM 9.40
CHEMBL56 8-OH-DPAT Ki = 0.5 nM 9.30
CHEMBL368061 Ki = 0.5 nM 9.30
CHEMBL354210 Ki = 1.1 nM 8.96
CHEMBL368061 Ki = 1.5 nM 8.82
CHEMBL177031 Ki = 4.0 nM 8.40
CHEMBL49 BUSPIRONE Ki = 7.0 nM 8.15
CHEMBL177031 Ki = 10.0 nM 8.00
CHEMBL366388 Ki = 17.0 nM 7.77
CHEMBL368061 Ki = 50.0 nM 7.30
CHEMBL177031 Ki = 210.0 nM 6.68