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Assay Detail

CHEMBL616951

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

Binding
Binding affinity at 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT in rat brain.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

A 3-D model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogues of 8-hydroxy-2-(dipropylamino)tetralin.
Mellin C, Vallgårda J, Nelson DL, Björk L, Yu H, Andén NE, Csöregh I, Arvidsson LE, Hacksell U.
J Med Chem (1991) 34 : 497 -510
PubMed 1995871 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.08 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL505765 1 8.50
CHEMBL541621 1 8.21
CHEMBL2368632 1 8.10
CHEMBL545095 1 6.82
CHEMBL542510 1 6.41
CHEMBL542753 1 5.86
CHEMBL544668 1 5.69
CHEMBL555263 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL505765 Ki = 3.18 nM 8.50
CHEMBL541621 Ki = 6.11 nM 8.21
CHEMBL2368632 Ki = 8.04 nM 8.10
CHEMBL545095 Ki = 151.0 nM 6.82
CHEMBL542510 Ki = 394.0 nM 6.41
CHEMBL542753 Ki = 1389.0 nM 5.86
CHEMBL544668 Ki = 2021.0 nM 5.69
CHEMBL555263 Ki > 10000.0 nM -