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Assay Detail

CHEMBL615958

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

Binding
Displacement of [3H]2-(di-N-propylamino)-8-hydroxytetralin from central 5-hydroxytryptamine 1A receptor recognition sites in rat frontal cortex homogenates.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands.
Kuipers W, van Wijngaarden I, Kruse CG, ter Horst-van Amstel M, Tulp MT, IJzerman AP.
J Med Chem (1995) 38 : 1942 -1954
PubMed 7783126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.07 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294456 1 8.28
CHEMBL61242 1 8.24
CHEMBL60809 1 8.00
CHEMBL434784 1 7.92
CHEMBL61028 1 7.89
CHEMBL61032 1 7.89
CHEMBL277120 1 7.75
CHEMBL305308 1 7.75
CHEMBL57583 1 7.55
CHEMBL301049 1 7.46
CHEMBL282614 ELTOPRAZINE 2.0 1 7.40
CHEMBL301451 1 7.14
CHEMBL301644 1 7.08
CHEMBL432134 1 6.98
CHEMBL291572 1 6.92
CHEMBL59340 1 6.89
CHEMBL62195 1 6.85
CHEMBL9666 1 6.77
CHEMBL60803 1 6.70
CHEMBL60341 1 6.70
CHEMBL59396 1 6.66
CHEMBL303771 1 6.66
CHEMBL58591 1 6.52
CHEMBL59597 1 6.50
CHEMBL61438 1 6.37
CHEMBL9434 PHENYLPIPERAZINE 1 6.30
CHEMBL58963 1 6.00
CHEMBL59517 1 4.70
CHEMBL60340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294456 Ki = 5.2 nM 8.28
CHEMBL61242 Ki = 5.8 nM 8.24
CHEMBL60809 Ki = 9.9 nM 8.00
CHEMBL434784 Ki = 12.0 nM 7.92
CHEMBL61028 Ki = 13.0 nM 7.89
CHEMBL61032 Ki = 13.0 nM 7.89
CHEMBL277120 Ki = 18.0 nM 7.75
CHEMBL305308 Ki = 18.0 nM 7.75
CHEMBL57583 Ki = 28.0 nM 7.55
CHEMBL301049 Ki = 35.0 nM 7.46
CHEMBL282614 ELTOPRAZINE Ki = 40.0 nM 7.40
CHEMBL301451 Ki = 73.0 nM 7.14
CHEMBL301644 Ki = 84.0 nM 7.08
CHEMBL432134 Ki = 105.0 nM 6.98
CHEMBL291572 Ki = 120.0 nM 6.92
CHEMBL59340 Ki = 130.0 nM 6.89
CHEMBL62195 Ki = 140.0 nM 6.85
CHEMBL9666 Ki = 170.0 nM 6.77
CHEMBL60803 Ki = 200.0 nM 6.70
CHEMBL60341 Ki = 200.0 nM 6.70
CHEMBL59396 Ki = 220.0 nM 6.66
CHEMBL303771 Ki = 220.0 nM 6.66
CHEMBL58591 Ki = 300.0 nM 6.52
CHEMBL59597 Ki = 320.0 nM 6.50
CHEMBL61438 Ki = 430.0 nM 6.37
CHEMBL9434 PHENYLPIPERAZINE Ki = 500.0 nM 6.30
CHEMBL58963 Ki = 1000.0 nM 6.00
CHEMBL59517 Ki = 20000.0 nM 4.70
CHEMBL60340 Ki > 10000.0 nM -