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Assay Detail

CHEMBL616343

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

Binding
Inhibition of [3H]2-(di-N-propylamino)-8-hydroxytetralin binding to 5-HT1A receptor of rat frontal cortex homogenates
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Frontal cortex
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A series of N4-imidoethyl derivatives of 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazine as 5-HT1A receptor ligands: synthesis and structure-affinity relationships.
van Steen BJ, van Wijngaarden I, Tulp MT, Soudijn W.
J Med Chem (1995) 38 : 4303 -4308
PubMed 7473558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.61 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335401 1 9.15
CHEMBL136494 1 8.42
CHEMBL135880 1 8.33
CHEMBL135885 1 8.32
CHEMBL138596 1 8.19
CHEMBL137482 1 8.00
CHEMBL81733 1 7.49
CHEMBL136748 1 7.20
CHEMBL137061 1 6.96
CHEMBL135888 1 6.82
CHEMBL132600 1 6.46
CHEMBL136493 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335401 Ki = 0.7079 nM 9.15
CHEMBL136494 Ki = 3.802 nM 8.42
CHEMBL135880 Ki = 4.677 nM 8.33
CHEMBL135885 Ki = 4.786 nM 8.32
CHEMBL138596 Ki = 6.457 nM 8.19
CHEMBL137482 Ki = 10.0 nM 8.00
CHEMBL81733 Ki = 32.36 nM 7.49
CHEMBL136748 Ki = 63.1 nM 7.20
CHEMBL137061 Ki = 109.65 nM 6.96
CHEMBL135888 Ki = 151.36 nM 6.82
CHEMBL132600 Ki = 346.74 nM 6.46
CHEMBL136493 Ki = 977.24 nM 6.01