Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL616152

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

Binding
Inhibition of [3H]8-OH-DPAT binding to 5-hydroxytryptamine 1A receptor of rat frontal cortex membranes
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Functional characteristics of a series of N4-substituted 1-(2,3-dihydro-1,4-benzodioxin-5-yl)piperazines as 5-HT1A receptor ligands. Structure-activity relationships.
van Steen BJ, van Wijngaarden I, Ronken E, Soudijn W.
Bioorg Med Chem Lett (1998) 8 : 2457 -2462
PubMed 9873561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.98 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311015 1 9.64
CHEMBL312339 1 9.54
CHEMBL81728 1 9.53
CHEMBL311275 1 9.49
CHEMBL82215 1 9.17
CHEMBL79261 DU 125530 2.0 1 9.15
CHEMBL81095 1 8.98
CHEMBL311976 1 8.91
CHEMBL81118 1 8.87
CHEMBL1742477 FLESINOXAN 2.0 1 8.77
CHEMBL8412 IPSAPIRONE 2.0 1 8.26
CHEMBL81733 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311015 Ki = 0.2291 nM 9.64
CHEMBL312339 Ki = 0.2884 nM 9.54
CHEMBL81728 Ki = 0.2951 nM 9.53
CHEMBL311275 Ki = 0.3236 nM 9.49
CHEMBL82215 Ki = 0.6761 nM 9.17
CHEMBL79261 DU 125530 Ki = 0.7079 nM 9.15
CHEMBL81095 Ki = 1.047 nM 8.98
CHEMBL311976 Ki = 1.23 nM 8.91
CHEMBL81118 Ki = 1.349 nM 8.87
CHEMBL1742477 FLESINOXAN Ki = 1.698 nM 8.77
CHEMBL8412 IPSAPIRONE Ki = 5.495 nM 8.26
CHEMBL81733 Ki = 31.62 nM 7.50