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Assay Detail

CHEMBL616049

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

Functional
Potency against human 5-hydroxytryptamine 1A receptor expressed in CHO cells (experiment 1)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

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
EC50 7 8.20 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL81728 1 9.02
CHEMBL311015 1 8.87
CHEMBL82215 1 8.54
CHEMBL81118 1 8.28
CHEMBL311275 1 8.17
CHEMBL81095 1 7.90
CHEMBL311976 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL81728 EC50 = 0.955 nM 9.02
CHEMBL311015 EC50 = 1.349 nM 8.87
CHEMBL82215 EC50 = 2.884 nM 8.54
CHEMBL81118 EC50 = 5.248 nM 8.28
CHEMBL311275 EC50 = 6.761 nM 8.17
CHEMBL81095 EC50 = 12.59 nM 7.90
CHEMBL311976 EC50 = 251.19 nM 6.60