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Assay Detail

CHEMBL615168

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

Binding
Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.
van Niel MB, Beer MS, Castro JL, Cheng SK, Evans DC, Heald A, Hitzel L, Hunt P, Mortishire-Smith R, O'Connor D, Watt AP, MacLeod AM.
Bioorg Med Chem Lett (1999) 9 : 3243 -3248
PubMed 10576696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 8.13 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327126 1 8.96
CHEMBL326751 1 8.92
CHEMBL111065 1 8.48
CHEMBL111713 1 8.46
CHEMBL323441 1 7.68
CHEMBL500 PINDOLOL 4.0 1 7.57
CHEMBL114452 1 7.51
CHEMBL114453 1 7.43
CHEMBL113326 1 -
CHEMBL111021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327126 EC50 = 1.1 nM 8.96
CHEMBL326751 EC50 = 1.2 nM 8.92
CHEMBL111065 EC50 = 3.3 nM 8.48
CHEMBL111713 EC50 = 3.5 nM 8.46
CHEMBL323441 EC50 = 21.0 nM 7.68
CHEMBL500 PINDOLOL EC50 = 27.0 nM 7.57
CHEMBL114452 EC50 = 31.0 nM 7.51
CHEMBL114453 EC50 = 37.0 nM 7.43
CHEMBL113326 EC50 > 10000.0 nM -
CHEMBL111021 EC50 > 10000.0 nM -