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

CHEMBL615406

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
19
Total Activities
19
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

5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.
Matzen L, van Amsterdam C, Rautenberg W, Greiner HE, Harting J, Seyfried CA, Böttcher H.
J Med Chem (2000) 43 : 1149 -1157
PubMed 10737747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.79 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274922 1 7.77
CHEMBL16035 1 7.57
CHEMBL15837 1 7.30
CHEMBL15139 1 7.24
CHEMBL279646 1 7.00
CHEMBL15965 1 6.80
CHEMBL430122 1 6.63
CHEMBL279320 1 6.63
CHEMBL15961 1 6.52
CHEMBL15928 GR-127935 1 6.44
CHEMBL2079627 1 6.43
CHEMBL15855 1 6.40
CHEMBL278917 1 6.18
CHEMBL15909 1 6.16
CHEMBL280000 1 -
CHEMBL280314 1 -
CHEMBL276928 1 -
CHEMBL15933 1 -
CHEMBL15808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274922 IC50 = 17.0 nM 7.77
CHEMBL16035 IC50 = 27.0 nM 7.57
CHEMBL15837 IC50 = 50.0 nM 7.30
CHEMBL15139 IC50 = 57.0 nM 7.24
CHEMBL279646 IC50 = 100.0 nM 7.00
CHEMBL15965 IC50 = 160.0 nM 6.80
CHEMBL430122 IC50 = 233.0 nM 6.63
CHEMBL279320 IC50 = 233.0 nM 6.63
CHEMBL15961 IC50 = 300.0 nM 6.52
CHEMBL15928 GR-127935 IC50 = 360.0 nM 6.44
CHEMBL2079627 IC50 = 367.0 nM 6.43
CHEMBL15855 IC50 = 400.0 nM 6.40
CHEMBL278917 IC50 = 667.0 nM 6.18
CHEMBL15909 IC50 = 700.0 nM 6.16
CHEMBL280000 IC50 > 300.0 nM -
CHEMBL280314 IC50 > 500.0 nM -
CHEMBL276928 IC50 > 200.0 nM -
CHEMBL15933 IC50 > 1000.0 nM -
CHEMBL15808 IC50 > 800.0 nM -