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Assay Detail

CHEMBL615161

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

Functional
Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Studies toward the discovery of the next generation of antidepressants. 3. Dual 5-HT1A and serotonin transporter affinity within a class of N-aryloxyethylindolylalkylamines.
Mewshaw RE, Zhou D, Zhou P, Shi X, Hornby G, Spangler T, Scerni R, Smith D, Schechter LE, Andree TH.
J Med Chem (2004) 47 : 3823 -3842
PubMed 15239661 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.05 9.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127171 1 9.47
CHEMBL330827 1 8.85
CHEMBL331609 1 8.80
CHEMBL126424 1 8.70
CHEMBL126407 1 8.54
CHEMBL340705 1 8.52
CHEMBL340301 1 8.40
CHEMBL338982 1 8.33
CHEMBL31354 WAY-100,635 1 8.15
CHEMBL2112645 1 7.89
CHEMBL419240 1 7.80
CHEMBL338587 1 7.59
CHEMBL126536 1 7.46
CHEMBL126484 1 7.38
CHEMBL124818 1 7.36
CHEMBL125902 1 7.34
CHEMBL126253 1 7.22
CHEMBL2112644 1 7.01
CHEMBL332589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127171 EC50 = 0.34 nM 9.47
CHEMBL330827 EC50 = 1.4 nM 8.85
CHEMBL331609 EC50 = 1.6 nM 8.80
CHEMBL126424 EC50 = 2.0 nM 8.70
CHEMBL126407 EC50 = 2.9 nM 8.54
CHEMBL340705 EC50 = 3.0 nM 8.52
CHEMBL340301 EC50 = 4.0 nM 8.40
CHEMBL338982 EC50 = 4.7 nM 8.33
CHEMBL31354 WAY-100,635 EC50 = 7.1 nM 8.15
CHEMBL2112645 EC50 = 13.0 nM 7.89
CHEMBL419240 EC50 = 15.7 nM 7.80
CHEMBL338587 EC50 = 25.8 nM 7.59
CHEMBL126536 EC50 = 35.0 nM 7.46
CHEMBL126484 EC50 = 41.6 nM 7.38
CHEMBL124818 EC50 = 44.0 nM 7.36
CHEMBL125902 EC50 = 46.0 nM 7.34
CHEMBL126253 EC50 = 60.8 nM 7.22
CHEMBL2112644 EC50 = 97.4 nM 7.01
CHEMBL332589 EC50 - nM -