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Assay Detail

CHEMBL615753

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

Binding
Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 30 8.16 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL340705 1 9.27
CHEMBL330827 1 9.16
CHEMBL419240 1 9.15
CHEMBL331609 1 9.06
CHEMBL31354 WAY-100,635 1 9.02
CHEMBL126484 1 8.89
CHEMBL126424 1 8.82
CHEMBL338982 1 8.80
CHEMBL126407 1 8.80
CHEMBL2112645 1 8.70
CHEMBL340301 1 8.60
CHEMBL338587 1 8.38
CHEMBL124700 1 8.24
CHEMBL124818 1 8.11
CHEMBL124638 1 8.07
CHEMBL2112644 1 8.04
CHEMBL125902 1 8.01
CHEMBL338520 1 7.97
CHEMBL340895 1 7.89
CHEMBL126253 1 7.78
CHEMBL339810 1 7.77
CHEMBL339490 1 7.65
CHEMBL124069 1 7.58
CHEMBL340873 1 7.54
CHEMBL127171 1 7.46
CHEMBL435612 1 7.46
CHEMBL126536 1 7.45
CHEMBL338482 1 7.32
CHEMBL332589 1 7.04
CHEMBL339559 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL340705 Ki = 0.54 nM 9.27
CHEMBL330827 Ki = 0.69 nM 9.16
CHEMBL419240 Ki = 0.7 nM 9.15
CHEMBL331609 Ki = 0.87 nM 9.06
CHEMBL31354 WAY-100,635 Ki = 0.96 nM 9.02
CHEMBL126484 Ki = 1.3 nM 8.89
CHEMBL126424 Ki = 1.5 nM 8.82
CHEMBL338982 Ki = 1.6 nM 8.80
CHEMBL126407 Ki = 1.6 nM 8.80
CHEMBL2112645 Ki = 2.0 nM 8.70
CHEMBL340301 Ki = 2.5 nM 8.60
CHEMBL338587 Ki = 4.2 nM 8.38
CHEMBL124700 Ki = 5.8 nM 8.24
CHEMBL124818 Ki = 7.7 nM 8.11
CHEMBL124638 Ki = 8.5 nM 8.07
CHEMBL2112644 Ki = 9.2 nM 8.04
CHEMBL125902 Ki = 9.8 nM 8.01
CHEMBL338520 Ki = 10.7 nM 7.97
CHEMBL340895 Ki = 12.9 nM 7.89
CHEMBL126253 Ki = 16.8 nM 7.78
CHEMBL339810 Ki = 17.1 nM 7.77
CHEMBL339490 Ki = 22.4 nM 7.65
CHEMBL124069 Ki = 26.6 nM 7.58
CHEMBL340873 Ki = 29.2 nM 7.54
CHEMBL127171 Ki = 35.0 nM 7.46
CHEMBL435612 Ki = 35.1 nM 7.46
CHEMBL126536 Ki = 35.5 nM 7.45
CHEMBL338482 Ki = 48.0 nM 7.32
CHEMBL332589 Ki = 91.4 nM 7.04
CHEMBL339559 Ki = 170.0 nM 6.77