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Assay Detail

CHEMBL1013157

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

Binding
Displacement of 3H]paroxetine from rat cortical adrenergic alpha1 receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.
Zhou D, Zhou P, Evrard DA, Meagher K, Webb M, Harrison BL, Huryn DM, Golembieski J, Hornby GA, Schechter LE, Smith DL, Andree TH, Mewshaw RE.
Bioorg Med Chem (2008) 16 : 6707 -6723
PubMed 18571421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.14 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519616 1 8.52
CHEMBL481337 1 8.38
CHEMBL520265 1 7.96
CHEMBL481523 1 7.64
CHEMBL494483 1 7.58
CHEMBL517996 1 7.47
CHEMBL518946 1 7.32
CHEMBL481113 1 7.22
CHEMBL494276 1 7.19
CHEMBL481914 1 7.18
CHEMBL481754 1 7.11
CHEMBL481753 1 7.09
CHEMBL481524 1 6.93
CHEMBL481109 1 6.81
CHEMBL481747 1 6.75
CHEMBL359495 1 6.71
CHEMBL522671 1 6.58
CHEMBL520753 1 6.53
CHEMBL480932 1 6.28
CHEMBL493037 1 5.61
CHEMBL481108 1 -
CHEMBL482266 1 -
CHEMBL479986 1 -
CHEMBL481125 1 -
CHEMBL481126 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519616 Ki = 3.0 nM 8.52
CHEMBL481337 Ki = 4.2 nM 8.38
CHEMBL520265 Ki = 11.0 nM 7.96
CHEMBL481523 Ki = 23.1 nM 7.64
CHEMBL494483 Ki = 26.0 nM 7.58
CHEMBL517996 Ki = 34.0 nM 7.47
CHEMBL518946 Ki = 47.6 nM 7.32
CHEMBL481113 Ki = 60.5 nM 7.22
CHEMBL494276 Ki = 65.0 nM 7.19
CHEMBL481914 Ki = 66.0 nM 7.18
CHEMBL481754 Ki = 78.0 nM 7.11
CHEMBL481753 Ki = 82.0 nM 7.09
CHEMBL481524 Ki = 118.0 nM 6.93
CHEMBL481109 Ki = 156.0 nM 6.81
CHEMBL481747 Ki = 177.0 nM 6.75
CHEMBL359495 Ki = 196.0 nM 6.71
CHEMBL522671 Ki = 266.0 nM 6.58
CHEMBL520753 Ki = 293.0 nM 6.53
CHEMBL480932 Ki = 522.0 nM 6.28
CHEMBL493037 Ki = 2430.0 nM 5.61
CHEMBL481108 Ki - -
CHEMBL482266 Ki - -
CHEMBL479986 Ki - -
CHEMBL481125 Ki - -
CHEMBL481126 Ki - -