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Assay Detail

CHEMBL616366

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Binding
Binding affinity for 5-hydroxytryptamine 1A receptor determined using [3H]8-OH-DPAT as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
Feenstra RW, de Moes J, Hofma JJ, Kling H, Kuipers W, Long SK, Tulp MT, van der Heyden JA, Kruse CG.
Bioorg Med Chem Lett (2001) 11 : 2345 -2349
PubMed 11527728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.59 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77472 1 9.04
CHEMBL58377 1 9.00
CHEMBL292187 ELOPIPRAZOLE 2.0 1 8.82
CHEMBL80230 1 8.12
CHEMBL76990 1 8.11
CHEMBL78058 1 8.10
CHEMBL218166 BIFEPRUNOX 3.0 1 8.03
CHEMBL306830 1 7.85
CHEMBL78241 1 7.82
CHEMBL308345 1 7.80
CHEMBL310045 1 7.77
CHEMBL74805 1 7.68
CHEMBL309215 1 7.68
CHEMBL80156 1 7.64
CHEMBL310048 1 7.58
CHEMBL75621 1 7.50
CHEMBL420016 1 7.50
CHEMBL305834 1 7.46
CHEMBL308875 1 7.42
CHEMBL77334 1 7.39
CHEMBL77934 1 7.38
CHEMBL305920 1 7.31
CHEMBL308476 1 7.07
CHEMBL306634 1 6.89
CHEMBL419275 1 6.70
CHEMBL85 RISPERIDONE 4.0 1 6.60
CHEMBL42 CLOZAPINE 4.0 1 6.57
CHEMBL54 HALOPERIDOL 4.0 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77472 Ki = 0.91 nM 9.04
CHEMBL58377 Ki = 1.0 nM 9.00
CHEMBL292187 ELOPIPRAZOLE Ki = 1.5 nM 8.82
CHEMBL80230 Ki = 7.6 nM 8.12
CHEMBL76990 Ki = 7.8 nM 8.11
CHEMBL78058 Ki = 7.9 nM 8.10
CHEMBL218166 BIFEPRUNOX Ki = 9.3 nM 8.03
CHEMBL306830 Ki = 14.0 nM 7.85
CHEMBL78241 Ki = 15.0 nM 7.82
CHEMBL308345 Ki = 16.0 nM 7.80
CHEMBL310045 Ki = 17.0 nM 7.77
CHEMBL74805 Ki = 21.0 nM 7.68
CHEMBL309215 Ki = 21.0 nM 7.68
CHEMBL80156 Ki = 23.0 nM 7.64
CHEMBL310048 Ki = 26.0 nM 7.58
CHEMBL75621 Ki = 32.0 nM 7.50
CHEMBL420016 Ki = 32.0 nM 7.50
CHEMBL305834 Ki = 35.0 nM 7.46
CHEMBL308875 Ki = 38.0 nM 7.42
CHEMBL77334 Ki = 41.0 nM 7.39
CHEMBL77934 Ki = 42.0 nM 7.38
CHEMBL305920 Ki = 49.0 nM 7.31
CHEMBL308476 Ki = 85.0 nM 7.07
CHEMBL306634 Ki = 130.0 nM 6.89
CHEMBL419275 Ki = 200.0 nM 6.70
CHEMBL85 RISPERIDONE Ki = 253.0 nM 6.60
CHEMBL42 CLOZAPINE Ki = 270.0 nM 6.57
CHEMBL54 HALOPERIDOL Ki = 2800.0 nM 5.55