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Assay Detail

CHEMBL616160

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Binding
pKi value against rat 5-hydroxytryptamine 1A receptor.
18
Total Activities
18
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 (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines.
Kuipers W, Kruse CG, van Wijngaarden I, Standaar PJ, Tulp MT, Veldman N, Spek AL, IJzerman AP.
J Med Chem (1997) 40 : 300 -312
PubMed 9022796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.28 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107141 1 9.50
CHEMBL108229 1 9.10
CHEMBL58792 FLUANISONE 2.0 1 9.00
CHEMBL105345 1 9.00
CHEMBL58377 1 9.00
CHEMBL106854 1 8.90
CHEMBL419910 1 8.80
CHEMBL104805 1 8.70
CHEMBL104515 ANISOPIROL 2.0 1 8.60
CHEMBL105747 1 8.50
CHEMBL107903 1 8.30
CHEMBL278799 1 7.80
CHEMBL107336 1 7.80
CHEMBL104593 1 7.70
CHEMBL323982 1 7.70
CHEMBL104204 1 7.70
CHEMBL26447 1 6.80
CHEMBL104591 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107141 Ki = 0.3162 nM 9.50
CHEMBL108229 Ki = 0.7943 nM 9.10
CHEMBL58792 FLUANISONE Ki = 1.0 nM 9.00
CHEMBL105345 Ki = 1.0 nM 9.00
CHEMBL58377 Ki = 1.0 nM 9.00
CHEMBL106854 Ki = 1.259 nM 8.90
CHEMBL419910 Ki = 1.585 nM 8.80
CHEMBL104805 Ki = 1.995 nM 8.70
CHEMBL104515 ANISOPIROL Ki = 2.512 nM 8.60
CHEMBL105747 Ki = 3.162 nM 8.50
CHEMBL107903 Ki = 5.012 nM 8.30
CHEMBL278799 Ki = 15.85 nM 7.80
CHEMBL107336 Ki = 15.85 nM 7.80
CHEMBL104593 Ki = 19.95 nM 7.70
CHEMBL323982 Ki = 19.95 nM 7.70
CHEMBL104204 Ki = 19.95 nM 7.70
CHEMBL26447 Ki = 158.49 nM 6.80
CHEMBL104591 Ki = 794.33 nM 6.10