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Assay Detail

CHEMBL890994

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

Binding
Displacement of [3H]ketanserin from rat 5HT2A receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and in vitro binding studies of substituted piperidine naphthamides. Part II: Influence of the substitution on the benzyl moiety on the affinity for D2L, D4.2, and 5-HT2A receptors.
Carato P, Graulich A, Jensen N, Roth BL, Liégeois JF.
Bioorg Med Chem Lett (2007) 17 : 1570 -1574
PubMed 17251022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.71 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228972 1 7.36
CHEMBL395867 1 7.28
CHEMBL234825 1 7.06
CHEMBL233579 1 6.88
CHEMBL233580 1 6.88
CHEMBL234646 1 6.82
CHEMBL234645 1 6.80
CHEMBL234647 1 6.76
CHEMBL234472 1 6.65
CHEMBL234826 1 6.65
CHEMBL232197 1 6.64
CHEMBL233581 1 6.62
CHEMBL234644 1 6.56
CHEMBL395631 1 6.33
CHEMBL394042 1 6.28
CHEMBL234827 1 6.26
CHEMBL234001 1 6.16
CHEMBL229019 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228972 Ki = 44.0 nM 7.36
CHEMBL395867 Ki = 53.0 nM 7.28
CHEMBL234825 Ki = 87.0 nM 7.06
CHEMBL233579 Ki = 133.0 nM 6.88
CHEMBL233580 Ki = 133.0 nM 6.88
CHEMBL234646 Ki = 151.0 nM 6.82
CHEMBL234645 Ki = 158.0 nM 6.80
CHEMBL234647 Ki = 175.0 nM 6.76
CHEMBL234472 Ki = 223.0 nM 6.65
CHEMBL234826 Ki = 222.0 nM 6.65
CHEMBL232197 Ki = 228.0 nM 6.64
CHEMBL233581 Ki = 242.0 nM 6.62
CHEMBL234644 Ki = 278.0 nM 6.56
CHEMBL395631 Ki = 462.0 nM 6.33
CHEMBL394042 Ki = 524.0 nM 6.28
CHEMBL234827 Ki = 545.0 nM 6.26
CHEMBL234001 Ki = 695.0 nM 6.16
CHEMBL229019 Ki > 1000.0 nM -