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Assay Detail

CHEMBL887348

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

Binding
Displacement of [3H]ketanserin from rat cloned 5HT2A receptor
12
Total Activities
12
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 I: Influence of the substitution on the basic nitrogen and the position of the amide 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 : 1565 -1569
PubMed 17254782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.78 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388620 1 7.38
CHEMBL228972 1 7.36
CHEMBL229024 1 7.30
CHEMBL229023 1 6.96
CHEMBL388396 1 6.68
CHEMBL229025 1 6.67
CHEMBL387951 1 6.64
CHEMBL228865 1 6.61
CHEMBL228866 1 6.41
CHEMBL387952 1 6.31
CHEMBL229021 1 6.26
CHEMBL229019 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388620 Ki = 42.0 nM 7.38
CHEMBL228972 Ki = 44.0 nM 7.36
CHEMBL229024 Ki = 50.0 nM 7.30
CHEMBL229023 Ki = 110.0 nM 6.96
CHEMBL388396 Ki = 211.0 nM 6.68
CHEMBL229025 Ki = 213.0 nM 6.67
CHEMBL387951 Ki = 228.0 nM 6.64
CHEMBL228865 Ki = 248.0 nM 6.61
CHEMBL228866 Ki = 390.0 nM 6.41
CHEMBL387952 Ki = 487.0 nM 6.31
CHEMBL229021 Ki = 543.0 nM 6.26
CHEMBL229019 Ki > 1000.0 nM -