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Assay Detail

CHEMBL980603

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

Binding
Displacement of [3H]MDL100907 from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
Parker MA, Kurrasch DM, Nichols DE.
Bioorg Med Chem (2008) 16 : 4661 -4669
PubMed 18296055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.64 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL149024 1 9.64
CHEMBL101008 1 7.83
CHEMBL267777 RITANSERIN 2.0 1 7.44
CHEMBL465525 1 6.50
CHEMBL65547 PSILOCIN 2.0 1 6.49
CHEMBL445687 1 6.32
CHEMBL12420 N,N-DIMETHYLTRYPTAMINE 2.0 1 5.79
CHEMBL509461 1 5.60
CHEMBL13086 1 5.43
CHEMBL13147 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL149024 Ki = 0.23 nM 9.64
CHEMBL101008 Ki = 14.8 nM 7.83
CHEMBL267777 RITANSERIN Ki = 36.0 nM 7.44
CHEMBL465525 Ki = 313.0 nM 6.50
CHEMBL65547 PSILOCIN Ki = 323.0 nM 6.49
CHEMBL445687 Ki = 476.0 nM 6.32
CHEMBL12420 N,N-DIMETHYLTRYPTAMINE Ki = 1636.0 nM 5.79
CHEMBL509461 Ki = 2505.0 nM 5.60
CHEMBL13086 Ki = 3676.0 nM 5.43
CHEMBL13147 Ki = 4611.0 nM 5.34