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Assay Detail

CHEMBL882467

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

Binding
Inhibition constant against rat 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand with the compound (10 uM) dissolved in DMSO
11
Total Activities
11
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

SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
Sard H, Kumaran G, Morency C, Roth BL, Toth BA, He P, Shuster L.
Bioorg Med Chem Lett (2005) 15 : 4555 -4559
PubMed 16061378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.86 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198124 1 6.70
CHEMBL197664 1 6.23
CHEMBL194588 1 6.08
CHEMBL197646 1 6.00
CHEMBL370859 1 5.77
CHEMBL371899 1 5.16
CHEMBL445331 1 5.08
CHEMBL198123 1 -
CHEMBL371753 1 -
CHEMBL382750 1 -
CHEMBL194203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198124 Ki = 200.0 nM 6.70
CHEMBL197664 Ki = 590.0 nM 6.23
CHEMBL194588 Ki = 834.0 nM 6.08
CHEMBL197646 Ki = 1008.0 nM 6.00
CHEMBL370859 Ki = 1683.0 nM 5.77
CHEMBL371899 Ki = 6903.0 nM 5.16
CHEMBL445331 Ki = 8367.0 nM 5.08
CHEMBL198123 Ki > 10000.0 nM -
CHEMBL371753 Ki > 10000.0 nM -
CHEMBL382750 Ki > 10000.0 nM -
CHEMBL194203 Ki > 10000.0 nM -