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Assay Detail

CHEMBL882471

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

Binding
Inhibition constant against human 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand with the compound (10 uM) dissolved in DMSO
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

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 13 6.05 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370859 1 6.91
CHEMBL198124 1 6.51
CHEMBL197646 1 6.47
CHEMBL364061 1 6.37
CHEMBL370221 1 6.30
CHEMBL198617 1 6.23
CHEMBL197664 1 6.05
CHEMBL194588 1 6.04
CHEMBL194202 1 6.01
CHEMBL371753 1 5.52
CHEMBL382750 1 5.12
CHEMBL371899 1 5.01
CHEMBL198123 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370859 Ki = 122.0 nM 6.91
CHEMBL198124 Ki = 310.0 nM 6.51
CHEMBL197646 Ki = 335.0 nM 6.47
CHEMBL364061 Ki = 429.0 nM 6.37
CHEMBL370221 Ki = 498.0 nM 6.30
CHEMBL198617 Ki = 588.0 nM 6.23
CHEMBL197664 Ki = 900.0 nM 6.05
CHEMBL194588 Ki = 923.0 nM 6.04
CHEMBL194202 Ki = 982.0 nM 6.01
CHEMBL371753 Ki = 3000.0 nM 5.52
CHEMBL382750 Ki = 7600.0 nM 5.12
CHEMBL371899 Ki = 9753.0 nM 5.01
CHEMBL198123 Ki > 10000.0 nM -