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Assay Detail

CHEMBL882450

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

Binding
Inhibition constant against human 5-hydroxytryptamine 2B receptor using [3H]LSD 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 2B (CHEMBL1833)
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 6.50 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198124 1 8.24
CHEMBL197646 1 8.08
CHEMBL197664 1 7.42
CHEMBL198617 1 7.01
CHEMBL371899 1 6.94
CHEMBL371753 1 6.77
CHEMBL364061 1 6.37
CHEMBL194202 1 6.13
CHEMBL194588 1 5.91
CHEMBL370221 1 5.91
CHEMBL198123 1 5.26
CHEMBL445331 1 5.25
CHEMBL382750 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198124 Ki = 5.8 nM 8.24
CHEMBL197646 Ki = 8.39 nM 8.08
CHEMBL197664 Ki = 38.0 nM 7.42
CHEMBL198617 Ki = 98.0 nM 7.01
CHEMBL371899 Ki = 116.0 nM 6.94
CHEMBL371753 Ki = 170.0 nM 6.77
CHEMBL364061 Ki = 423.0 nM 6.37
CHEMBL194202 Ki = 745.0 nM 6.13
CHEMBL194588 Ki = 1242.0 nM 5.91
CHEMBL370221 Ki = 1242.0 nM 5.91
CHEMBL198123 Ki = 5500.0 nM 5.26
CHEMBL445331 Ki = 5566.0 nM 5.25
CHEMBL382750 Ki = 6300.0 nM 5.20