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Assay Detail

CHEMBL829975

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

Binding
Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor
16
Total Activities
15
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
Fernández J, Alonso JM, Andrés JI, Cid JM, Díaz A, Iturrino L, Gil P, Megens A, Sipido VK, Trabanco AA.
J Med Chem (2005) 48 : 1709 -1712
PubMed 15771415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 8.35 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193639 2 9.68
CHEMBL363581 1 9.19
CHEMBL329566 1 9.03
CHEMBL366164 1 8.82
CHEMBL435301 1 8.62
CHEMBL364270 1 8.43
CHEMBL194659 1 8.37
CHEMBL6437 MIANSERIN 4.0 1 8.36
CHEMBL195706 1 8.12
CHEMBL193435 1 8.05
CHEMBL85 RISPERIDONE 4.0 1 7.92
CHEMBL715 OLANZAPINE 4.0 1 7.85
CHEMBL195856 1 7.77
CHEMBL42 CLOZAPINE 4.0 1 7.68
CHEMBL654 MIRTAZAPINE 4.0 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193639 Ki = 0.21 nM 9.68
CHEMBL363581 Ki = 0.65 nM 9.19
CHEMBL329566 Ki = 0.93 nM 9.03
CHEMBL366164 Ki = 1.5 nM 8.82
CHEMBL435301 Ki = 2.4 nM 8.62
CHEMBL364270 Ki = 3.7 nM 8.43
CHEMBL194659 Ki = 4.3 nM 8.37
CHEMBL6437 MIANSERIN Ki = 4.4 nM 8.36
CHEMBL195706 Ki = 7.6 nM 8.12
CHEMBL193435 Ki = 8.9 nM 8.05
CHEMBL85 RISPERIDONE Ki = 12.0 nM 7.92
CHEMBL715 OLANZAPINE Ki = 14.0 nM 7.85
CHEMBL195856 Ki = 17.0 nM 7.77
CHEMBL42 CLOZAPINE Ki = 21.0 nM 7.68
CHEMBL654 MIRTAZAPINE Ki = 39.0 nM 7.41
CHEMBL193639 Ki < 0.42 nM -