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Assay Detail

CHEMBL829614

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

Binding
Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor
17
Total Activities
16
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

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 17 8.21 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193639 2 9.62
CHEMBL85 RISPERIDONE 4.0 1 9.09
CHEMBL366164 1 8.80
CHEMBL715 OLANZAPINE 4.0 1 8.64
CHEMBL329566 1 8.60
CHEMBL6437 MIANSERIN 4.0 1 8.37
CHEMBL435301 1 8.22
CHEMBL42 CLOZAPINE 4.0 1 8.20
CHEMBL363581 1 7.89
CHEMBL193435 1 7.82
CHEMBL364270 1 7.66
CHEMBL195856 1 7.42
CHEMBL654 MIRTAZAPINE 4.0 1 7.16
CHEMBL54 HALOPERIDOL 4.0 1 6.36
CHEMBL195706 1 -
CHEMBL194659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193639 Ki = 0.24 nM 9.62
CHEMBL193639 Ki = 0.56 nM 9.25
CHEMBL85 RISPERIDONE Ki = 0.81 nM 9.09
CHEMBL366164 Ki = 1.6 nM 8.80
CHEMBL715 OLANZAPINE Ki = 2.3 nM 8.64
CHEMBL329566 Ki = 2.5 nM 8.60
CHEMBL6437 MIANSERIN Ki = 4.3 nM 8.37
CHEMBL435301 Ki = 6.0 nM 8.22
CHEMBL42 CLOZAPINE Ki = 6.3 nM 8.20
CHEMBL363581 Ki = 13.0 nM 7.89
CHEMBL193435 Ki = 15.0 nM 7.82
CHEMBL364270 Ki = 22.0 nM 7.66
CHEMBL195856 Ki = 38.0 nM 7.42
CHEMBL654 MIRTAZAPINE Ki = 69.0 nM 7.16
CHEMBL54 HALOPERIDOL Ki = 435.0 nM 6.36
CHEMBL195706 Ki > 5454.0 nM -
CHEMBL194659 Ki > 5454.0 nM -