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Assay Detail

CHEMBL828756

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

Binding
Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor
15
Total Activities
14
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

Alpha-2A adrenergic receptor (CHEMBL1867)
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 15 7.17 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6437 MIANSERIN 4.0 1 8.32
CHEMBL85 RISPERIDONE 4.0 1 8.00
CHEMBL435301 1 8.00
CHEMBL654 MIRTAZAPINE 4.0 1 7.70
CHEMBL42 CLOZAPINE 4.0 1 7.62
CHEMBL193639 2 7.18
CHEMBL363581 1 7.14
CHEMBL329566 1 6.90
CHEMBL366164 1 6.81
CHEMBL715 OLANZAPINE 4.0 1 6.72
CHEMBL195706 1 6.60
CHEMBL194659 1 6.57
CHEMBL364270 1 6.52
CHEMBL193435 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6437 MIANSERIN Ki = 4.8 nM 8.32
CHEMBL85 RISPERIDONE Ki = 10.0 nM 8.00
CHEMBL435301 Ki = 10.0 nM 8.00
CHEMBL654 MIRTAZAPINE Ki = 20.0 nM 7.70
CHEMBL42 CLOZAPINE Ki = 24.0 nM 7.62
CHEMBL193639 Ki = 66.0 nM 7.18
CHEMBL363581 Ki = 72.0 nM 7.14
CHEMBL193639 Ki = 79.0 nM 7.10
CHEMBL329566 Ki = 126.0 nM 6.90
CHEMBL366164 Ki = 156.0 nM 6.81
CHEMBL715 OLANZAPINE Ki = 192.0 nM 6.72
CHEMBL195706 Ki = 251.0 nM 6.60
CHEMBL194659 Ki = 269.0 nM 6.57
CHEMBL364270 Ki = 302.0 nM 6.52
CHEMBL193435 Ki = 407.0 nM 6.39