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Assay Detail

CHEMBL829679

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

Binding
Inhibition of [3H]pyrilamine binding to human Histamine H1 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

Histamine H1 receptor (CHEMBL231)
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 8.52 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL329566 1 9.37
CHEMBL193639 2 9.28
CHEMBL42 CLOZAPINE 4.0 1 8.96
CHEMBL715 OLANZAPINE 4.0 1 8.92
CHEMBL363581 1 8.92
CHEMBL366164 1 8.85
CHEMBL654 MIRTAZAPINE 4.0 1 8.80
CHEMBL6437 MIANSERIN 4.0 1 8.77
CHEMBL435301 1 8.37
CHEMBL194659 1 8.12
CHEMBL364270 1 7.85
CHEMBL85 RISPERIDONE 4.0 1 7.48
CHEMBL195706 1 7.48
CHEMBL193435 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL329566 Ki = 0.43 nM 9.37
CHEMBL193639 Ki = 0.52 nM 9.28
CHEMBL193639 Ki = 0.6 nM 9.22
CHEMBL42 CLOZAPINE Ki = 1.1 nM 8.96
CHEMBL715 OLANZAPINE Ki = 1.2 nM 8.92
CHEMBL363581 Ki = 1.2 nM 8.92
CHEMBL366164 Ki = 1.4 nM 8.85
CHEMBL654 MIRTAZAPINE Ki = 1.6 nM 8.80
CHEMBL6437 MIANSERIN Ki = 1.7 nM 8.77
CHEMBL435301 Ki = 4.3 nM 8.37
CHEMBL194659 Ki = 7.5 nM 8.12
CHEMBL364270 Ki = 14.0 nM 7.85
CHEMBL85 RISPERIDONE Ki = 33.0 nM 7.48
CHEMBL195706 Ki = 33.0 nM 7.48
CHEMBL193435 Ki = 42.0 nM 7.38