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Assay Detail

CHEMBL2432449

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

Binding
Inhibition of histamine H2 receptor (unknown origin) by PDSP assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H2 receptor (CHEMBL1941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-substituted 8-aminopentacyclo[5.4.0.0(2,6).0(3,10).0(5,9)]undecanes as σ receptor ligands with potential neuroprotective effects.
Banister SD, Manoli M, Barron ML, Werry EL, Kassiou M.
Bioorg Med Chem (2013) 21 : 6038 -6052
PubMed 23981939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 5.52 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2429890 1 5.94
CHEMBL2432046 1 5.83
CHEMBL2432051 1 5.76
CHEMBL2432056 1 5.73
CHEMBL1643899 1 5.67
CHEMBL2432058 1 5.52
CHEMBL2432045 1 5.46
CHEMBL2205827 1 5.45
CHEMBL2432048 1 5.41
CHEMBL1643900 1 5.35
CHEMBL1643902 1 5.35
CHEMBL2432039 1 5.20
CHEMBL2432062 1 5.07
CHEMBL2205820 1 -
CHEMBL602850 1 -
CHEMBL2205835 1 -
CHEMBL2205830 1 -
CHEMBL608560 1 -
CHEMBL2205831 1 -
CHEMBL2432047 1 -
CHEMBL2432050 1 -
CHEMBL2432055 1 -
CHEMBL2432044 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2429890 Ki = 1157.0 nM 5.94
CHEMBL2432046 Ki = 1480.0 nM 5.83
CHEMBL2432051 Ki = 1733.0 nM 5.76
CHEMBL2432056 Ki = 1868.0 nM 5.73
CHEMBL1643899 Ki = 2148.0 nM 5.67
CHEMBL2432058 Ki = 3038.0 nM 5.52
CHEMBL2432045 Ki = 3471.0 nM 5.46
CHEMBL2205827 Ki = 3581.0 nM 5.45
CHEMBL2432048 Ki = 3896.0 nM 5.41
CHEMBL1643900 Ki = 4423.0 nM 5.35
CHEMBL1643902 Ki = 4450.0 nM 5.35
CHEMBL2432039 Ki = 6268.0 nM 5.20
CHEMBL2432062 Ki = 8517.0 nM 5.07
CHEMBL2205820 Ki - -
CHEMBL602850 Ki - -
CHEMBL2205835 Ki - -
CHEMBL2205830 Ki - -
CHEMBL608560 Ki - -
CHEMBL2205831 Ki - -
CHEMBL2432047 Ki - -
CHEMBL2432050 Ki - -
CHEMBL2432055 Ki > 10000.0 nM -
CHEMBL2432044 Ki > 10000.0 nM -