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Assay Detail

CHEMBL880732

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Binding
In vitro binding affinity towards histamine H1 receptor expressed in CHO-K1 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-lipoxygenase inhibitors with histamine H(1) receptor antagonist activity.
Lewis TA, Bayless L, Eckman JB, Ellis JL, Grewal G, Libertine L, Marie Nicolas J, Scannell RT, Wels BF, Wenberg K, Wypij DM.
Bioorg Med Chem Lett (2004) 14 : 2265 -2268
PubMed 15081022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.04 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307609 1 8.40
CHEMBL1000 CETIRIZINE 4.0 1 7.85
CHEMBL305662 1 7.30
CHEMBL73135 1 6.82
CHEMBL74688 1 6.75
CHEMBL312082 1 6.72
CHEMBL73706 1 6.26
CHEMBL74779 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307609 Ki = 4.0 nM 8.40
CHEMBL1000 CETIRIZINE Ki = 14.0 nM 7.85
CHEMBL305662 Ki = 50.0 nM 7.30
CHEMBL73135 Ki = 150.0 nM 6.82
CHEMBL74688 Ki = 180.0 nM 6.75
CHEMBL312082 Ki = 190.0 nM 6.72
CHEMBL73706 Ki = 550.0 nM 6.26
CHEMBL74779 Ki = 660.0 nM 6.18