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Assay Detail

CHEMBL4410552

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

Binding
Antagonist activity at histamine H1 receptor (unknown origin)
18
Total Activities
18
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 H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel desloratadine derivatives with anti-inflammatory and H1 antagonize activities.
Li F, Xu Q, Zhu Q, Chu Z, Lin G, Mo J, Zhao Y, Li J, He G, Xu Y.
Bioorg Med Chem Lett (2019) 29 : 126712 -126712
PubMed 31679973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.91 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1172 DESLORATADINE 4.0 1 8.73
CHEMBL4446961 1 8.53
CHEMBL4591702 1 8.44
CHEMBL4467816 1 8.34
CHEMBL4556553 1 8.32
CHEMBL4587694 1 8.21
CHEMBL4451332 1 8.09
CHEMBL4539150 1 8.05
CHEMBL4473466 1 8.03
CHEMBL4581995 1 7.92
CHEMBL4473399 1 7.75
CHEMBL4518271 1 7.68
CHEMBL4539056 1 7.55
CHEMBL4529928 1 7.55
CHEMBL4557928 1 7.43
CHEMBL4458953 1 7.40
CHEMBL4445636 1 7.28
CHEMBL4565774 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1172 DESLORATADINE IC50 = 1.84 nM 8.73
CHEMBL4446961 IC50 = 2.95 nM 8.53
CHEMBL4591702 IC50 = 3.67 nM 8.44
CHEMBL4467816 IC50 = 4.56 nM 8.34
CHEMBL4556553 IC50 = 4.74 nM 8.32
CHEMBL4587694 IC50 = 6.23 nM 8.21
CHEMBL4451332 IC50 = 8.14 nM 8.09
CHEMBL4539150 IC50 = 8.9 nM 8.05
CHEMBL4473466 IC50 = 9.28 nM 8.03
CHEMBL4581995 IC50 = 11.97 nM 7.92
CHEMBL4473399 IC50 = 17.65 nM 7.75
CHEMBL4518271 IC50 = 20.98 nM 7.68
CHEMBL4539056 IC50 = 28.41 nM 7.55
CHEMBL4529928 IC50 = 27.88 nM 7.55
CHEMBL4557928 IC50 = 36.71 nM 7.43
CHEMBL4458953 IC50 = 40.22 nM 7.40
CHEMBL4445636 IC50 = 52.85 nM 7.28
CHEMBL4565774 IC50 = 81.78 nM 7.09