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Assay Detail

CHEMBL882906

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

Binding
Inhibitory concentration against histamine H1 receptor
6
Total Activities
6
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

Designed multiple ligands. An emerging drug discovery paradigm.
Morphy R, Rankovic Z.
J Med Chem (2005) 48 : 6523 -6543
PubMed 16220969 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330366 1 8.52
CHEMBL91397 RUPATADINE 4.0 1 8.41
CHEMBL95051 1 7.23
CHEMBL10971 SCH-37370 1 7.00
CHEMBL998 LORATADINE 4.0 1 6.54
CHEMBL93556 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330366 IC50 = 3.0 nM 8.52
CHEMBL91397 RUPATADINE IC50 = 3.9 nM 8.41
CHEMBL95051 IC50 = 59.0 nM 7.23
CHEMBL10971 SCH-37370 IC50 = 100.0 nM 7.00
CHEMBL998 LORATADINE IC50 = 290.0 nM 6.54
CHEMBL93556 IC50 = 309.0 nM 6.51