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Assay Detail

CHEMBL1921331

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

Binding
Displacement of [3H]-histamine from mouse H4R expressed in HEK293T cells
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK-293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL5657)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.
Mowbray CE, Bell AS, Clarke NP, Collins M, Jones RM, Lane CA, Liu WL, Newman SD, Paradowski M, Schenck EJ, Selby MD, Swain NA, Williams DH.
Bioorg Med Chem Lett (2011) 21 : 6596 -6602
PubMed 21920751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.05 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129198 JNJ-7777120 1 8.41
CHEMBL1915540 ADRIFORANT 2.0 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129198 JNJ-7777120 Ki = 3.89 nM 8.41
CHEMBL1915540 ADRIFORANT Ki = 20.89 nM 7.68