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Assay Detail

CHEMBL855020

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

Binding
Displacement of [3H]histamine from human histamine H4 receptor
8
Total Activities
8
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 H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of S-(2-guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist.
Lim HD, Smits RA, Bakker RA, van Dam CM, de Esch IJ, Leurs R.
J Med Chem (2006) 49 : 6650 -6651
PubMed 17154494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.36 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE 4.0 1 7.90
CHEMBL557151 1 7.50
CHEMBL534494 1 6.60
CHEMBL2311029 1 6.50
CHEMBL539343 1 6.40
CHEMBL534498 1 5.50
CHEMBL535387 1 5.40
CHEMBL534496 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1533310 HISTAMINE DIHYDROCHLORIDE Ki = 12.59 nM 7.90
CHEMBL557151 Ki = 31.62 nM 7.50
CHEMBL534494 Ki = 251.19 nM 6.60
CHEMBL2311029 Ki = 316.23 nM 6.50
CHEMBL539343 Ki = 398.11 nM 6.40
CHEMBL534498 Ki = 3162.28 nM 5.50
CHEMBL535387 Ki = 3981.07 nM 5.40
CHEMBL534496 Ki = 7943.28 nM 5.10