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Assay Detail

CHEMBL1005955

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Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in SK-NM-C cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-N-MC
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.
Kiss R, Kiss B, Könczöl A, Szalai F, Jelinek I, László V, Noszál B, Falus A, Keseru GM.
J Med Chem (2008) 51 : 3145 -3153
PubMed 18459760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.10 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19439 IMETIT 1 8.44
CHEMBL14690 CLOBENPROPIT 1 8.30
CHEMBL498770 IODOPHENPROPIT 1 8.11
CHEMBL90 HISTAMINE 4.0 1 7.87
CHEMBL129198 JNJ-7777120 1 7.77
CHEMBL1162351 1 7.07
CHEMBL12344 DIMAPRIT 1 7.05
CHEMBL268229 1 6.74
CHEMBL1162352 1 6.66
CHEMBL260374 THIOPERAMIDE 1 6.48
CHEMBL1162347 1 6.05
CHEMBL1162346 1 5.91
CHEMBL1162345 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19439 IMETIT Ki = 3.6 nM 8.44
CHEMBL14690 CLOBENPROPIT Ki = 5.0 nM 8.30
CHEMBL498770 IODOPHENPROPIT Ki = 7.8 nM 8.11
CHEMBL90 HISTAMINE Ki = 13.4 nM 7.87
CHEMBL129198 JNJ-7777120 Ki = 17.0 nM 7.77
CHEMBL1162351 Ki = 85.0 nM 7.07
CHEMBL12344 DIMAPRIT Ki = 90.0 nM 7.05
CHEMBL268229 Ki = 184.0 nM 6.74
CHEMBL1162352 Ki = 219.0 nM 6.66
CHEMBL260374 THIOPERAMIDE Ki = 328.0 nM 6.48
CHEMBL1162347 Ki = 897.0 nM 6.05
CHEMBL1162346 Ki = 1240.0 nM 5.91
CHEMBL1162345 Ki = 1480.0 nM 5.83