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Assay Detail

CHEMBL700768

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Binding
Binding affinity to the human histamine H4 receptor
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The first potent and selective non-imidazole human histamine H4 receptor antagonists.
Jablonowski JA, Grice CA, Chai W, Dvorak CA, Venable JD, Kwok AK, Ly KS, Wei J, Baker SM, Desai PJ, Jiang W, Wilson SJ, Thurmond RL, Karlsson L, Edwards JP, Lovenberg TW, Carruthers NI.
J Med Chem (2003) 46 : 3957 -3960
PubMed 12954048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.27 7.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12608 IMPROMIDINE 2.0 1 7.91
CHEMBL260374 THIOPERAMIDE 1 7.57
CHEMBL268229 1 6.84
CHEMBL12160 BURIMAMIDE 1 6.75
CHEMBL129257 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12608 IMPROMIDINE Ki = 12.3 nM 7.91
CHEMBL260374 THIOPERAMIDE Ki = 27.0 nM 7.57
CHEMBL268229 Ki = 146.0 nM 6.84
CHEMBL12160 BURIMAMIDE Ki = 180.0 nM 6.75
CHEMBL129257 Ki > 10000.0 nM -