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Assay Detail

CHEMBL829151

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

Binding
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
8
Total Activities
8
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 Expert

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Terzioglu N, van Rijn RM, Bakker RA, De Esch IJ, Leurs R.
Bioorg Med Chem Lett (2004) 14 : 5251 -5256
PubMed 15454206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 5.73 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129198 JNJ-7777120 1 6.00
CHEMBL362163 1 6.00
CHEMBL186456 1 6.00
CHEMBL128613 1 5.80
CHEMBL187210 1 5.50
CHEMBL186108 1 5.50
CHEMBL365257 1 5.50
CHEMBL185951 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129198 JNJ-7777120 EC50 = 1000.0 nM 6.00
CHEMBL362163 EC50 = 1000.0 nM 6.00
CHEMBL186456 EC50 = 1000.0 nM 6.00
CHEMBL128613 EC50 = 1584.89 nM 5.80
CHEMBL187210 EC50 = 3162.28 nM 5.50
CHEMBL186108 EC50 = 3162.28 nM 5.50
CHEMBL365257 EC50 = 3162.28 nM 5.50
CHEMBL185951 EC50 = 3162.28 nM 5.50