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Assay Detail

CHEMBL951436

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

Binding
Binding affinity to human histamine H3 receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
Liu H, Altenbach RJ, Carr TL, Chandran P, Hsieh GC, Lewis LG, Manelli AM, Milicic I, Marsh KC, Miller TR, Strakhova MI, Vortherms TA, Wakefield BD, Wetter JM, Witte DG, Honore P, Esbenshade TA, Brioni JD, Cowart MD.
J Med Chem (2008) 51 : 7094 -7098
PubMed 18983139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.84 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL519240 1 6.03
CHEMBL129198 JNJ-7777120 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL519240 Ki = 933.25 nM 6.03
CHEMBL129198 JNJ-7777120 Ki = 2238.72 nM 5.65