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Assay Detail

CHEMBL953126

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

Binding
Displacement of radiolabeled saralasin from human AT1 receptor
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Type-1 angiotensin II receptor (CHEMBL227)
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
IC50 1 9.17 9.17
Ki 1 9.48 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL938 SARALASIN 4.0 2 9.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL938 SARALASIN Ki = 0.33 nM 9.48
CHEMBL938 SARALASIN IC50 = 0.67 nM 9.17