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Assay Detail

CHEMBL3420247

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

Binding
Inhibition of HO1 in Sprague-Dawley rat spleen microsomal fraction assessed as reduction in bilirubin formation incubated for 60 mins by double beam spectrophotometry
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Spleen
Subcellular Microsomal
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Heme oxygenase 1 (CHEMBL5035)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel imidazole derivatives as heme oxygenase-1 (HO-1) and heme oxygenase-2 (HO-2) inhibitors and their cytotoxic activity in human-derived cancer cell lines.
Salerno L, Pittalà V, Romeo G, Modica MN, Marrazzo A, Siracusa MA, Sorrenti V, Di Giacomo C, Vanella L, Parayath NN, Greish K.
Eur J Med Chem (2015) 96 : 162 -172
PubMed 25874340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.77 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415248 1 6.05
CHEMBL3415249 1 6.00
CHEMBL3415255 1 4.78
CHEMBL3415246 1 4.77
CHEMBL3415254 1 4.75
CHEMBL3415251 1 4.74
CHEMBL3415256 1 4.70
CHEMBL3415247 1 4.51
CHEMBL3415243 1 4.47
CHEMBL3415253 1 4.44
CHEMBL3415250 1 4.40
CHEMBL3415245 1 4.38
CHEMBL3415242 1 4.37
CHEMBL3415244 1 4.36
CHEMBL3415252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415248 IC50 = 900.0 nM 6.05
CHEMBL3415249 IC50 = 1000.0 nM 6.00
CHEMBL3415255 IC50 = 16600.0 nM 4.78
CHEMBL3415246 IC50 = 16900.0 nM 4.77
CHEMBL3415254 IC50 = 17700.0 nM 4.75
CHEMBL3415251 IC50 = 18400.0 nM 4.74
CHEMBL3415256 IC50 = 20000.0 nM 4.70
CHEMBL3415247 IC50 = 30900.0 nM 4.51
CHEMBL3415243 IC50 = 34000.0 nM 4.47
CHEMBL3415253 IC50 = 36300.0 nM 4.44
CHEMBL3415250 IC50 = 39800.0 nM 4.40
CHEMBL3415245 IC50 = 42000.0 nM 4.38
CHEMBL3415242 IC50 = 42600.0 nM 4.37
CHEMBL3415244 IC50 = 44000.0 nM 4.36
CHEMBL3415252 IC50 > 100000.0 nM -