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Assay Detail

CHEMBL3420440

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

Binding
Inhibition of HO2 in Sprague-Dawley rat brain microsomal fraction assessed as reduction in bilirubin formation incubated for 60 mins by double beam spectrophotometry
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Heme oxygenase 2 (CHEMBL3348)
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 22 5.04 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3415249 1 6.10
CHEMBL3415256 1 6.10
CHEMBL3415251 1 6.05
CHEMBL3415242 1 6.05
CHEMBL3415244 1 6.05
CHEMBL3415252 1 6.05
CHEMBL3415253 1 6.05
CHEMBL3415250 1 4.95
CHEMBL1404869 1 4.95
CHEMBL3415248 1 4.90
CHEMBL3415255 1 4.54
CHEMBL2414451 1 4.47
CHEMBL3415254 1 4.45
CHEMBL2414452 1 4.44
CHEMBL3415243 1 4.39
CHEMBL2414449 1 4.38
CHEMBL1452451 1 4.35
CHEMBL3415246 1 4.31
CHEMBL3415247 1 4.13
CHEMBL2414447 1 4.11
CHEMBL2414444 1 -
CHEMBL3415245 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3415249 IC50 = 800.0 nM 6.10
CHEMBL3415256 IC50 = 800.0 nM 6.10
CHEMBL3415251 IC50 = 900.0 nM 6.05
CHEMBL3415242 IC50 = 900.0 nM 6.05
CHEMBL3415244 IC50 = 900.0 nM 6.05
CHEMBL3415252 IC50 = 900.0 nM 6.05
CHEMBL3415253 IC50 = 900.0 nM 6.05
CHEMBL3415250 IC50 = 11200.0 nM 4.95
CHEMBL1404869 IC50 = 11200.0 nM 4.95
CHEMBL3415248 IC50 = 12500.0 nM 4.90
CHEMBL3415255 IC50 = 28800.0 nM 4.54
CHEMBL2414451 IC50 = 33900.0 nM 4.47
CHEMBL3415254 IC50 = 35500.0 nM 4.45
CHEMBL2414452 IC50 = 36300.0 nM 4.44
CHEMBL3415243 IC50 = 41000.0 nM 4.39
CHEMBL2414449 IC50 = 41700.0 nM 4.38
CHEMBL1452451 IC50 = 44700.0 nM 4.35
CHEMBL3415246 IC50 = 49000.0 nM 4.31
CHEMBL3415247 IC50 = 74100.0 nM 4.13
CHEMBL2414447 IC50 = 77600.0 nM 4.11
CHEMBL2414444 IC50 > 100000.0 nM -
CHEMBL3415245 IC50 > 100000.0 nM -