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Assay Detail

CHEMBL1015211

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

Binding
Inhibition of heme oxygenase-2 in Sprague-Dawley rat brain microsomal fraction assessed as carbon monoxide formation by gas chromatography
34
Total Activities
34
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

Synthesis and evaluation of imidazole-dioxolane compounds as selective heme oxygenase inhibitors: effect of substituents at the 4-position of the dioxolane ring.
Vlahakis JZ, Hum M, Rahman MN, Jia Z, Nakatsu K, Szarek WA.
Bioorg Med Chem (2009) 17 : 2461 -2475
PubMed 19268600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 4.95 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472795 1 6.30
CHEMBL474379 1 5.77
CHEMBL515086 1 5.62
CHEMBL474359 1 5.60
CHEMBL459480 1 5.48
CHEMBL464300 1 5.36
CHEMBL474555 1 5.30
CHEMBL179494 1 5.22
CHEMBL208047 1 5.16
CHEMBL473375 1 5.15
CHEMBL421109 1 5.10
CHEMBL474360 1 4.92
CHEMBL514775 1 4.91
CHEMBL473364 1 4.89
CHEMBL473177 1 4.89
CHEMBL474961 1 4.82
CHEMBL473167 1 4.80
CHEMBL516227 1 4.72
CHEMBL447959 1 4.72
CHEMBL514329 1 4.72
CHEMBL516064 1 4.66
CHEMBL472782 1 4.66
CHEMBL459907 1 4.58
CHEMBL472975 1 4.52
CHEMBL475163 1 4.47
CHEMBL460114 1 4.42
CHEMBL368045 1 4.38
CHEMBL472796 1 4.37
CHEMBL3216038 1 4.16
CHEMBL515233 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472795 IC50 = 500.0 nM 6.30
CHEMBL474379 IC50 = 1700.0 nM 5.77
CHEMBL515086 IC50 = 2400.0 nM 5.62
CHEMBL474359 IC50 = 2500.0 nM 5.60
CHEMBL459480 IC50 = 3300.0 nM 5.48
CHEMBL464300 IC50 = 4400.0 nM 5.36
CHEMBL474555 IC50 = 5000.0 nM 5.30
CHEMBL179494 IC50 = 6000.0 nM 5.22
CHEMBL208047 IC50 = 7000.0 nM 5.16
CHEMBL473375 IC50 = 7100.0 nM 5.15
CHEMBL421109 IC50 = 8000.0 nM 5.10
CHEMBL474360 IC50 = 12000.0 nM 4.92
CHEMBL514775 IC50 = 12300.0 nM 4.91
CHEMBL473364 IC50 = 13000.0 nM 4.89
CHEMBL473177 IC50 = 13000.0 nM 4.89
CHEMBL474961 IC50 = 15000.0 nM 4.82
CHEMBL473167 IC50 = 16000.0 nM 4.80
CHEMBL516227 IC50 = 19000.0 nM 4.72
CHEMBL514329 IC50 = 19000.0 nM 4.72
CHEMBL447959 IC50 = 19000.0 nM 4.72
CHEMBL516064 IC50 = 22000.0 nM 4.66
CHEMBL472782 IC50 = 22000.0 nM 4.66
CHEMBL459907 IC50 = 26000.0 nM 4.58
CHEMBL472975 IC50 = 30000.0 nM 4.52
CHEMBL475163 IC50 = 34000.0 nM 4.47
CHEMBL460114 IC50 = 38000.0 nM 4.42
CHEMBL368045 IC50 = 42000.0 nM 4.38
CHEMBL472796 IC50 = 43000.0 nM 4.37
CHEMBL3216038 IC50 = 69000.0 nM 4.16
CHEMBL515233 IC50 > 100000.0 nM -
CHEMBL474572 IC50 > 100000.0 nM -
CHEMBL459908 IC50 = 122000.0 nM -
CHEMBL460115 IC50 > 100000.0 nM -
CHEMBL463223 IC50 = 305000.0 nM -