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Compound Detail

CHEMBL516064

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Cl.Clc1ccc(CC[C@@]2(Cn3ccnc3)OC[C@@H](COc3ccc(Br)cc3)O2)cc1

Basic Information

ChEMBL ID CHEMBL516064
Phase Preclinical
Structure Type MOL
InChI Key ZWAWLCPTWISOOC-HLUKFBSCSA-N
Parent Compound CHEMBL1187712
Active Moiety CHEMBL1187712
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

477.8
MW (Da)
5.12
ALogP
5
HBA
0
HBD
45.5
PSA (Ų)
0.45
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23BrCl2N2O3
MW 514.25
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.54

Activity Summary

IC50 3 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A1
CHEMBL3323
IC50 5.47 5.47 3400.0 1
Heme oxygenase 1
CHEMBL5035
IC50 5.46 5.46 3500.0 1
Heme oxygenase 2
CHEMBL3348
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19268600 10.1016/j.bmc.2009.01.078 Heme oxygenase 1 1
19268600 10.1016/j.bmc.2009.01.078 Heme oxygenase 2 1
19268600 10.1016/j.bmc.2009.01.078 Unchecked 1
19268600 10.1016/j.bmc.2009.01.078 Cytochrome P450 2E1 1
19268600 10.1016/j.bmc.2009.01.078 Cytochrome P450 3A1 1

Data from ChEMBL 36 via Core Engine