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Compound Detail

CHEMBL515086

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Cl.Clc1ccc(CC[C@@]2(Cn3ccnc3)OC[C@@H](CSc3ccc(Br)cc3)O2)cc1

Basic Information

ChEMBL ID CHEMBL515086
Phase Preclinical
Structure Type MOL
InChI Key PNQVUKWRIHCJMZ-IKGOIYPNSA-N
Parent Compound CHEMBL581562
Active Moiety CHEMBL581562
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

493.9
MW (Da)
5.84
ALogP
5
HBA
0
HBD
36.3
PSA (Ų)
0.37
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 C22H23BrCl2N2O2S
MW 530.32
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.73

Activity Summary

IC50 5 meas. best 6.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.05 6.05 900.0 1
Cytochrome P450 3A1
CHEMBL3323
IC50 5.68 5.68 2100.0 1
Heme oxygenase 1
CHEMBL5035
IC50 5.68 5.68 2100.0 1
Heme oxygenase 2
CHEMBL3348
IC50 5.62 5.62 2400.0 1
CHO
CHEMBL613853
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16495054 10.1016/j.bmcl.2006.01.122 CHO 2
16495054 10.1016/j.bmcl.2006.01.122 Plasmodium falciparum 1
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