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Compound Detail

CHEMBL556487

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O=C(NC1CC1c1ccccc1)N1CCC(c2nc(-c3ccncc3)no2)CC1

Basic Information

ChEMBL ID CHEMBL556487
Phase Preclinical
Structure Type MOL
InChI Key BLVRDPUKIXDEBG-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

389.5
MW (Da)
3.58
ALogP
5
HBA
1
HBD
84.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O2
MW 389.46
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.80

Activity Summary

IC50 4 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional epoxide hydrolase 2
CHEMBL2409
IC50 7.85 7.685 14.0 2
Bifunctional epoxide hydrolase 2
CHEMBL5669
IC50 7.82 7.82 15.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19645482 10.1021/jm900725r Bifunctional epoxide hydrolase 2 3
19645482 10.1021/jm900725r Epoxide hydrolase 1 1
19645482 10.1021/jm900725r Cytochrome P450 2C9 1
19645482 10.1021/jm900725r Cytochrome P450 2D6 1
19645482 10.1021/jm900725r Cytochrome P450 3A4 1
19645482 10.1021/jm900725r Voltage-dependent L-type calcium channel subunit alpha-1C 1
19645482 10.1021/jm900725r Voltage-gated inwardly rectifying potassium channel KCNH2 1
19645482 10.1021/jm900725r Sodium channel protein type 5 subunit alpha 1

Data from ChEMBL 36 via Core Engine