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Compound Detail

CHEMBL239074

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CCc1nc(N)nc(N)c1-c1ccc2c(c1)N(CCNC(C)=O)C(=O)C(C)(c1ccc(Cl)cc1)O2

Basic Information

ChEMBL ID CHEMBL239074
Phase Preclinical
Structure Type MOL
InChI Key HOBWYNFQYPRIDL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
7
Publications
0
Known Names

Molecular Properties

495.0
MW (Da)
3.30
ALogP
7
HBA
3
HBD
136.5
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27ClN6O3
MW 494.98
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.78

Activity Summary

IC50 3 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A4
CHEMBL340
IC50 6.23 6.23 590.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.92 4.92 12000.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 4.72 4.72 19000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 3A4 IC50 = 590.0 nM 6.23 Inhibition of CYP3A4 17574423
Cytochrome P450 2C9 IC50 = 12000.0 nM 4.92 Inhibition of CYP2C9 17574423
Cytochrome P450 2D6 IC50 = 19000.0 nM 4.72 Inhibition of CYP2D6 17574423

Literature References

PubMed DOI Target Context # Activities
17574423 10.1016/j.bmc.2007.05.069 Renin 1
17574423 10.1016/j.bmc.2007.05.069 Liver microsomes 1
17574423 10.1016/j.bmc.2007.05.069 No relevant target 1
17574423 10.1016/j.bmc.2007.05.069 Caco-2 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 3A4 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 2D6 1
17574423 10.1016/j.bmc.2007.05.069 Cytochrome P450 2C9 1

Data from ChEMBL 36 via Core Engine