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Compound Detail

CHEMBL525001

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Cc1nc2c3c(c(-n4ccccc4=O)cn2c1C)CC[C@@H](c1ccccc1)N3

Basic Information

ChEMBL ID CHEMBL525001
Phase Preclinical
Structure Type MOL
InChI Key GFGBAMIIMZDJCH-IBGZPJMESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

370.5
MW (Da)
4.20
ALogP
5
HBA
1
HBD
51.3
PSA (Ų)
0.58
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N4O
MW 370.46
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.72

Activity Summary

IC50 3 meas. best 6.2

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.2 6.2 631.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.25 5.25 5600.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.11 5.11 7700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 630.96 nM 6.2 Inhibition of H+/K+ ATPase 19467868
Cytochrome P450 2C9 IC50 = 5600.0 nM 5.25 Inhibition of CYP2C9 19467868
Cytochrome P450 3A4 IC50 = 7700.0 nM 5.11 Inhibition of CYP3A4 using diethoxyfluorescein as substrate 19467868

Literature References

PubMed DOI Target Context # Activities
19467868 10.1016/j.bmcl.2009.04.127 Cytochrome P450 3A4 2
19467868 10.1016/j.bmcl.2009.04.127 Cytochrome P450 2C9 1
19467868 10.1016/j.bmcl.2009.04.127 Rattus norvegicus 1
19467868 10.1016/j.bmcl.2009.04.127 Unchecked 1
19467868 10.1016/j.bmcl.2009.04.127 No relevant target 1

Data from ChEMBL 36 via Core Engine