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Compound Detail

CHEMBL546890

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COc1ccc(CNc2ccc3nc(N)nc(N)c3c2)cc1

Basic Information

ChEMBL ID CHEMBL546890
Phase Preclinical
Structure Type MOL
InChI Key RQSBJSIIKPEFOX-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

295.4
MW (Da)
2.41
ALogP
6
HBA
3
HBD
99.1
PSA (Ų)
0.68
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 C16H17N5O
MW 295.35
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.10

Activity Summary

IC50 2 meas. best 5.24
Kd 2 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL4614
Kd 5.8 5.8 1580.0 1
Pteridine reductase 1
CHEMBL6194
Kd 5.54 5.54 2850.0 1
No relevant target
CHEMBL2362975
IC50 5.24 5.24 5720.0 1
Leishmania mexicana
CHEMBL612880
IC50 4.84 4.84 14590.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25576738 10.1016/j.ejmech.2014.12.051 No relevant target 2
25576738 10.1016/j.ejmech.2014.12.051 Leishmania mexicana 2
25899334 10.1016/j.ejmech.2015.04.028 Trypanosoma cruzi 2
25899334 10.1016/j.ejmech.2015.04.028 Plasmodium berghei 2
25576738 10.1016/j.ejmech.2014.12.051 Bifunctional dihydrofolate reductase-thymidylate synthase 1
25576738 10.1016/j.ejmech.2014.12.051 Pteridine reductase 1 1
25899334 10.1016/j.ejmech.2015.04.028 Leishmania mexicana 1
25899334 10.1016/j.ejmech.2015.04.028 Vero 1
25899334 10.1016/j.ejmech.2015.04.028 No relevant target 1

Data from ChEMBL 36 via Core Engine