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Compound Detail

CHEMBL23338

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C/C=C/c1cc(Cc2cnc(N)nc2N)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL23338
Phase Preclinical
Structure Type MOL
InChI Key ZWUMGQPKPLFJSY-SNAWJCMRSA-N
5
Targets
6
Activities
2
Assay Types
2
PK Parameters
20
Publications
0
Known Names

Molecular Properties

300.4
MW (Da)
2.28
ALogP
6
HBA
2
HBD
96.3
PSA (Ų)
0.88
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H20N4O2
MW 300.36
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.27

Activity Summary

IC50 4 meas. best 8.49
Ki 2 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
Ki 9.05 9.05 0.9 1
Dihydrofolate reductase
CHEMBL1681620
Ki 8.85 8.85 1.4 1
Dihydrofolate reductase
CHEMBL1809
IC50 8.49 8.49 3.2 1
Dihydrofolate reductase
CHEMBL202
IC50 7.03 7.03 93.0 1
Dihydrofolate reductase
CHEMBL4012
IC50 7.03 7.03 93.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.24 4.24 57000.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 25.0 % Canis lupus familiaris
T1/2 2.25 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2754716 10.1021/jm00128a043 Dihydrofolate reductase 5
2754716 10.1021/jm00128a043 Shigella flexneri 1
2754716 10.1021/jm00128a043 Bacteroides thetaiotaomicron 1
2754716 10.1021/jm00128a043 Clostridioides difficile 1
2754716 10.1021/jm00128a043 Clostridium perfringens 1
2754716 10.1021/jm00128a043 Fusobacterium nucleatum 1
2754716 10.1021/jm00128a043 Bacteroides fragilis 1
2754716 10.1021/jm00128a043 Proteus vulgaris 1
2754716 10.1021/jm00128a043 Klebsiella aerogenes 1
2754716 10.1021/jm00128a043 Klebsiella pneumoniae 1
2754716 10.1021/jm00128a043 Serratia marcescens 1
2754716 10.1021/jm00128a043 Escherichia coli 1
3121854 10.1021/jm00396a018 Dihydrofolate reductase 1
2754716 10.1021/jm00128a043 NON-PROTEIN TARGET 1
2754716 10.1021/jm00128a043 Mycolicibacterium smegmatis 1
2754716 10.1021/jm00128a043 Pasteurella multocida 1
2754716 10.1021/jm00128a043 Staphylococcus aureus 1
2754716 10.1021/jm00128a043 Streptococcus pyogenes 1
2754716 10.1021/jm00128a043 ADMET 1
2754716 10.1021/jm00128a043 Canis familiaris 1

Data from ChEMBL 36 via Core Engine