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Compound Detail

CHEMBL22477

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Nc1nc(N)c2c(COc3ccc4ccccc4c3)coc2n1

Basic Information

ChEMBL ID CHEMBL22477
Phase Preclinical
Structure Type MOL
InChI Key YDFHNAXSZILGRP-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

306.3
MW (Da)
3.12
ALogP
6
HBA
2
HBD
100.2
PSA (Ų)
0.60
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N4O2
MW 306.32
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -0.43

Activity Summary

IC50 4 meas. best 4.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1926
IC50 4.85 4.85 14000.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.22 4.22 60256.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9548816 10.1021/jm970537w Dihydrofolate reductase 2
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 2
9548816 10.1021/jm970537w Bifunctional dihydrofolate reductase-thymidylate synthase 1
9548816 10.1021/jm970537w Dihydrofolate reductase; P. carinii vs rat 1
9548816 10.1021/jm970537w Dihydrofolate reductase; T. gondii vs rat 1
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine