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Compound Detail

CHEMBL39851

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Nc1nc(O)c2c(Cl)c(NCc3ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc3)ccc2n1

Basic Information

ChEMBL ID CHEMBL39851
Phase Preclinical
Structure Type MOL
InChI Key GBFUWHPCXNMVFC-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

473.9
MW (Da)
2.23
ALogP
8
HBA
6
HBD
187.8
PSA (Ų)
0.27
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20ClN5O6
MW 473.87
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.56

Activity Summary

IC50 6 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 7.0 7.0 100.0 1
Thymidylate synthase
CHEMBL3160
IC50 5.4 5.4 4000.0 1
HT-29
CHEMBL384
IC50 5.17 5.17 6700.0 1
HuTu80
CHEMBL614582
IC50 5.07 5.07 8500.0 1
WiDr
CHEMBL614647
IC50 4.96 4.96 11000.0 1
SW480
CHEMBL612544
IC50 4.42 4.42 38000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3339615 10.1021/jm00397a031 Thymidylate synthase 1
3339615 10.1021/jm00397a031 Dihydrofolate reductase 1
3612694 10.1021/jm00391a042 HuTu80 1
3612694 10.1021/jm00391a042 HT-29 1
3612694 10.1021/jm00391a042 SW480 1
3612694 10.1021/jm00391a042 WiDr 1

Data from ChEMBL 36 via Core Engine