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Compound Detail

CHEMBL128033

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C#CCN(Cc1cc2c(O)nc(C)nc2cc1C)c1ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)O)c(F)c1

Basic Information

ChEMBL ID CHEMBL128033
Phase Preclinical
Structure Type MOL
InChI Key HJSKHBHZEYJWNS-NRFANRHFSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

508.5
MW (Da)
2.78
ALogP
7
HBA
4
HBD
152.9
PSA (Ų)
0.30
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25FN4O6
MW 508.51
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.08

Activity Summary

IC50 4 meas. best 8.05
Ki 1 meas. best 8.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
Ki 8.12 8.12 7.5 1
Thymidylate synthase
CHEMBL3160
IC50 8.05 8.05 9.0 1
L1210
CHEMBL386
IC50 7.1 7.1 80.0 1
L1210 (RD1694)
CHEMBL614713
IC50 6.37 6.37 430.0 1
L1210 (1565)
CHEMBL614000
IC50 5.23 5.23 5920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10508430 10.1021/jm9803727 L1210 2
10508430 10.1021/jm9803727 L1210 (1565) 2
10508430 10.1021/jm9803727 L1210 (RD1694) 2
10508430 10.1021/jm9803727 Thymidylate synthase 1

Data from ChEMBL 36 via Core Engine