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Compound Detail

CHEMBL24701

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C#CCN(Cc1ccc2nc(C)n(C)c(=O)c2c1)c1ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL24701
Phase Preclinical
Structure Type MOL
InChI Key ZZLZQCHJVCQSAK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

490.5
MW (Da)
1.93
ALogP
7
HBA
3
HBD
141.8
PSA (Ų)
0.37
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26N4O6
MW 490.52
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.94

Activity Summary

IC50 1 meas. best 4.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL1952
IC50 4.95 4.95 11300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidylate synthase IC50 = 11300.0 nM 4.95 Inhibition of purified human thymidylate synthase from a SV40-transformed human ... 2542557

Literature References

PubMed DOI Target Context # Activities
2542557 10.1021/jm00126a023 Thymidylate synthase 1
2542557 10.1021/jm00126a023 Unchecked 1

Data from ChEMBL 36 via Core Engine