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Compound Detail

CHEMBL161641

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Cc1cc2nc(CN3CCN(C)CC3)nc(O)c2cc1CN(C)c1ccc(C(=O)NC(CCC(=O)O)C(=O)O)c(F)c1

Basic Information

ChEMBL ID CHEMBL161641
Phase Preclinical
Structure Type MOL
InChI Key JGRJYCLVVYNZMI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

582.6
MW (Da)
2.21
ALogP
9
HBA
4
HBD
159.4
PSA (Ų)
0.26
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H35FN6O6
MW 582.63
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.34

Activity Summary

IC50 1 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
IC50 7.55 7.55 28.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidylate synthase IC50 = 28.0 nM 7.55 In vitro inhibitory activity against thymidylate synthase partially purified fro... 8576912

Literature References

PubMed DOI Target Context # Activities
8576912 10.1021/jm950645n Thymidylate synthase 1
8576912 10.1021/jm950645n L1210 1

Data from ChEMBL 36 via Core Engine