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Compound Detail

CHEMBL289749

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Cc1nc(O)c2cc(CN(C)c3ccc(C(=O)N[C@@H](CCC(=O)O)C(=O)N(C)[C@@H](CCC(=O)O)C(=O)O)c(F)c3)c(C)cc2n1

Basic Information

ChEMBL ID CHEMBL289749
Phase Preclinical
Structure Type MOL
InChI Key KQQPGFABUPFVAK-UPVQGACJSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

627.6
MW (Da)
2.47
ALogP
9
HBA
5
HBD
210.6
PSA (Ų)
0.17
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H34FN5O9
MW 627.63
Aromatic Rings 3
Heavy Atoms 45
NP-Likeness -0.83

Activity Summary

IC50 4 meas. best 6.2
Ki 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
Ki 8.52 8.52 3.0 1
WIL2
CHEMBL612809
IC50 6.2 6.2 630.0 1
Mus musculus
CHEMBL375
IC50 6.14 5.6567 730.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9154971 10.1021/jm960878u Mus musculus 3
9154971 10.1021/jm960878u Thymidylate synthase 1
9154971 10.1021/jm960878u WIL2 1

Data from ChEMBL 36 via Core Engine