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Compound Detail

CHEMBL263325

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Cc1nc(O)c2cc(CN(C)c3ccc(C(=O)N[C@@H](CCC(=O)N[C@H](CCC(=O)O)C(=O)O)C(=O)O)c(F)c3)ccc2n1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL263325
Phase Preclinical
Structure Type MOL
InChI Key PGNLNOVZZMPIDB-NSLUPJTDSA-N
Parent Compound CHEMBL1182734
Active Moiety CHEMBL1182734
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

599.6
MW (Da)
1.82
ALogP
9
HBA
6
HBD
219.3
PSA (Ų)
0.16
QED
2
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H31F4N5O11
MW 713.59
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness -0.99

Activity Summary

IC50 4 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL3160
IC50 8.06 8.06 8.8 1
L1210
CHEMBL386
IC50 6.19 6.19 650.0 1
WIL2
CHEMBL612809
IC50 6.05 6.05 900.0 1
L1210 (1565)
CHEMBL614000
IC50 4.68 4.68 21000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8568829 10.1021/jm950471+ Thymidylate synthase 1
8568829 10.1021/jm950471+ L1210 1
8568829 10.1021/jm950471+ WIL2 1
8568829 10.1021/jm950471+ L1210 (1565) 1

Data from ChEMBL 36 via Core Engine