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Compound Detail

CHEMBL295681

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C#CCN(Cc1ccc2nc(N)nc(O)c2c1)c1ccc(C(=O)NC(CCC(=O)NC(CCC(=O)O)C(=O)O)C(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL295681
Phase Preclinical
Structure Type MOL
InChI Key KNOINSLORCVBMA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

606.6
MW (Da)
0.95
ALogP
10
HBA
7
HBD
245.4
PSA (Ų)
0.12
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30N6O9
MW 606.59
Aromatic Rings 3
Heavy Atoms 44
NP-Likeness -0.67

Activity Summary

Ki 1 meas. best 9.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL1952
Ki 9.65 9.65 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidylate synthase Ki = 0.224 nM 9.65 Compound was tested for inhibition of human (WI-L2) thymidylate synthase 2909728

Literature References

PubMed DOI Target Context # Activities
2909728 10.1021/jm00121a029 Thymidylate synthase 2

Data from ChEMBL 36 via Core Engine