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Compound Detail

CHEMBL351840

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CCc1ccc2nc(C)nc(O)c2c1Sc1ccncc1

Basic Information

ChEMBL ID CHEMBL351840
Phase Preclinical
Structure Type MOL
InChI Key OWOBVOVYNUJDKU-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

297.4
MW (Da)
3.75
ALogP
5
HBA
1
HBD
58.9
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15N3OS
MW 297.38
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -1.09

Activity Summary

Ki 2 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL1952
Ki 6.7 6.465 200.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Thymidylate synthase Ki = 200.0 nM 6.7 Inhibition of human Thymidylate synthase 8459400
Thymidylate synthase Ki = 590.0 nM 6.23 Inhibition of human Thymidylate synthase 8459400

Literature References

PubMed DOI Target Context # Activities
8459400 10.1021/jm00058a010 Thymidylate synthase 2
8459400 10.1021/jm00058a010 L1210 2
8459400 10.1021/jm00058a010 CCRF-CEM 1
8459400 10.1021/jm00058a010 GC3/MTK- 1
8459400 10.1021/jm00058a010 No relevant target 1

Data from ChEMBL 36 via Core Engine