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Compound Detail

CHEMBL5416039

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Cn1cc2cc(-n3cc4cnc(NCC(F)(F)F)nc4c(-c4ccc(OC(F)F)cc4)c3=O)ccc2n1

Basic Information

ChEMBL ID CHEMBL5416039
Phase Preclinical
Structure Type MOL
InChI Key FDMGAADQKLIBRB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

516.4
MW (Da)
4.91
ALogP
8
HBA
1
HBD
86.9
PSA (Ų)
0.32
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17F5N6O2
MW 516.43
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.48

Activity Summary

IC50 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
S-adenosylmethionine synthase isoform type-2
CHEMBL3313835
IC50 7.3 7.3 50.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
S-adenosylmethionine synthase isoform type-2 IC50 = 50.0 nM 7.3 Inhibition of human MAT2A 37591318

Literature References

PubMed DOI Target Context # Activities
37591318 10.1016/j.bmcl.2023.129450 S-adenosylmethionine synthase isoform type-2 2
37591318 10.1016/j.bmcl.2023.129450 S-adenosylmethionine synthase isoform type-1 2

Data from ChEMBL 36 via Core Engine