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Compound Detail

CHEMBL4525944

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OC[C@H]1O[C@@H](n2cnc3c(N4CCN(c5ccc(-c6ccc(C(F)(F)F)cc6)cc5)CC4)ncnc32)[C@H](O)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL4525944
Phase Preclinical
Structure Type MOL
InChI Key PGKQOVNBSQECEZ-HUBRGWSESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

556.5
MW (Da)
2.45
ALogP
10
HBA
3
HBD
120.0
PSA (Ų)
0.34
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27F3N6O4
MW 556.55
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -0.23

Activity Summary

Ki 1 meas. best 7.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine kinase
CHEMBL4523271
Ki 7.67 7.67 21.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenosine kinase Ki = 21.3 nM 7.67 Inhibition of wild-type N-terminal TEV cleavage site-fused/His-tagged Mycobacter... 31002508

Literature References

PubMed DOI Target Context # Activities
31002508 10.1021/acs.jmedchem.9b00020 Adenosine kinase 2
31002508 10.1021/acs.jmedchem.9b00020 Mycobacterium tuberculosis 1
31002508 10.1021/acs.jmedchem.9b00020 NHDF 1

Data from ChEMBL 36 via Core Engine