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Compound Detail

CHEMBL4749428

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O=P(O)(O)CP(=O)(O)OC[C@H]1O[C@@H](n2ncc3c(NC4CCCC4)nc(Cl)nc32)[C@H](O)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL4749428
Phase Preclinical
Structure Type MOL
InChI Key NFTWTQKEWHLKFB-RTWAVKEYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

527.8
MW (Da)
0.79
ALogP
11
HBA
6
HBD
209.4
PSA (Ų)
0.21
QED
3
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H24ClN5O9P2
MW 527.80
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.12

Activity Summary

IC50 1 meas. best 10.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5'-nucleotidase
CHEMBL5957
IC50 10.57 10.57 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 10.5 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5'-nucleotidase IC50 = 0.027 nM 10.57 Inhibition of human CD73 expressed in CHO cells using AMP as substrate preincuba... 32614585

Literature References

PubMed DOI Target Context # Activities
32614585 10.1021/acs.jmedchem.0c00525 5'-nucleotidase 1
32614585 10.1021/acs.jmedchem.0c00525 ADMET 1

Data from ChEMBL 36 via Core Engine