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Compound Detail

CHEMBL4760944

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O=P(O)(O)CS(=O)(=O)C[C@H]1O[C@@H](n2ncc3c(NCc4ccccc4Cl)nc(Cl)nc32)[C@H](O)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL4760944
Phase Preclinical
Structure Type MOL
InChI Key DFTWSJXWXYKCCX-VMUDFCTBSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

568.3
MW (Da)
0.91
ALogP
11
HBA
5
HBD
197.0
PSA (Ų)
0.19
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20Cl2N5O8PS
MW 568.33
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.74

Activity Summary

IC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5'-nucleotidase
CHEMBL5957
IC50 7.89 7.89 13.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 306.9 ng.hr.mL-1 Rattus norvegicus
Cmax 60.0 nM Rattus norvegicus
T1/2 3.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
5'-nucleotidase IC50 = 13.0 nM 7.89 Inhibition of human C-terminal His6-tagged CD73 expressed in CHO cells preincuba... 32865411

Literature References

PubMed DOI Target Context # Activities
32865411 10.1021/acs.jmedchem.0c01086 ADMET 3
32865411 10.1021/acs.jmedchem.0c01086 5'-nucleotidase 1

Data from ChEMBL 36 via Core Engine