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Compound Detail

CHEMBL4857535

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Nc1ncn(Cc2c(Cl)cncc2Cl)c2ncnc1-2

Basic Information

ChEMBL ID CHEMBL4857535
Phase Preclinical
Structure Type MOL
InChI Key KMNIIJGMSOSTDR-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

295.1
MW (Da)
2.11
ALogP
6
HBA
1
HBD
82.5
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H8Cl2N6
MW 295.13
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -0.99

Activity Summary

IC50 1 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Low molecular weight phosphotyrosine protein phosphatase
CHEMBL4903
IC50 7.08 7.08 83.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 9501.0 ng.hr.mL-1 Mus musculus
CL 18.0 mL.min-1.kg-1 Mus musculus
Cmax 27852.13 nM Mus musculus
F 100.0 % Mus musculus
T1/2 0.71 hr Mus musculus
Vd 0.81 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33914534 10.1021/acs.jmedchem.0c02126 ADMET 10
33914534 10.1021/acs.jmedchem.0c02126 Mus musculus 4
33914534 10.1021/acs.jmedchem.0c02126 Low molecular weight phosphotyrosine protein phosphatase 2

Data from ChEMBL 36 via Core Engine