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Compound Detail

CHEMBL4875137

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Cc1ccccc1-c1nc2c(N)ncn(Cc3c(Cl)cncc3Cl)c-2n1

Basic Information

ChEMBL ID CHEMBL4875137
Phase Preclinical
Structure Type MOL
InChI Key UVQGPPRBCFJWSO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
2
Publications
0
Known Names

Molecular Properties

385.3
MW (Da)
4.09
ALogP
6
HBA
1
HBD
82.5
PSA (Ų)
0.57
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H14Cl2N6
MW 385.26
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.10

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Low molecular weight phosphotyrosine protein phosphatase
CHEMBL4903
IC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 38.0 ng.hr.mL-1 Mus musculus
CL 103.0 mL.min-1.kg-1 Mus musculus
Cmax 44.13 nM Mus musculus
F 3.0 % Mus musculus
T1/2 1.55 hr Mus musculus
Vd 4.04 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 6
33914534 10.1021/acs.jmedchem.0c02126 Low molecular weight phosphotyrosine protein phosphatase 1

Data from ChEMBL 36 via Core Engine