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Compound Detail

CHEMBL2376925

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CN1CCN(CCNC(=O)c2cccc(-n3ncc4cc(Nc5c(Cl)cccc5Cl)ccc43)c2)CC1

Basic Information

ChEMBL ID CHEMBL2376925
Phase Preclinical
Structure Type MOL
InChI Key SFBKURBOWXSUBT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

523.5
MW (Da)
5.05
ALogP
6
HBA
2
HBD
65.4
PSA (Ų)
0.36
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28Cl2N6O
MW 523.47
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.86

Activity Summary

IC50 2 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.3 7.3 50.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.92 5.92 1200.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 198.92 ng.hr.mL-1 Rattus norvegicus
CL 34.0 mL.min-1.kg-1 Rattus norvegicus
F 20.0 % Rattus norvegicus
T1/2 0.03333 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23518277 10.1016/j.bmcl.2013.02.082 Rattus norvegicus 4
23518277 10.1016/j.bmcl.2013.02.082 Unchecked 1
23518277 10.1016/j.bmcl.2013.02.082 Plasma 1
23518277 10.1016/j.bmcl.2013.02.082 Mitogen-activated protein kinase 8 1
23518277 10.1016/j.bmcl.2013.02.082 Brain 1
23518277 10.1016/j.bmcl.2013.02.082 Mitogen-activated protein kinase 10 1

Data from ChEMBL 36 via Core Engine