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Compound Detail

CHEMBL517561

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Nc1nccc(-c2ccc3nc(C4COc5ccc(F)cc5C4)oc3c2)n1

Basic Information

ChEMBL ID CHEMBL517561
Phase Preclinical
Structure Type MOL
InChI Key SKTFFJCCFCEJCG-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

362.4
MW (Da)
3.72
ALogP
6
HBA
1
HBD
87.1
PSA (Ų)
0.58
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15FN4O2
MW 362.36
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -0.82

Activity Summary

IC50 3 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 2
CHEMBL2973
IC50 7.82 7.685 15.0 2
Unchecked
CHEMBL612545
IC50 5.54 5.54 2912.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.517 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18996009 10.1016/j.bmcl.2008.10.095 Rho-associated protein kinase 2 2
18996009 10.1016/j.bmcl.2008.10.095 Unchecked 1
18996009 10.1016/j.bmcl.2008.10.095 Liver microsomes 1

Data from ChEMBL 36 via Core Engine