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Compound Detail

CHEMBL550795

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O=C(O)c1ccc(-c2c[nH]c3ncc(-c4ccccc4)cc23)cc1

Basic Information

ChEMBL ID CHEMBL550795
Phase Preclinical
Structure Type MOL
InChI Key KSFDVNIKNYXUIP-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

314.3
MW (Da)
4.60
ALogP
2
HBA
2
HBD
66.0
PSA (Ų)
0.58
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C20H14N2O2
MW 314.34
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -0.40

Activity Summary

IC50 4 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Sgk1
CHEMBL2343
IC50 7.4 6.645 40.0 2
Tyrosine-protein kinase receptor UFO
CHEMBL4895
IC50 6.74 6.74 182.0 1
Calcium/calmodulin-dependent protein kinase kinase 2
CHEMBL5284
IC50 6.7 6.7 199.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 392.0 ng.hr.mL-1 Rattus norvegicus
AUC 154.0 ng.hr/ml/mg/kg Rattus norvegicus
CL 64.4 mL.min-1.kg-1 Rattus norvegicus
T1/2 9.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19497745 10.1016/j.bmcl.2009.05.051 Rattus norvegicus 5
19497745 10.1016/j.bmcl.2009.05.051 Serine/threonine-protein kinase Sgk1 2
28094183 10.1016/j.bmcl.2017.01.015 Tyrosine-protein kinase receptor UFO 2
19497745 10.1016/j.bmcl.2009.05.051 No relevant target 1
29653895 10.1016/j.bmcl.2018.03.034 Calcium/calmodulin-dependent protein kinase kinase 2 1
29653895 10.1016/j.bmcl.2018.03.034 No relevant target 1

Data from ChEMBL 36 via Core Engine