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Compound Detail

CHEMBL313814

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O=C(NC1CNCCC[C@H]1OC(=O)c1cc(O)c(Cc2c(O)cccc2C(=O)O)c(O)c1)c1ccc(O)cc1

Basic Information

ChEMBL ID CHEMBL313814
Phase Preclinical
Structure Type MOL
InChI Key JKBLKEZCQDCPCX-UIDYPRJRSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

536.5
MW (Da)
2.51
ALogP
9
HBA
7
HBD
185.7
PSA (Ų)
0.22
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 C28H28N2O9
MW 536.54
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness 0.45

Activity Summary

IC50 1 meas. best 6.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
cAMP-dependent protein kinase catalytic subunit alpha
CHEMBL2654
IC50 6.33 6.33 470.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
cAMP-dependent protein kinase catalytic subunit alpha IC50 = 470.0 nM 6.33 Inhibition of cAMP-dependent Protein kinase A (PKA) 12036372

Literature References

PubMed DOI Target Context # Activities
12036372 10.1021/jm020018f Protein kinase C alpha type 1
12036372 10.1021/jm020018f Protein kinase C beta type 1
12036372 10.1021/jm020018f Protein kinase C epsilon type 1
12036372 10.1021/jm020018f cAMP-dependent protein kinase catalytic subunit alpha 1

Data from ChEMBL 36 via Core Engine