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Compound Detail

CHEMBL486457

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COc1ccc(C(=O)OCC2(CO)C/C(=C/c3ccncc3)C(=O)O2)cc1

Basic Information

ChEMBL ID CHEMBL486457
Phase Preclinical
Structure Type MOL
InChI Key WMHJQZNDOYVBOS-YBEGLDIGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

369.4
MW (Da)
2.01
ALogP
7
HBA
1
HBD
95.0
PSA (Ų)
0.61
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19NO6
MW 369.37
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness 0.47

Activity Summary

Ki 2 meas. best 5.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ras guanyl-releasing protein 3
CHEMBL3638
Ki 5.44 5.44 3660.0 1
Protein kinase C alpha type
CHEMBL299
Ki 4.59 4.59 25400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18707088 10.1021/jm800380b Protein kinase C alpha type 1
18707088 10.1021/jm800380b Ras guanyl-releasing protein 3 1
18707088 10.1021/jm800380b No relevant target 1
18707088 10.1021/jm800380b Unchecked 1

Data from ChEMBL 36 via Core Engine