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Compound Detail

CHEMBL4167589

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CN(C)c1ccc(/C=C2\CC(CO)(COC(=O)c3ccc(Cl)cc3)OC2=O)cc1

Basic Information

ChEMBL ID CHEMBL4167589
Phase Preclinical
Structure Type MOL
InChI Key JOBSWTWSOLMKSR-GZTJUZNOSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

415.9
MW (Da)
3.32
ALogP
6
HBA
1
HBD
76.1
PSA (Ų)
0.58
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 C22H22ClNO5
MW 415.87
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.15

Activity Summary

Ki 3 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ras guanyl-releasing protein 3
CHEMBL3638
Ki 8.74 8.74 1.8 1
Protein kinase C epsilon type
CHEMBL3582
Ki 8.19 8.19 6.4 1
Protein kinase C alpha type
CHEMBL299
Ki 7.59 7.59 25.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29860841 10.1021/acs.jmedchem.8b00661 Unchecked 2
29860841 10.1021/acs.jmedchem.8b00661 Protein kinase C alpha type 1
29860841 10.1021/acs.jmedchem.8b00661 Protein kinase C epsilon type 1
29860841 10.1021/acs.jmedchem.8b00661 Ras guanyl-releasing protein 3 1

Data from ChEMBL 36 via Core Engine