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Compound Detail

CHEMBL1789784

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N=C(N)[C@@H]1CCCN1C(=O)c1ccc(-c2nc(-c3cccc(CCC4CCCCC4)c3)co2)cc1

Basic Information

ChEMBL ID CHEMBL1789784
Phase Preclinical
Structure Type MOL
InChI Key NVUDSIMEAKSLGA-SANMLTNESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

470.6
MW (Da)
6.06
ALogP
4
HBA
2
HBD
96.2
PSA (Ų)
0.32
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34N4O2
MW 470.62
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.71

Activity Summary

Ki 2 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine kinase 1
CHEMBL4394
Ki 7.33 7.33 47.0 1
Sphingosine kinase 2
CHEMBL3023
Ki 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sphingosine kinase 1 Ki = 47.0 nM 7.33 Inhibition of SK1 (unknown origin) 26780304
Sphingosine kinase 2 Ki = 4200.0 nM 5.38 Inhibition of SK2 (unknown origin) 26780304

Literature References

PubMed DOI Target Context # Activities
26780304 10.1021/acs.jmedchem.5b01439 Sphingosine kinase 1 1
26780304 10.1021/acs.jmedchem.5b01439 Sphingosine kinase 2 1

Data from ChEMBL 36 via Core Engine