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Compound Detail

CHEMBL3814849

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Cl.N=C(N)N1CCC[C@H]1c1nc(-c2ccc3cc(OCc4ccc(C(F)(F)F)cc4)ccc3c2)no1

Basic Information

ChEMBL ID CHEMBL3814849
Phase Preclinical
Structure Type MOL
InChI Key AGKWEAMVXLGQKS-BOXHHOBZSA-N
Parent Compound CHEMBL3815191
Active Moiety CHEMBL3815191
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

481.5
MW (Da)
5.52
ALogP
5
HBA
2
HBD
101.3
PSA (Ų)
0.29
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23ClF3N5O2
MW 517.94
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.17

Activity Summary

Ki 2 meas. best 5.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine kinase 2
CHEMBL3023
Ki 5.99 5.99 1020.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sphingosine kinase 2 Ki = 1020.0 nM 5.99 Inhibition of human recombinant SphK2 using sphingosine as substrate incubated f... 26985306

Literature References

PubMed DOI Target Context # Activities
26985306 10.1021/acsmedchemlett.5b00304 Sphingosine kinase 1 2
26985306 10.1021/acsmedchemlett.5b00304 Sphingosine kinase 2 2
26985306 10.1021/acsmedchemlett.5b00304 Unchecked 1
33445156 10.1016/j.ejmech.2020.113121 Sphingosine kinase 1 1
33445156 10.1016/j.ejmech.2020.113121 Sphingosine kinase 2 1
33445156 10.1016/j.ejmech.2020.113121 Unchecked 1

Data from ChEMBL 36 via Core Engine