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Compound Detail

CHEMBL4209494

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Cl.O=C(O)CN1CCC2(CC1)COc1cc(S(=O)(=O)Cc3c(Cl)cccc3Cl)ccc12

Basic Information

ChEMBL ID CHEMBL4209494
Phase Preclinical
Structure Type MOL
InChI Key BVSDFSLUSVZODX-UHFFFAOYSA-N
Parent Compound CHEMBL4302573
Active Moiety CHEMBL4302573
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

470.4
MW (Da)
3.78
ALogP
5
HBA
1
HBD
83.9
PSA (Ų)
0.72
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22Cl3NO5S
MW 506.84
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.83

Activity Summary

EC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 5
CHEMBL2274
EC50 6.1 6.1 794.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 33.0 uL/min Homo sapiens
T1/2 2.15 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29254642 10.1016/j.bmcl.2017.12.018 ADMET 2
29254642 10.1016/j.bmcl.2017.12.018 Sphingosine 1-phosphate receptor 3 1
29254642 10.1016/j.bmcl.2017.12.018 Sphingosine 1-phosphate receptor 1 1
29254642 10.1016/j.bmcl.2017.12.018 Sphingosine 1-phosphate receptor 5 1
29254642 10.1016/j.bmcl.2017.12.018 No relevant target 1

Data from ChEMBL 36 via Core Engine