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Compound Detail

CHEMBL4205124

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Cl.O=C(O)CCN1CCC2(CC1)COc1cc(SCc3c(Cl)cccc3Cl)ccc12

Basic Information

ChEMBL ID CHEMBL4205124
Phase Preclinical
Structure Type MOL
InChI Key BCFLIUJPZYQFET-UHFFFAOYSA-N
Parent Compound CHEMBL4302786
Active Moiety CHEMBL4302786
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
5.49
ALogP
4
HBA
1
HBD
49.8
PSA (Ų)
0.59
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H24Cl3NO3S
MW 488.86
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.68

Activity Summary

EC50 2 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 5
CHEMBL2274
EC50 7.9 7.9 12.6 1
Sphingosine 1-phosphate receptor 3
CHEMBL3892
EC50 5.4 5.4 3981.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 21.0 uL/min Homo sapiens
T1/2 1.083 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 Unchecked 2
29254642 10.1016/j.bmcl.2017.12.018 No relevant target 1
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

Data from ChEMBL 36 via Core Engine