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Compound Detail

CHEMBL1097184

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CCC/N=C1\S/C(=C\c2ccc(OCC(O)CO)c(Cl)c2)C(=O)N1c1ccccc1C

Basic Information

ChEMBL ID CHEMBL1097184
Phase Preclinical
Structure Type MOL
InChI Key LPAUOXUZGSBGDU-XHOZKXSISA-N
2
Targets
2
Activities
1
Assay Types
9
PK Parameters
6
Publications
0
Known Names

Molecular Properties

461.0
MW (Da)
4.27
ALogP
6
HBA
2
HBD
82.4
PSA (Ų)
0.57
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN2O4S
MW 460.98
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.12

Activity Summary

EC50 2 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 1
CHEMBL4333
EC50 7.92 7.92 12.0 1
Sphingosine 1-phosphate receptor 3
CHEMBL3892
EC50 6.76 6.76 174.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.0 mL.min-1.g-1 Homo sapiens
CL 9.1 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL - - Canis lupus familiaris
CL 41.0 mL.min-1.kg-1 Rattus norvegicus
CL - - Canis lupus familiaris
CL 27.0 mL.min-1.g-1 Rattus norvegicus
Cmax 674.65 nM Rattus norvegicus
F 90.0 % Rattus norvegicus
T1/2 1.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20446681 10.1021/jm100181s Rattus norvegicus 8
20446681 10.1021/jm100181s Liver microsomes 2
20446681 10.1021/jm100181s ADMET 2
20446681 10.1021/jm100181s Hepatocyte 1
20446681 10.1021/jm100181s Sphingosine 1-phosphate receptor 3 1
20446681 10.1021/jm100181s Sphingosine 1-phosphate receptor 1 1

Data from ChEMBL 36 via Core Engine