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Compound Detail

CHEMBL381872

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O=C(O)C1CN(Cc2ccc(-c3noc(-c4ccc(CCC(F)(F)F)cc4)n3)cc2)C1

Basic Information

ChEMBL ID CHEMBL381872
Phase Preclinical
Structure Type MOL
InChI Key XYFAADCQOGUWOC-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

431.4
MW (Da)
4.41
ALogP
5
HBA
1
HBD
79.5
PSA (Ų)
0.60
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20F3N3O3
MW 431.41
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.30

Activity Summary

IC50 4 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 5
CHEMBL2274
IC50 9.52 9.52 0.3 1
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 9.4 9.4 0.4 1
Sphingosine 1-phosphate receptor 4
CHEMBL3230
IC50 6.37 6.37 430.0 1
Sphingosine 1-phosphate receptor 3
CHEMBL3892
IC50 4.89 4.89 13000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.3 mL.min-1.kg-1 Rattus norvegicus
F 50.0 % Rattus norvegicus
T1/2 5.8 hr Rattus norvegicus
Vd 2.3 L.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16190743 10.1021/jm0503244 ADMET 4
16190743 10.1021/jm0503244 Sphingosine 1-phosphate receptor 1 1
16190743 10.1021/jm0503244 Sphingosine 1-phosphate receptor 2 1
16190743 10.1021/jm0503244 Sphingosine 1-phosphate receptor 3 1
16190743 10.1021/jm0503244 Sphingosine 1-phosphate receptor 4 1
16190743 10.1021/jm0503244 Sphingosine 1-phosphate receptor 5 1

Data from ChEMBL 36 via Core Engine