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Compound Detail

CHEMBL3740090

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CC(C)CCOc1ccc(CN2CC(C(=O)O)C2)cc1

Basic Information

ChEMBL ID CHEMBL3740090
Phase Preclinical
Structure Type MOL
InChI Key DYYJMZJVDUIBGB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
13
Publications
0
Known Names

Molecular Properties

277.4
MW (Da)
2.63
ALogP
3
HBA
1
HBD
49.8
PSA (Ų)
0.83
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 C16H23NO3
MW 277.36
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.78

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 5
CHEMBL2274
IC50 8.52 8.52 3.0 1
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 5.46 5.46 3460.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 17300.0 ng.hr.mL-1 Mus musculus
Cmax 42543.99 nM Mus musculus
T1/2 3.3 hr Mus musculus
Tmax 0.4 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26509640 10.1021/acs.jmedchem.5b00928 Mus musculus 4
- 10.6019/CHEMBL4888484 Plasmodium falciparum 2
26509640 10.1021/acs.jmedchem.5b00928 Sphingosine 1-phosphate receptor 1 1
26509640 10.1021/acs.jmedchem.5b00928 Sphingosine 1-phosphate receptor 3 1
26509640 10.1021/acs.jmedchem.5b00928 Sphingosine 1-phosphate receptor 5 1
26509640 10.1021/acs.jmedchem.5b00928 Unchecked 1
26509640 10.1021/acs.jmedchem.5b00928 No relevant target 1
26509640 10.1021/acs.jmedchem.5b00928 Molecular identity unknown 1
26509640 10.1021/acs.jmedchem.5b00928 ADMET 1
26509640 10.1021/acs.jmedchem.5b00928 Cytochrome P450 1A2 1
26509640 10.1021/acs.jmedchem.5b00928 Cytochrome P450 2C9 1
26509640 10.1021/acs.jmedchem.5b00928 Cytochrome P450 2D6 1
26509640 10.1021/acs.jmedchem.5b00928 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine