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Compound Detail

CHEMBL1938947

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Cn1cc(C(=O)Nc2ccc(-c3cccnc3)c(C(F)(F)F)c2)c(=O)c2ccccc21

Basic Information

ChEMBL ID CHEMBL1938947
Phase Preclinical
Structure Type MOL
InChI Key QOFDJYAYOCDSDG-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
1
PK Parameters
10
Publications
0
Known Names

Molecular Properties

423.4
MW (Da)
4.87
ALogP
4
HBA
1
HBD
64.0
PSA (Ų)
0.51
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H16F3N3O2
MW 423.39
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.32

Activity Summary

EC50 3 meas. best 6.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 1
CHEMBL4333
EC50 6.51 6.51 310.0 2
Sphingosine 1-phosphate receptor 3
CHEMBL3892
EC50 5.6 5.6 2500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.0 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22104144 10.1016/j.bmcl.2011.10.085 No relevant target 3
32330036 10.1021/acs.jmedchem.9b02092 ADMET 3
22104144 10.1016/j.bmcl.2011.10.085 Sphingosine 1-phosphate receptor 1 2
22104144 10.1016/j.bmcl.2011.10.085 LLC-PK1 2
32330036 10.1021/acs.jmedchem.9b02092 Sphingosine 1-phosphate receptor 1 2
32330036 10.1021/acs.jmedchem.9b02092 Sphingosine 1-phosphate receptor 3 2
22104144 10.1016/j.bmcl.2011.10.085 Sphingosine 1-phosphate receptor 3 1
22104144 10.1016/j.bmcl.2011.10.085 Liver microsomes 1
22104144 10.1016/j.bmcl.2011.10.085 Rattus norvegicus 1
32330036 10.1021/acs.jmedchem.9b02092 No relevant target 1

Data from ChEMBL 36 via Core Engine