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Compound Detail

CHEMBL224720

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FC(F)(F)c1cccc(-c2noc(-c3cc(-c4ccccc4)c(C(F)(F)F)s3)n2)c1

Basic Information

ChEMBL ID CHEMBL224720
Phase Preclinical
Structure Type MOL
InChI Key OYMNPJXKQVTQTR-UHFFFAOYSA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

440.4
MW (Da)
7.17
ALogP
4
HBA
0
HBD
38.9
PSA (Ų)
0.32
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H10F6N2OS
MW 440.37
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.38

Activity Summary

EC50 4 meas. best 7.89
IC50 3 meas. best 7.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sphingosine 1-phosphate receptor 1
CHEMBL4333
EC50 7.89 6.59 13.0 4
Sphingosine 1-phosphate receptor 1
CHEMBL4333
IC50 7.43 7.43 37.0 2
Sphingosine 1-phosphate receptor 5
CHEMBL2274
IC50 5.34 5.34 4600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724696 U2OS 24
- 10.6019/CHEMBL5724696 TERT-RPE1 24
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4689842 HEK-293T 10
- 10.6019/CHEMBL4689842 Fibroblast 9
22104144 10.1016/j.bmcl.2011.10.085 Sphingosine 1-phosphate receptor 1 2
- 10.6019/CHEMBL5209801 Adhesion G-protein coupled receptor F1 2
- 10.6019/CHEMBL5209801 CX3C chemokine receptor 1 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL5209801 G-protein coupled receptor 35 2
- 10.6019/CHEMBL5209801 N-formyl peptide receptor 2 2
- 10.6019/CHEMBL5442687 Sphingosine 1-phosphate receptor 1 2
- 10.6019/CHEMBL5209801 Alpha-2A adrenergic receptor 2
- 10.6019/CHEMBL5209801 Sphingosine 1-phosphate receptor 1 2
- 10.6019/CHEMBL5209801 Type-1 angiotensin II receptor 2
- 10.6019/CHEMBL5209801 C5a anaphylatoxin chemotactic receptor 1 2
- 10.6019/CHEMBL5209801 Free fatty acid receptor 4 2
- 10.6019/CHEMBL5209801 Glucose-dependent insulinotropic receptor 2
- 10.6019/CHEMBL5209801 Apelin receptor 2

Data from ChEMBL 36 via Core Engine