Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL518857

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CN(C)C(=O)c1cccc(Nc2c(N[C@@H](c3ccc4c(c3)OCO4)C(F)(F)F)c(=O)c2=O)c1O

Basic Information

ChEMBL ID CHEMBL518857
Phase Preclinical
Structure Type MOL
InChI Key YVZGSKYWJOEQBN-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

477.4
MW (Da)
2.88
ALogP
8
HBA
3
HBD
117.2
PSA (Ų)
0.37
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18F3N3O6
MW 477.40
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.72

Activity Summary

Ki 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
Ki 8.3 8.3 5.0 1
C-X-C chemokine receptor type 1
CHEMBL4029
Ki 8.1 8.1 8.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 4377.76 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-X-C chemokine receptor type 2 Ki = 5.0 nM 8.3 Binding affinity to CXCR2 19196511
C-X-C chemokine receptor type 1 Ki = 8.0 nM 8.1 Binding affinity to CXCR1 19196511

Literature References

PubMed DOI Target Context # Activities
19196511 10.1016/j.bmcl.2009.01.033 C-X-C chemokine receptor type 2 1
19196511 10.1016/j.bmcl.2009.01.033 C-X-C chemokine receptor type 1 1
19196511 10.1016/j.bmcl.2009.01.033 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine