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Compound Detail

CHEMBL491312

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C=CC(F)(F)[C@@H](Nc1c(Nc2cccc(C(=O)N(C)C)c2O)c(=O)c1=O)c1ccc(C)o1

Basic Information

ChEMBL ID CHEMBL491312
Phase Preclinical
Structure Type MOL
InChI Key GOXSELCOLRKLCT-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

445.4
MW (Da)
3.31
ALogP
7
HBA
3
HBD
111.9
PSA (Ų)
0.28
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H21F2N3O5
MW 445.42
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.81

Activity Summary

Ki 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
Ki 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-X-C chemokine receptor type 2 Ki = 9.0 nM 8.05 Binding affinity to CXCR2 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

Data from ChEMBL 36 via Core Engine