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Compound Detail

CHEMBL254776

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CN(C)C(=O)c1cccc(Nc2c(N[C@@H](c3cc(F)cc(F)c3)C3CC3)c(=O)c2=O)c1O

Basic Information

ChEMBL ID CHEMBL254776
Phase Preclinical
Structure Type MOL
InChI Key YRIRIKSPUSIVKI-QGZVFWFLSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

441.4
MW (Da)
3.28
ALogP
6
HBA
3
HBD
98.7
PSA (Ų)
0.38
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 C23H21F2N3O4
MW 441.43
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.96

Activity Summary

Ki 1 meas. best 8.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
Ki 8.35 8.35 4.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - 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 = 4.5 nM 8.35 Displacement of [125I]IL8 from human CXCR2 by SPA assay 18304809

Literature References

PubMed DOI Target Context # Activities
18304809 10.1016/j.bmcl.2008.02.010 C-X-C chemokine receptor type 2 1
18304809 10.1016/j.bmcl.2008.02.010 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine