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Compound Detail

CHEMBL254881

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CCc1cc(NC(=O)N[C@H](C)[C@@H](O)CN(CCCc2ccc(F)cc2)CC2CC2)cc(-c2nnnn2C)c1

Basic Information

ChEMBL ID CHEMBL254881
Phase Preclinical
Structure Type MOL
InChI Key JBSFMYIPFYTPEY-BCHFMIIMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

523.7
MW (Da)
3.79
ALogP
7
HBA
3
HBD
108.2
PSA (Ų)
0.31
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H38FN7O2
MW 523.66
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 3
CHEMBL3473
IC50 9.22 9.22 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 3 IC50 = 0.6 nM 9.22 Displacement of [125I] eotaxin from human CCR3 receptor in CHO cells 18160284

Literature References

PubMed DOI Target Context # Activities
18160284 10.1016/j.bmcl.2007.11.087 C-C chemokine receptor type 3 2

Data from ChEMBL 36 via Core Engine