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Compound Detail

CHEMBL464301

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CN(C)C(=O)c1cccc(Nc2c(N[C@@H](c3ccccc3)C(F)(F)F)c(=O)c2=O)c1O

Basic Information

ChEMBL ID CHEMBL464301
Phase Preclinical
Structure Type MOL
InChI Key IPLGVPPLWIAZSG-IBGZPJMESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

433.4
MW (Da)
3.15
ALogP
6
HBA
3
HBD
98.7
PSA (Ų)
0.41
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 C21H18F3N3O4
MW 433.39
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.89

Activity Summary

Ki 2 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
Ki 7.85 7.85 14.0 1
C-X-C chemokine receptor type 1
CHEMBL4029
Ki 7.4 7.4 40.0 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 = 14.0 nM 7.85 Binding affinity to CXCR2 19196511
C-X-C chemokine receptor type 1 Ki = 40.0 nM 7.4 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

Data from ChEMBL 36 via Core Engine