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Compound Detail

CHEMBL464902

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CN1C[C@@H](NC(=O)Nc2cccc(-c3nnnn3C)c2)[C@H](CN2CCC[C@@H](Cc3ccc(F)cc3)C2)OC1=O

Basic Information

ChEMBL ID CHEMBL464902
Phase Preclinical
Structure Type MOL
InChI Key RHPFRSVVYGFARI-IEXUWNMDSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

536.6
MW (Da)
2.91
ALogP
8
HBA
2
HBD
117.5
PSA (Ų)
0.48
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33FN8O3
MW 536.61
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.60

Activity Summary

IC50 2 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 3
CHEMBL3473
IC50 9.64 9.64 0.2 1
Cytochrome P450 2D6
CHEMBL289
IC50 5.37 5.37 4300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 3 IC50 = 0.23 nM 9.64 Binding affinity to CCR3 receptor 19010676
Cytochrome P450 2D6 IC50 = 4300.0 nM 5.37 Inhibition of CYP2D6 19010676

Literature References

PubMed DOI Target Context # Activities
19010676 10.1016/j.bmcl.2008.11.002 C-C chemokine receptor type 3 1
19010676 10.1016/j.bmcl.2008.11.002 Cytochrome P450 2D6 1
19010676 10.1016/j.bmcl.2008.11.002 Eosinophil 1

Data from ChEMBL 36 via Core Engine