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Compound Detail

CHEMBL397749

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N=C(N)Nc1nc(C(CCN2CCC(c3ccccc3)CC2)C(=O)NCc2cc(C(F)(F)F)cc(C(F)(F)F)c2)cs1

Basic Information

ChEMBL ID CHEMBL397749
Phase Preclinical
Structure Type MOL
InChI Key WMZBGVXJAMWDEI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

612.6
MW (Da)
6.16
ALogP
5
HBA
4
HBD
107.1
PSA (Ų)
0.13
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30F6N6OS
MW 612.64
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -1.23

Activity Summary

IC50 1 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 2
CHEMBL4015
IC50 8.89 8.89 1.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 2 IC50 = 1.3 nM 8.89 Displacement of [125I]MCP1 from human CCR2 expressed in monocytes 17092717

Literature References

PubMed DOI Target Context # Activities
17092717 10.1016/j.bmcl.2006.10.059 C-C chemokine receptor type 2 1

Data from ChEMBL 36 via Core Engine