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Compound Detail

CHEMBL246410

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Cc1ccc(CNC[C@H](NC(=O)CNC(=O)c2cccc(C(F)(F)F)c2)C(=O)NC(C)(C)C)cc1N

Basic Information

ChEMBL ID CHEMBL246410
Phase Preclinical
Structure Type MOL
InChI Key VKEIRGOCEUAYTA-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

507.6
MW (Da)
2.52
ALogP
5
HBA
5
HBD
125.3
PSA (Ų)
0.33
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32F3N5O3
MW 507.56
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -1.29

Activity Summary

IC50 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 2
CHEMBL4015
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 2 IC50 = 120.0 nM 6.92 Displacement of [125]MCP1 from CCR2 in human PBMCs 17720492

Literature References

PubMed DOI Target Context # Activities
17720492 10.1016/j.bmcl.2007.07.028 C-C chemokine receptor type 2 1
17720492 10.1016/j.bmcl.2007.07.028 C-C chemokine receptor type 1 1

Data from ChEMBL 36 via Core Engine