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Compound Detail

CHEMBL3233181

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CC(C)N(C)[C@@H]1CC[C@H](N2CC[C@H](NC(=O)c3cccc(C(C)(C)C)n3)C2=O)[C@H](CS(C)(=O)=O)C1

Basic Information

ChEMBL ID CHEMBL3233181
Phase Preclinical
Structure Type MOL
InChI Key ZOFFAXRBJWRDRL-MXNKGDRCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

506.7
MW (Da)
2.63
ALogP
6
HBA
1
HBD
99.7
PSA (Ų)
0.61
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 C26H42N4O4S
MW 506.71
Aromatic Rings 1
Heavy Atoms 35
NP-Likeness -0.82

Activity Summary

IC50 1 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 2
CHEMBL4015
IC50 9.15 9.15 0.7 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 2 IC50 = 0.7 nM 9.15 Displacement of [125I]-labeled human MCP1 from CCR2 in human PBMC 24613378

Literature References

PubMed DOI Target Context # Activities
24613378 10.1016/j.bmcl.2014.02.013 C-C chemokine receptor type 2 1
24613378 10.1016/j.bmcl.2014.02.013 Voltage-gated inwardly rectifying potassium channel KCNH2 1
24613378 10.1016/j.bmcl.2014.02.013 Unchecked 1

Data from ChEMBL 36 via Core Engine