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Compound Detail

CHEMBL1681876

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CNC(=O)c1cnc(N2CCN(C3CCN(Cc4ccc(Cl)cc4)CC3)[C@@H](c3ccccc3)C2)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL1681876
Phase Preclinical
Structure Type MOL
InChI Key BQGPSOUAQNSHSM-HHHXNRCGSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

538.5
MW (Da)
5.28
ALogP
5
HBA
1
HBD
51.7
PSA (Ų)
0.46
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H33Cl2N5O
MW 538.52
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.44

Activity Summary

IC50 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 3
CHEMBL4441
IC50 6.08 6.08 830.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-X-C chemokine receptor type 3 IC50 = 830.0 nM 6.08 Antagonist activity at human CXCR3 21277198

Literature References

PubMed DOI Target Context # Activities
21277198 10.1016/j.bmcl.2010.12.114 C-X-C chemokine receptor type 3 1

Data from ChEMBL 36 via Core Engine