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Compound Detail

CHEMBL207725

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CCCCCCCCSc1cc(N[C@@H](CC(C)C)C(=O)NCCCOCC)nc(-n2ccnc2)n1

Basic Information

ChEMBL ID CHEMBL207725
Phase Preclinical
Structure Type MOL
InChI Key XJXYYMCUGCGBPZ-QFIPXVFZSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

504.8
MW (Da)
5.48
ALogP
8
HBA
2
HBD
94.0
PSA (Ų)
0.15
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H44N6O2S
MW 504.75
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -1.19

Activity Summary

IC50 1 meas.
Ki 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-X-C chemokine receptor type 2
CHEMBL2434
Ki 7.22 7.22 60.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-X-C chemokine receptor type 2 Ki = 60.0 nM 7.22 Binding affinity to human CXCR2 receptor transfected in CHO cell 16540318

Literature References

PubMed DOI Target Context # Activities
16540318 10.1016/j.bmcl.2006.02.028 C-X-C chemokine receptor type 2 1
16540318 10.1016/j.bmcl.2006.02.028 Liver microsomes 1
28165741 10.1021/acs.jmedchem.6b01309 C-X-C chemokine receptor type 2 1

Data from ChEMBL 36 via Core Engine