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Compound Detail

CHEMBL391239

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COS(=O)(=O)NC(=O)Cc1cc(Cl)ccc1OCC(=O)N1C[C@H](C)N(Cc2ccc(F)cc2)C[C@H]1C

Basic Information

ChEMBL ID CHEMBL391239
Phase Preclinical
Structure Type MOL
InChI Key PKPSNPAVDRFCKI-DLBZAZTESA-N
2
Targets
2
Activities
1
Assay Types
13
PK Parameters
7
Publications
0
Known Names

Molecular Properties

542.0
MW (Da)
2.53
ALogP
7
HBA
1
HBD
105.2
PSA (Ų)
0.52
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 C24H29ClFN3O6S
MW 542.03
Aromatic Rings 2
Heavy Atoms 36
NP-Likeness -1.33

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.7 8.7 2.0 1
C-C chemokine receptor type 1
CHEMBL2413
IC50 7.36 7.36 44.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.7 mL.min-1.kg-1 Homo sapiens
CL 26.0 mL.min-1.kg-1 Rattus norvegicus
CL 11.0 mL.min-1.kg-1 Canis lupus familiaris
CL 18.0 mL.min-1.kg-1 Macaca fascicularis
CL 0.09 mL.min-1.kg-1 Canis lupus familiaris
CL 1.2 mL.min-1.kg-1 Macaca fascicularis
CL 4.5 mL.min-1.kg-1 Rattus norvegicus
F 100.0 % Canis lupus familiaris
F 24.0 % Macaca fascicularis
F 19.0 % Rattus norvegicus
T1/2 13.0 hr Canis lupus familiaris
T1/2 1.2 hr Macaca fascicularis
T1/2 1.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 2.0 nM 8.7 Activity at CCL3 by chemotaxis assay 17383873
C-C chemokine receptor type 1 IC50 = 44.0 nM 7.36 Binding Affinity at CCL3 17383873

Literature References

PubMed DOI Target Context # Activities
17383873 10.1016/j.bmcl.2007.03.037 Canis familiaris 4
17383873 10.1016/j.bmcl.2007.03.037 Cynomolgus monkey 4
17383873 10.1016/j.bmcl.2007.03.037 Rattus norvegicus 4
17383873 10.1016/j.bmcl.2007.03.037 Liver microsomes 2
17383873 10.1016/j.bmcl.2007.03.037 ADMET 2
17383873 10.1016/j.bmcl.2007.03.037 C-C chemokine receptor type 1 1
17383873 10.1016/j.bmcl.2007.03.037 Unchecked 1

Data from ChEMBL 36 via Core Engine