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Compound Detail

CHEMBL234606

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CC(C)(O)CC[C@@H](CN)C[C@H](O)[C@H](Cc1cccc(F)c1)NC(=O)c1cnc2ccccc2n1

Basic Information

ChEMBL ID CHEMBL234606
Phase Preclinical
Structure Type MOL
InChI Key CDMIHUXRKUKJQL-OUOWLKGYSA-N
2
Targets
2
Activities
1
Assay Types
10
PK Parameters
6
Publications
0
Known Names

Molecular Properties

468.6
MW (Da)
2.99
ALogP
6
HBA
4
HBD
121.4
PSA (Ų)
0.34
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33FN4O3
MW 468.57
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.09

Activity Summary

IC50 2 meas. best 7.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.18 7.18 66.0 1
C-C chemokine receptor type 1
CHEMBL2413
IC50 6.32 6.32 480.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.0 mL.min-1.kg-1 Homo sapiens
CL 38.0 mL.min-1.kg-1 Rattus norvegicus
CL 11.0 mL.min-1.kg-1 Canis lupus familiaris
CL 20.0 mL.min-1.kg-1 Macaca fascicularis
CL 13.0 mL.min-1.kg-1 Canis lupus familiaris
CL 17.0 mL.min-1.kg-1 Macaca fascicularis
F 48.0 % Canis lupus familiaris
F 10.0 % Macaca fascicularis
T1/2 1.5 hr Canis lupus familiaris
T1/2 0.9 hr Macaca fascicularis

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 66.0 nM 7.18 Activity at CCL3 by chemotaxis assay 17383873
C-C chemokine receptor type 1 IC50 = 480.0 nM 6.32 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 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