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Compound Detail

CHEMBL328139

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C[C@H](O)[C@@H](CCc1cccc(Cl)c1Cl)n1cnc(C(N)=O)c1

Basic Information

ChEMBL ID CHEMBL328139
Phase Preclinical
Structure Type MOL
InChI Key HCJYSIGJDKNVRU-TVQRCGJNSA-N
1
Targets
2
Activities
2
Assay Types
16
PK Parameters
9
Publications
0
Known Names

Molecular Properties

342.2
MW (Da)
2.84
ALogP
4
HBA
2
HBD
81.1
PSA (Ų)
0.85
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C15H17Cl2N3O2
MW 342.23
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.70

Activity Summary

IC50 1 meas. best 7.82
Ki 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine deaminase
CHEMBL1910
Ki 7.89 7.89 13.0 1
Adenosine deaminase
CHEMBL1910
IC50 7.82 7.82 15.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2110.0 ng.hr.mL-1 Rattus norvegicus
AUC 2110.0 ng.hr.mL-1 Rattus norvegicus
CL 111.0 mL.min-1.kg-1 Rattus norvegicus
CL 21.0 mL.min-1.kg-1 Canis lupus familiaris
CL 4.5 mL.min-1.kg-1 Homo sapiens
CL 111.0 mL.min-1.kg-1 Rattus norvegicus
CL 21.0 mL.min-1.kg-1 Canis lupus familiaris
CL 4.5 mL.min-1.kg-1 Homo sapiens
Cmax 4762.88 nM Rattus norvegicus
Cmax 4762.88 nM Rattus norvegicus
F 44.0 % Rattus norvegicus
F 43.0 % Canis lupus familiaris
F 44.0 % Rattus norvegicus
F 43.0 % Canis lupus familiaris
T1/2 1.66 hr Rattus norvegicus
T1/2 1.66 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16033254 10.1021/jm050413g ADMET 8
15139750 10.1021/jm0499559 Rattus norvegicus 5
16033254 10.1021/jm050413g Mus musculus 3
15139750 10.1021/jm0499559 Adenosine deaminase 2
15139750 10.1021/jm0499559 Canis familiaris 2
15139750 10.1021/jm0499559 No relevant target 1
15139750 10.1021/jm0499559 ADMET 1
16033254 10.1021/jm050413g Adenosine deaminase 1
16033254 10.1021/jm050413g Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine