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Compound Detail

CHEMBL340297

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Cn1cc(CC[C@H](CO)n2cnc(C(N)=O)c2)c2cc(OCCCc3ccc(Cl)cc3)ccc21

Basic Information

ChEMBL ID CHEMBL340297
Phase Preclinical
Structure Type MOL
InChI Key LOLFJCSELDRAPA-OAQYLSRUSA-N
1
Targets
2
Activities
2
Assay Types
11
PK Parameters
4
Publications
0
Known Names

Molecular Properties

481.0
MW (Da)
4.30
ALogP
6
HBA
2
HBD
95.3
PSA (Ų)
0.31
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 C26H29ClN4O3
MW 481.00
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -0.61

Activity Summary

IC50 1 meas. best 8.17
Ki 1 meas. best 8.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenosine deaminase
CHEMBL1910
Ki 8.31 8.31 4.9 1
Adenosine deaminase
CHEMBL1910
IC50 8.17 8.17 6.7 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 260.0 ng.hr.mL-1 Rattus norvegicus
AUC 260.0 ng.hr.mL-1 Rattus norvegicus
CL 643.0 mL.min-1.kg-1 Rattus norvegicus
CL - mL.min-1.kg-1 Canis lupus familiaris
CL - mL.min-1.kg-1 Homo sapiens
Cmax 436.59 nM Rattus norvegicus
Cmax 436.59 nM Rattus norvegicus
F 10.0 % Rattus norvegicus
F 10.0 % Rattus norvegicus
F - % Canis lupus familiaris
T1/2 1.09 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16033254 10.1021/jm050413g ADMET 8
15239652 10.1021/jm0306374 Rattus norvegicus 3
15239652 10.1021/jm0306374 Adenosine deaminase 1
16033254 10.1021/jm050413g Adenosine deaminase 1

Data from ChEMBL 36 via Core Engine