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Compound Detail

CHEMBL501916

LODENOSINE
🧪 Phase II
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🧪 Phase II
Nc1ncnc2c1ncn2[C@@H]1O[C@H](CO)C[C@@H]1F

Basic Information

ChEMBL ID CHEMBL501916
Name LODENOSINE
Phase Phase II
Structure Type MOL
InChI Key KBEMFSMODRNJHE-JFWOZONXSA-N

Known Names

F-DDA Lodenosina Lodenosine NSC-613792
3
Targets
7
Activities
2
Assay Types
14
PK Parameters
20
Publications
4
Known Names

Molecular Properties

253.2
MW (Da)
0.03
ALogP
7
HBA
2
HBD
99.1
PSA (Ų)
0.78
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -nosine
USAN Year 1997

Extended Properties

Molecular Formula C10H12FN5O2
MW 253.24
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness 0.70

Activity Summary

EC50 6 meas. best 5.94
IC50 1 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 5.94 5.7467 1160.0 3
ADMET
CHEMBL612558
IC50 5.48 5.48 3300.0 1
CCRF-CEM
CHEMBL382
EC50 4.43 4.415 36700.0 2
ADMET
CHEMBL612558
EC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3.0 - Mus musculus
AUC 3.9 - Mus musculus
AUC 0.8 - Mus musculus
AUC - - Mus musculus
AUC 8.6 - Mus musculus
AUC 4.8 - Mus musculus
AUC 1.0 - Mus musculus
AUC - - Mus musculus
T1/2 2.92 - Mus musculus
T1/2 0.91 - Mus musculus
T1/2 1.74 - Mus musculus
T1/2 - - Mus musculus
T1/2 - hr -
T1/2 0.01667 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2106581 10.1021/jm00165a015 H9 18
8917656 10.1021/jm960140c Mus musculus 16
2033591 10.1021/jm00109a018 ADMET 15
10229630 10.1021/jm981097r CCRF-CEM 3
11430019 10.1021/np0003995 ADMET 2
11430019 10.1021/np0003995 Human immunodeficiency virus 1 2
- 10.1016/0960-894X(95)00133-E ADMET 2
- 10.1016/0960-894X(95)00133-E Homo sapiens 2
3499515 10.1021/jm00394a034 MT4 2
10229630 10.1021/jm981097r C3H/3T3 2
2033591 10.1021/jm00109a018 No relevant target 1
34213340 10.1021/acs.jmedchem.1c00790 No relevant target 1
8648601 10.1021/jm9509197 ADMET 1
10229630 10.1021/jm981097r Unchecked 1
10229630 10.1021/jm981097r No relevant target 1
10229630 10.1021/jm981097r ADMET 1
3499515 10.1021/jm00394a034 Unchecked 1
- 10.1016/0960-894X(95)00133-E Vero 1
- 10.1016/0960-894X(95)00133-E CCRF-CEM 1
7520081 10.1021/jm00042a005 Human immunodeficiency virus type 1 reverse transcriptase 1

Data from ChEMBL 36 via Core Engine