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Compound Detail

CHEMBL374483

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Cc1cn([C@H]2C=C[C@@H](COP3(=O)OCc4cc([N+](=O)[O-])ccc4O3)O2)c(=O)[nH]c1=O

Basic Information

ChEMBL ID CHEMBL374483
Phase Preclinical
Structure Type MOL
InChI Key SRMWBQBYWCFQTM-JSAANWGUSA-N
3
Targets
6
Activities
1
Assay Types
9
PK Parameters
11
Publications
0
Known Names

Molecular Properties

437.3
MW (Da)
1.94
ALogP
10
HBA
1
HBD
152.0
PSA (Ų)
0.32
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H16N3O9P
MW 437.30
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness 0.03

Activity Summary

EC50 6 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 6.54 6.54 290.0 1
CCRF-CEM
CHEMBL382
EC50 6.54 5.78 290.0 3
Human immunodeficiency virus 2
CHEMBL380
EC50 6.4 5.4 400.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.1 hr -
T1/2 0.15 hr -
T1/2 0.06 hr -
T1/2 - hr -
T1/2 0.12 hr -
T1/2 4.1 hr -
T1/2 0.15 hr -
T1/2 0.06 hr -
T1/2 0.15 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9554875 10.1021/jm970664s ADMET 6
9554875 10.1021/jm970664s CCRF-CEM 4
- 10.1016/S0960-894X(96)00597-5 ADMET 3
- 10.1016/S0960-894X(96)00597-5 CCRF-CEM 3
17335187 10.1021/jm0613267 Human immunodeficiency virus 2 2
- 10.1016/S0960-894X(96)00597-5 No relevant target 1
17335187 10.1021/jm0613267 No relevant target 1
17335187 10.1021/jm0613267 CCRF-CEM 1
17335187 10.1021/jm0613267 ADMET 1
17335187 10.1021/jm0613267 Serum 1
17335187 10.1021/jm0613267 Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine