Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL1236524

GALIDESIVIR
🧪 Phase II
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
🧪 Phase II
Nc1ncnc2c([C@@H]3N[C@H](CO)[C@@H](O)[C@H]3O)c[nH]c12
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1236524
Name GALIDESIVIR
Phase Phase II
Structure Type MOL
InChI Key AMFDITJFBUXZQN-KUBHLMPHSA-N
Active Moiety CHEMBL4594369

Known Names

BCX-4430 Bcx4430 Galidesivir Immucillin a
16
Targets
33
Activities
2
Assay Types
2
PK Parameters
20
Publications
4
Known Names
3
Indications
5
Mechanisms

Molecular Properties

265.3
MW (Da)
-1.73
ALogP
7
HBA
6
HBD
140.3
PSA (Ų)
0.38
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product Prodrug
USAN Stem -vir

Extended Properties

Molecular Formula C11H15N5O3
MW 265.27
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness 1.01

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
RNA-directed RNA polymerase L inhibitor INHIBITOR RNA-directed RNA polymerase L ✓ ✓
Genome polyprotein inhibitor INHIBITOR Genome polyprotein ✓ ✓
Genome polyprotein inhibitor INHIBITOR Genome polyprotein ✓ ✓
RNA-directed RNA polymerase L inhibitor INHIBITOR RNA-directed RNA polymerase L ✓ ✓
Replicase polyprotein 1ab inhibitor INHIBITOR Replicase polyprotein 1ab ✓ ✓

Indications

Fever Marburg Virus Disease Severe Acute Respiratory Syndrome

Activity Summary

EC50 31 meas. best 6.0
Ki 2 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Purine nucleoside phosphorylase
CHEMBL4338
 Ki 7.48 7.48 33.0 1
Influenza B virus
CHEMBL613129
 EC50 6.0 6.0 1000.0 1
Influenza A virus
CHEMBL613740
 EC50 6.0 5.64 1000.0 3
Measles morbillivirus
CHEMBL613738
 EC50 5.75 5.75 1800.0 1
Purine nucleoside phosphorylase
CHEMBL2935
 Ki 5.58 5.58 2600.0 1
Marburgvirus
CHEMBL4296577
 EC50 5.52 5.44 3000.0 2
Ebolavirus
CHEMBL4434621
 EC50 5.52 5.1267 3000.0 3
Sudan ebolavirus
CHEMBL5291667
 EC50 5.52 5.52 3000.0 1
Unchecked
CHEMBL612545
 EC50 5.47 5.47 3400.0 1
dengue virus type 2
CHEMBL613966
 EC50 5.38 4.874 4200.0 5
Zika virus
CHEMBL4296612
 EC50 4.92 4.7 12000.0 2
SARS-CoV-2
CHEMBL4303835
 EC50 4.85 4.4433 14150.0 3
Yellow fever virus
CHEMBL613731
 EC50 4.75 4.75 18000.0 1
Rift Valley fever virus
CHEMBL613130
 EC50 4.64 4.605 23000.0 2
Middle East respiratory syndrome-related coronavirus
CHEMBL4296578
 EC50 4.5 4.29 32000.0 5
SARS-CoV
CHEMBL4303836
 EC50 4.24 4.24 57700.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.08333 hr Mus musculus
T1/2 6.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Purine nucleoside phosphorylase Ki = 33.0 nM 7.48 Inhibition of human PNP using inosine as substrate by xanthine oxidase coupled a... 30627387
Influenza B virus EC50 = 1000.0 nM 6.0 Antiviral activity against Influenza B virus infected in dog MDCK cells assessed... 37077387
Influenza A virus EC50 = 1000.0 nM 6.0 Antiviral activity against Influenza A virus infected in dog MDCK cells assessed... 37077387
Measles morbillivirus EC50 = 1800.0 nM 5.75 Antiviral activity against Measles virus infected in African green monkey Vero c... 37077387
Purine nucleoside phosphorylase Ki = 2600.0 nM 5.58 Inhibition of bovine spleen PNP using inosine as substrate by xanthine oxidase c... 30627387
Sudan ebolavirus EC50 = 3000.0 nM 5.52 Antiviral activity against SUDV infected in human HeLa cells assessed as reducti... 37077387
Ebolavirus EC50 = 3000.0 nM 5.52 Antiviral activity against Ebola virus infected in human HeLa cells assessed as ... 37077387
Marburgvirus EC50 = 3000.0 nM 5.52 Antiviral activity against Marburg virus infected in human HeLa cells assessed a... 37077387
Influenza A virus EC50 = 3300.0 nM 5.48 Antiviral activity against Influenza A virus H1N1 infected in dog MDCK cells ass... 37077387
Unchecked EC50 = 3400.0 nM 5.47 Antiviral activity against SUDV Boniface by high-content image analysis 33352046
Influenza A virus EC50 = 3600.0 nM 5.44 Antiviral activity against Influenza A virus H1N1 infected in dog MDCK cells ass... 37077387
dengue virus type 2 EC50 = 4200.0 nM 5.38 Antiviral activity against DENV-2 infected in African green monkey Vero cells as... 37077387
Marburgvirus EC50 = 4400.0 nM 5.36 Antiviral activity against MARV musoke by high-content image analysis 33352046
Ebolavirus EC50 = 11800.0 nM 4.93 Antiviral activity against EBOV Kikwit by high-content image analysis 33352046
Ebolavirus EC50 = 11800.0 nM 4.93 Antiviral activity against EBOV Kikwit infected in HeLa cells 39248591
Zika virus EC50 = 12000.0 nM 4.92 Antiviral activity against Zika virus infected in African green monkey Vero 76 c... 37077387
dengue virus type 2 EC50 = 13000.0 nM 4.89 Antiviral activity against DENV-2 infected in human Huh-7 cells assessed as redu... 37077387
SARS-CoV-2 EC50 = 14150.0 nM 4.85 Antiviral activity against SARS-CoV-2 WA1/2020 infected in human Calu-3 cells pr... 36965227
dengue virus type 2 EC50 = 15000.0 nM 4.82 Antiviral activity against DENV-2 infected in African green monkey Vero cells as... 37077387
dengue virus type 2 EC50 = 16000.0 nM 4.8 Antiviral activity against DENV-2 infected in human Huh-7 cells assessed as redu... 37077387

Literature References

PubMed DOI Target Context # Activities
37077387 10.1021/acsmedchemlett.3c00048 ADMET 14
31549836 10.1021/acs.jmedchem.9b00775 NS5 8
37077387 10.1021/acsmedchemlett.3c00048 Vero 76 6
37077387 10.1021/acsmedchemlett.3c00048 dengue virus type 2 4
37077387 10.1021/acsmedchemlett.3c00048 Huh-7 4
37077387 10.1021/acsmedchemlett.3c00048 Middle East respiratory syndrome-related coronavirus 4
36965227 10.1016/j.ejmech.2023.115292 SARS-CoV-2 4
36965227 10.1016/j.ejmech.2023.115292 ADMET 4
37077387 10.1021/acsmedchemlett.3c00048 Influenza A virus 3
37077387 10.1021/acsmedchemlett.3c00048 Unchecked 2
37077387 10.1021/acsmedchemlett.3c00048 Rift Valley fever virus 2
37077387 10.1021/acsmedchemlett.3c00048 Yellow fever virus 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
37077387 10.1021/acsmedchemlett.3c00048 Zika virus 2
33186044 10.1021/acs.jmedchem.0c01140 ADMET 2
37077387 10.1021/acsmedchemlett.3c00048 Vero 2
30627387 10.1039/C8MD00372F Purine nucleoside phosphorylase 2
37077387 10.1021/acsmedchemlett.3c00048 MDCK 2
33352046 10.1021/acs.jnatprod.0c00968 Middle East respiratory syndrome-related coronavirus 1
39248591 10.1021/acs.jmedchem.4c01267 Ebolavirus 1

Data from ChEMBL 36 via Core Engine