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Compound Detail

CHEMBL3919119

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N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(CN)cc1)NC(=O)c1ccccc1)B(O)O

Basic Information

ChEMBL ID CHEMBL3919119
Phase Preclinical
Structure Type MOL
InChI Key FSDWYLVZNOVGAG-OALUTQOASA-N
8
Targets
99
Activities
3
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

454.3
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H31BN6O4
MW 454.34

Activity Summary

IC50 93 meas. best 7.19
Ki 4 meas. best 7.4
EC50 2 meas. best 4.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nonstructural protein 3
CHEMBL4523954
Ki 7.4 7.4 40.0 1
Unchecked
CHEMBL612545
Ki 7.4 7.26 40.0 3
NS3
CHEMBL5705861
IC50 7.19 6.925 65.0 2
Unchecked
CHEMBL612545
IC50 7.18 6.9133 66.0 3
Nonstructural protein 3
CHEMBL4523954
IC50 7.14 6.5171 73.0 28
Genome polyprotein
CHEMBL5980
IC50 6.65 6.4226 222.0 53
NS3 protease
CHEMBL5705862
IC50 6.51 6.505 310.0 2
NS3 protease
CHEMBL5705864
IC50 6.3 6.2 503.0 2
NS3 protease
CHEMBL5705863
IC50 6.11 6.07 784.0 3
NON-PROTEIN TARGET
CHEMBL3879801
EC50 4.52 4.47 30000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 40.0 nM 7.4 Inhibition of Zika virus N-terminal His-tagged NS2B-NS3 protease expressed in Es... 27966962
Nonstructural protein 3 Ki = 40.0 nM 7.4 Inhibition of N-terminal His6-tagged Zika virus NS2B (49 to 95 residues) - NS3 (... 31549836
Unchecked Ki = 51.0 nM 7.29 Inhibition of Dengue virus serotype 2 His-tagged NS2B-NS3 protease using Abz-Nle... 27966962
NS3 IC50 = 65.0 nM 7.19 Functional biochemical assay to identify treatments for viral infectious disease... -
Unchecked IC50 = 66.0 nM 7.18 Inhibition of Dengue virus serotype 2 His-tagged NS2B-NS3 protease using Abz-Nle... 27966962
Nonstructural protein 3 IC50 = 73.0 nM 7.14 Functional biochemical assay to identify treatments for viral infectious disease... -
Unchecked Ki = 82.0 nM 7.09 Inhibition of West Nile virus His-tagged NS2B-NS3 protease expressed in Escheric... 27966962
Unchecked IC50 = 110.0 nM 6.96 Inhibition of West Nile virus His-tagged NS2B-NS3 protease expressed in Escheric... 27966962
Nonstructural protein 3 IC50 = 141.0 nM 6.85 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 186.0 nM 6.73 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 211.0 nM 6.68 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 211.0 nM 6.68 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 217.0 nM 6.66 Functional biochemical assay to identify treatments for viral infectious disease... -
Genome polyprotein IC50 = 222.0 nM 6.65 Functional biochemical assay to identify treatments for viral infectious disease... -
Genome polyprotein IC50 = 236.0 nM 6.63 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 233.0 nM 6.63 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 237.0 nM 6.62 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 238.0 nM 6.62 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 241.0 nM 6.62 Functional biochemical assay to identify treatments for viral infectious disease... -
Genome polyprotein IC50 = 243.0 nM 6.61 Functional biochemical assay to identify treatments for viral infectious disease... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5604063 Genome polyprotein 63
- 10.6019/CHEMBL5604062 Nonstructural protein 3 36
- 10.6019/CHEMBL5606460 Genome polyprotein 30
- 10.6019/CHEMBL5606458 Nonstructural protein 3 24
27966962 10.1021/acs.jmedchem.6b01021 Unchecked 6
27966962 10.1021/acs.jmedchem.6b01021 NON-PROTEIN TARGET 3
- 10.6019/CHEMBL5604065 NS3 protease 3
31549836 10.1021/acs.jmedchem.9b00775 Nonstructural protein 3 2
- 10.6019/CHEMBL5604061 NS3 2
- 10.6019/CHEMBL5604064 NS3 protease 2
- 10.6019/CHEMBL5604066 NS3 protease 2
32605372 10.1021/acs.jmedchem.0c00413 Trypsin 1
32605372 10.1021/acs.jmedchem.0c00413 Prothrombin 1

Data from ChEMBL 36 via Core Engine