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Compound Detail

CHEMBL5599838

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CC(C)NC(=O)[C@H](Nc1ccc2c(c1)CNC2)c1cc(Cl)cc2[nH]c(-c3ccccc3)nc12

Basic Information

ChEMBL ID CHEMBL5599838
Phase Preclinical
Structure Type MOL
InChI Key NXAMBTBBWHMYHI-XMMPIXPASA-N
8
Targets
26
Activities
2
Assay Types
9
PK Parameters
15
Publications
0
Known Names

Molecular Properties

460.0
MW (Da)
5.16
ALogP
4
HBA
4
HBD
81.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H26ClN5O
MW 459.98
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.04

Activity Summary

IC50 24 meas. best 7.8
EC50 2 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nonstructural protein 3
CHEMBL4523954
IC50 7.8 7.4683 16.0 6
NS3
CHEMBL5705861
IC50 6.82 6.625 152.0 4
Zika virus
CHEMBL4296612
EC50 5.85 5.85 1417.0 1
NS3 protease
CHEMBL5705862
IC50 5.69 5.41 2056.0 2
NS3 protease
CHEMBL5705863
IC50 5.66 5.405 2207.0 2
Genome polyprotein
CHEMBL5980
IC50 5.39 4.9425 4105.0 8
NS3 protease
CHEMBL5705864
IC50 5.36 5.095 4384.0 2
dengue virus type 2
CHEMBL613966
EC50 5.3 5.3 5047.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 23.22 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 11.04 mL.min-1.g-1 Mus musculus
Fu 0.7 - Bos taurus
Fu 0.01 - Mus musculus
Fu 0.03 - Homo sapiens
T1/2 1.199 hr Homo sapiens
T1/2 2.888 hr Homo sapiens
T1/2 2.521 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nonstructural protein 3 IC50 = 16.0 nM 7.8 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 19.0 nM 7.72 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 33.0 nM 7.48 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 42.0 nM 7.38 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 54.0 nM 7.27 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 69.0 nM 7.16 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 152.0 nM 6.82 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 255.0 nM 6.59 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 280.0 nM 6.55 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 286.0 nM 6.54 Functional biochemical assay to identify treatments for viral infectious disease... -
Zika virus EC50 = 1417.0 nM 5.85 Functional CPE-based assay to measure dose dependent changes in antiviral-drug i... -
NS3 protease IC50 = 2056.0 nM 5.69 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 protease IC50 = 2207.0 nM 5.66 Functional biochemical assay to identify treatments for viral infectious disease... -
Genome polyprotein IC50 = 4105.0 nM 5.39 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 protease IC50 = 4384.0 nM 5.36 Functional biochemical assay to identify treatments for viral infectious disease... -
dengue virus type 2 EC50 = 5047.0 nM 5.3 Functional assay to measure dose dependent changes in antiviral-drug inhibitory ... -
Genome polyprotein IC50 = 5230.0 nM 5.28 Functional biochemical assay to identify treatments for viral infectious disease... -
Genome polyprotein IC50 = 6306.0 nM 5.2 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 protease IC50 = 7062.0 nM 5.15 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 protease IC50 = 7461.0 nM 5.13 Functional biochemical assay to identify treatments for viral infectious disease... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5674856 ADMET 15
- 10.6019/CHEMBL5665440 ADMET 12
- 10.6019/CHEMBL5604063 Genome polyprotein 8
- 10.6019/CHEMBL5674852 ADMET 8
- 10.6019/CHEMBL5604062 Nonstructural protein 3 6
- 10.6019/CHEMBL5661943 Zika virus 6
- 10.6019/CHEMBL5661943 dengue virus type 2 6
- 10.6019/CHEMBL5661955 ADMET 6
- 10.6019/CHEMBL5604061 NS3 4
- 10.6019/CHEMBL5604064 NS3 protease 2
- 10.6019/CHEMBL5604065 NS3 protease 2
- 10.6019/CHEMBL5604066 NS3 protease 2
- 10.6019/CHEMBL5606460 Genome polyprotein 2
- 10.6019/CHEMBL5674850 No relevant target 2
- 10.6019/CHEMBL5674854 No relevant target 2

Data from ChEMBL 36 via Core Engine