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Compound Detail

CHEMBL4868880

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Cc1nc2c(-c3ccc(S(C)(=O)=O)cc3)cnn2c(NCc2ccccn2)c1C

Basic Information

ChEMBL ID CHEMBL4868880
Phase Preclinical
Structure Type MOL
InChI Key IKPXFQBRUZBWKL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
9
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.5
MW (Da)
3.42
ALogP
7
HBA
1
HBD
89.2
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N5O2S
MW 407.50
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.98

Activity Summary

EC50 1 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 6.84 6.84 143.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 82209.0 ng.hr.mL-1 Mus musculus
AUC 162617.0 ng.hr.mL-1 Mus musculus
CL 21.78 mL.min-1.g-1 Homo sapiens
Cmax 32073.62 nM Mus musculus
Cmax 68220.86 nM Mus musculus
T1/2 2.9 hr Mus musculus
T1/2 2.4 hr Mus musculus
Tmax 1.33 hr Mus musculus
Tmax 1.67 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 143.0 nM 6.84 Anti wolbachia activity against Wolbachia infected in Aedes albopictus C6/36 ass... 34527179

Literature References

PubMed DOI Target Context # Activities
34527179 10.1021/acsmedchemlett.1c00216 ADMET 11
34527179 10.1021/acsmedchemlett.1c00216 Unchecked 3
34527179 10.1021/acsmedchemlett.1c00216 No relevant target 2

Data from ChEMBL 36 via Core Engine