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Compound Detail

CHEMBL4793809

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O=C(Nc1cnn(-c2csc(C(=O)NC3CC3)c2)c1)Nc1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4793809
Phase Preclinical
Structure Type MOL
InChI Key MJPWAJUXPIZNIX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
11
Publications
0
Known Names

Molecular Properties

401.9
MW (Da)
4.12
ALogP
5
HBA
3
HBD
88.0
PSA (Ų)
0.60
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 C18H16ClN5O2S
MW 401.88
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -2.50

Activity Summary

IC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.1 7.1 80.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 5.5 5.5 3200.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.13 5.13 7400.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.8167 hr Homo sapiens
T1/2 0.5833 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33488960 10.1021/acsmedchemlett.0c00533 ADMET 2
33488960 10.1021/acsmedchemlett.0c00533 Unchecked 2
33488960 10.1021/acsmedchemlett.0c00533 SH-SY5Y 1
33488960 10.1021/acsmedchemlett.0c00533 Cytochrome P450 3A4 1
33488960 10.1021/acsmedchemlett.0c00533 Cytochrome P450 2D6 1
33488960 10.1021/acsmedchemlett.0c00533 Cytochrome P450 2C9 1
33488960 10.1021/acsmedchemlett.0c00533 Cytochrome P450 1A2 1
33488960 10.1021/acsmedchemlett.0c00533 Mitogen-activated protein kinase 14 1
33488960 10.1021/acsmedchemlett.0c00533 Mitogen-activated protein kinase 9 1
33488960 10.1021/acsmedchemlett.0c00533 Mitogen-activated protein kinase 8 1
33488960 10.1021/acsmedchemlett.0c00533 Mitogen-activated protein kinase 10 1

Data from ChEMBL 36 via Core Engine