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Compound Detail

CHEMBL4753310

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O=C(Nc1cnn(-c2csc(C(=O)N[C@@H]3CCOC3)c2)c1)Nc1ccccc1Cl

Basic Information

ChEMBL ID CHEMBL4753310
Phase Preclinical
Structure Type MOL
InChI Key NDXBTYNWEFNKOR-GFCCVEGCSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
11
Publications
0
Known Names

Molecular Properties

431.9
MW (Da)
3.75
ALogP
6
HBA
3
HBD
97.3
PSA (Ų)
0.57
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 C19H18ClN5O3S
MW 431.91
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -2.12

Activity Summary

IC50 3 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 8.1 8.1 8.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.82 5.82 1500.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 5.7 5.7 2020.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.55 hr Homo sapiens
T1/2 0.2167 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