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Compound Detail

CHEMBL1802829

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CN(C)S(=O)(=O)Nc1ccc2ccc3ncc(-c4cnn(C)c4)cc3c(=O)c2c1

Basic Information

ChEMBL ID CHEMBL1802829
Phase Preclinical
Structure Type MOL
InChI Key AYNVIPPTDMPZRW-UHFFFAOYSA-N
2
Targets
6
Activities
1
Assay Types
6
PK Parameters
9
Publications
0
Known Names

Molecular Properties

409.5
MW (Da)
2.37
ALogP
6
HBA
1
HBD
97.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19N5O3S
MW 409.47
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.60

Activity Summary

IC50 6 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 8.4 7.328 4.0 5
Macrophage-stimulating protein receptor
CHEMBL2689
IC50 8.15 8.15 7.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 57.0 mL.min-1.kg-1 Canis lupus familiaris
CL 40.0 mL.min-1.kg-1 Rattus norvegicus
F 16.0 % Canis lupus familiaris
F 24.0 % Rattus norvegicus
T1/2 0.8 hr Canis lupus familiaris
T1/2 0.7 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23379595 10.1021/jm301619u Canis familiaris 4
23379595 10.1021/jm301619u Rattus norvegicus 4
23379595 10.1021/jm301619u Hepatocyte growth factor receptor 3
21608528 10.1021/jm200112k Hepatocyte growth factor receptor 2
23379595 10.1021/jm301619u Cytochrome P450 3A4 2
21608528 10.1021/jm200112k Unchecked 1
21608528 10.1021/jm200112k Voltage-gated inwardly rectifying potassium channel KCNH2 1
23379595 10.1021/jm301619u Voltage-gated inwardly rectifying potassium channel KCNH2 1
23379595 10.1021/jm301619u Macrophage-stimulating protein receptor 1

Data from ChEMBL 36 via Core Engine