Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL219483

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CNc1nc2ccccc2n1Cc1sc2c(c1C(=O)N1CCC1)c(=O)n(C)c(=O)n2CC(C)C

Basic Information

ChEMBL ID CHEMBL219483
Phase Preclinical
Structure Type MOL
InChI Key FVIJIRCHSMDMJH-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

480.6
MW (Da)
2.70
ALogP
9
HBA
1
HBD
94.2
PSA (Ų)
0.46
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H28N6O3S
MW 480.59
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.45

Activity Summary

IC50 2 meas. best 6.0
Ki 1 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monocarboxylate transporter 1
CHEMBL4360
Ki 7.23 7.23 59.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 6.0 6.0 1000.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.05 5.05 8900.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 3.0 uL.min-1.(10^6cells)-1 Rattus norvegicus
CL 3.0 uL.min-1.(10^6cells)-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Monocarboxylate transporter 1 Ki = 59.0 nM 7.23 Binding affinity to MCT1 17228867
Cytochrome P450 3A4 IC50 = 1000.0 nM 6.0 Inhibition of CYP3A4 17228867
Cytochrome P450 2C9 IC50 = 8900.0 nM 5.05 Inhibition of CYP2C9 17228867

Literature References

PubMed DOI Target Context # Activities
17228867 10.1021/jm060995h ADMET 2
17228867 10.1021/jm060995h Monocarboxylate transporter 1 1
17228867 10.1021/jm060995h Cytochrome P450 2C9 1
17228867 10.1021/jm060995h Cytochrome P450 3A4 1
17228867 10.1021/jm060995h No relevant target 1

Data from ChEMBL 36 via Core Engine