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Compound Detail

CHEMBL205845

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CC(C)Cn1c(=O)n(C)c(=O)c2c(S[C@@H]3CC[C@H](O)C3)c(Cc3ccccc3C(F)(F)F)sc21

Basic Information

ChEMBL ID CHEMBL205845
Phase Preclinical
Structure Type MOL
InChI Key FPZKMOBZAQYAOC-JKSUJKDBSA-N
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
5.03
ALogP
7
HBA
1
HBD
64.2
PSA (Ų)
0.50
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27F3N2O3S2
MW 512.62
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.89

Activity Summary

IC50 1 meas. best 6.7
Ki 1 meas. best 9.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monocarboxylate transporter 1
CHEMBL4360
Ki 9.38 9.38 0.4 1
Cytochrome P450 2C9
CHEMBL3397
IC50 6.7 6.7 200.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 31.0 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 = 0.42 nM 9.38 Binding affinity to MCT1 by FB assay 16455256
Cytochrome P450 2C9 IC50 = 200.0 nM 6.7 Inhibition of CYP2C9 16455256

Literature References

PubMed DOI Target Context # Activities
16455256 10.1016/j.bmcl.2006.01.024 Monocarboxylate transporter 1 1
16455256 10.1016/j.bmcl.2006.01.024 Hepatocyte 1
16455256 10.1016/j.bmcl.2006.01.024 Cytochrome P450 2C9 1
16455256 10.1016/j.bmcl.2006.01.024 No relevant target 1

Data from ChEMBL 36 via Core Engine