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Compound Detail

CHEMBL379682

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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 CHEMBL379682
Phase Preclinical
Structure Type MOL
InChI Key FPZKMOBZAQYAOC-HZPDHXFCSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
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

Ki 1 meas. best 9.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monocarboxylate transporter 1
CHEMBL4360
Ki 9.54 9.54 0.3 1

Pharmacokinetic Data

Parameter Value Units Species
CL 26.0 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 = 0.29 nM 9.54 Binding affinity to MCT1 by FB assay 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 No relevant target 1

Data from ChEMBL 36 via Core Engine