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Compound Detail

CHEMBL577395

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CC(C)(C)c1ccc2[nH]c3c(c2c1)CC(=O)N(Cc1ccc(Cl)c(Cl)c1)c1ccccc1-3

Basic Information

ChEMBL ID CHEMBL577395
Phase Preclinical
Structure Type MOL
InChI Key RZYATJZFRQBDLG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

463.4
MW (Da)
7.53
ALogP
1
HBA
1
HBD
36.1
PSA (Ų)
0.33
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24Cl2N2O
MW 463.41
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.95

Activity Summary

IC50 1 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Malate dehydrogenase, mitochondrial
CHEMBL5917
IC50 6.11 6.11 770.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Malate dehydrogenase, mitochondrial IC50 = 770.0 nM 6.11 Inhibition of mitochondrial malate dehydrogenase by spectrophotometry 19906467

Literature References

PubMed DOI Target Context # Activities
19906467 10.1016/j.ejmech.2009.10.018 Malate dehydrogenase, mitochondrial 1
19906467 10.1016/j.ejmech.2009.10.018 Cyclin-dependent kinase 1/cyclin B 1
19906467 10.1016/j.ejmech.2009.10.018 Glycogen synthase kinase-3 beta 1
19906467 10.1016/j.ejmech.2009.10.018 COLO 205 1
19906467 10.1016/j.ejmech.2009.10.018 HCT-116 1
19906467 10.1016/j.ejmech.2009.10.018 IGROV-1 1
19906467 10.1016/j.ejmech.2009.10.018 OVCAR-3 1

Data from ChEMBL 36 via Core Engine