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Compound Detail

CHEMBL444502

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COc1cc(C/C=C(\C)CCC(=O)O)ccc1-c1cnco1

Basic Information

ChEMBL ID CHEMBL444502
Phase Preclinical
Structure Type MOL
InChI Key RUQFCLKDOPFZEG-KGVSQERTSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

301.3
MW (Da)
3.70
ALogP
4
HBA
1
HBD
72.6
PSA (Ų)
0.79
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H19NO4
MW 301.34
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.74

Activity Summary

Ki 2 meas. best 4.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inosine-5'-monophosphate dehydrogenase 2
CHEMBL2002
Ki 4.84 4.84 14300.0 1
Inosine-5'-monophosphate dehydrogenase 1
CHEMBL1822
Ki 4.37 4.37 42800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Inosine-5'-monophosphate dehydrogenase 2 Ki = 14300.0 nM 4.84 Inhibition of human IMPDH2 18809333
Inosine-5'-monophosphate dehydrogenase 1 Ki = 42800.0 nM 4.37 Inhibition of human IMPDH1 18809333

Literature References

PubMed DOI Target Context # Activities
18809333 10.1016/j.bmc.2008.08.062 Inosine-5'-monophosphate dehydrogenase 2 1
18809333 10.1016/j.bmc.2008.08.062 Inosine-5'-monophosphate dehydrogenase 1 1
18809333 10.1016/j.bmc.2008.08.062 K562 1

Data from ChEMBL 36 via Core Engine