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Compound Detail

CHEMBL3098172

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COC(=O)[C@H](CO)NC(=O)CC/C(C)=C/Cc1c(O)c2c(c(C)c1OC)COC2=O

Basic Information

ChEMBL ID CHEMBL3098172
Phase Preclinical
Structure Type MOL
InChI Key GAMZMTPMBWXMIQ-RILDOFPPSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

421.4
MW (Da)
1.30
ALogP
8
HBA
3
HBD
131.4
PSA (Ų)
0.40
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H27NO8
MW 421.45
Aromatic Rings 1
Heavy Atoms 30
NP-Likeness 1.35

Activity Summary

IC50 3 meas. best 5.38
Ki 2 meas. best 7.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inosine-5'-monophosphate dehydrogenase 2
CHEMBL2002
Ki 7.03 7.03 94.0 1
Inosine-5'-monophosphate dehydrogenase 1
CHEMBL1822
Ki 5.99 5.99 1017.0 1
K562
CHEMBL385
IC50 5.38 5.38 4200.0 1
DU-145
CHEMBL613508
IC50 4.89 4.89 13000.0 1
HL-60
CHEMBL383
IC50 4.75 4.75 18000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24269162 10.1016/j.bmcl.2013.11.005 PC-3 1
24269162 10.1016/j.bmcl.2013.11.005 DU-145 1
24269162 10.1016/j.bmcl.2013.11.005 HL-60 1
24269162 10.1016/j.bmcl.2013.11.005 K562 1
24269162 10.1016/j.bmcl.2013.11.005 Inosine-5'-monophosphate dehydrogenase 2 1
24269162 10.1016/j.bmcl.2013.11.005 Inosine-5'-monophosphate dehydrogenase 1 1

Data from ChEMBL 36 via Core Engine