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Compound Detail

CHEMBL3288755

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CCN1C(=O)CN(c2ccc(Cc3cc([C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)ccc3Cl)cc2)C1=O

Basic Information

ChEMBL ID CHEMBL3288755
Phase Preclinical
Structure Type MOL
InChI Key OKQVIDODFGYTAX-IFPLKCGESA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
12
Publications
0
Known Names

Molecular Properties

490.9
MW (Da)
1.23
ALogP
7
HBA
4
HBD
130.8
PSA (Ų)
0.45
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H27ClN2O7
MW 490.94
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 0.13

Activity Summary

IC50 2 meas. best 7.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium/glucose cotransporter 2
CHEMBL3884
IC50 7.96 7.96 10.9 1
Sodium/glucose cotransporter 1
CHEMBL4979
IC50 4.76 4.76 17500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.3 mL.min-1.g-1 Homo sapiens
CL 1.9 mL.min-1.g-1 Rattus norvegicus
F 4.0 % Rattus norvegicus
T1/2 0.5833 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24842618 10.1016/j.bmc.2014.04.036 Liver microsome 2
24842618 10.1016/j.bmc.2014.04.036 Rattus norvegicus 2
24842618 10.1016/j.bmc.2014.04.036 Sodium/glucose cotransporter 2 1
24842618 10.1016/j.bmc.2014.04.036 Sodium/glucose cotransporter 1 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 1A2 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 2B6 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 2C9 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 2C19 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 2D6 1
24842618 10.1016/j.bmc.2014.04.036 Cytochrome P450 3A4 1
24842618 10.1016/j.bmc.2014.04.036 No relevant target 1
24842618 10.1016/j.bmc.2014.04.036 Unchecked 1

Data from ChEMBL 36 via Core Engine