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Compound Detail

CHEMBL1778785

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Cl.O=C(O)[C@@H]1C[C@H](Oc2cccc(Cl)c2)CN1

Basic Information

ChEMBL ID CHEMBL1778785
Phase Preclinical
Structure Type MOL
InChI Key UKPGMXGYVXPVBI-IYPAPVHQSA-N
Parent Compound CHEMBL1778764
Active Moiety CHEMBL1778764
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
5
Publications
0
Known Names

Molecular Properties

241.7
MW (Da)
1.53
ALogP
3
HBA
2
HBD
58.6
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H13Cl2NO3
MW 278.13
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.17

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.4 8.4 4.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 41.0 mL.min-1.kg-1 Rattus norvegicus
CL 49.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 2400000.0 nM Homo sapiens
T1/2 2.3 hr Homo sapiens
T1/2 0.4 hr Rattus norvegicus
T1/2 1.5 hr Canis lupus familiaris
Tmax 0.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 4.0 nM 8.4 Displacement of [3H]gabapentin from voltage gated calcium channel alpha2delta fr... 21550803

Literature References

PubMed DOI Target Context # Activities
21550803 10.1016/j.bmcl.2011.04.056 Plasma 4
21550803 10.1016/j.bmcl.2011.04.056 Rattus norvegicus 2
21550803 10.1016/j.bmcl.2011.04.056 Canis familiaris 2
21550803 10.1016/j.bmcl.2011.04.056 Unchecked 1
21550803 10.1016/j.bmcl.2011.04.056 No relevant target 1

Data from ChEMBL 36 via Core Engine