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Compound Detail

CHEMBL1209073

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COc1cncc(-c2ccccc2O[C@H]2C[C@@H]3CNC[C@H]2C3)c1.Cl

Basic Information

ChEMBL ID CHEMBL1209073
Phase Preclinical
Structure Type MOL
InChI Key PPNMSSHGJBECBJ-BQPCHSDVSA-N
Parent Compound CHEMBL1229180
Active Moiety CHEMBL1229180
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

310.4
MW (Da)
3.13
ALogP
4
HBA
1
HBD
43.4
PSA (Ų)
0.94
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H23ClN2O2
MW 346.86
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.06

Activity Summary

EC50 2 meas. best 7.54
Ki 2 meas. best 8.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.04 8.04 9.0 1
Unchecked
CHEMBL612545
EC50 7.54 7.54 28.9 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
EC50 7.49 7.49 32.7 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
Ki 7.03 7.03 94.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20663668 10.1016/j.bmcl.2010.06.142 Neuronal acetylcholine receptor; alpha3/beta4 3
20663668 10.1016/j.bmcl.2010.06.142 Unchecked 3
20663668 10.1016/j.bmcl.2010.06.142 MDCK 2
20663668 10.1016/j.bmcl.2010.06.142 Neuronal acetylcholine receptor; alpha4/beta2 1
20663668 10.1016/j.bmcl.2010.06.142 Neuronal acetylcholine receptor subunit alpha-7 1
20663668 10.1016/j.bmcl.2010.06.142 Voltage-gated inwardly rectifying potassium channel KCNH2 1
20663668 10.1016/j.bmcl.2010.06.142 Acetylcholine receptor; alpha1/beta1/delta/gamma 1

Data from ChEMBL 36 via Core Engine