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Compound Detail

CHEMBL2165448

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COCc1cc(OC[C@@H]2CCN2)no1

Basic Information

ChEMBL ID CHEMBL2165448
Phase Preclinical
Structure Type MOL
InChI Key DCPBGIZDLFBSSR-ZETCQYMHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

198.2
MW (Da)
0.56
ALogP
5
HBA
1
HBD
56.5
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H14N2O3
MW 198.22
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness -0.78

Activity Summary

Ki 1 meas. best 5.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha3/beta2
CHEMBL1907587
Ki 5.39 5.39 4100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuronal acetylcholine receptor; alpha3/beta2 Ki = 4100.0 nM 5.39 Displacement of [3H]epibatidine from rat alpha3beta2 nACHR 22148173

Literature References

PubMed DOI Target Context # Activities
22148173 10.1021/jm201301h Neuronal acetylcholine receptor; alpha4/beta4 2
22148173 10.1021/jm201301h Unchecked 1
22148173 10.1021/jm201301h Neuronal acetylcholine receptor; alpha4/beta2 1
22148173 10.1021/jm201301h Neuronal acetylcholine receptor; alpha3/beta4 1
22148173 10.1021/jm201301h Neuronal acetylcholine receptor; alpha2/beta4 1
22148173 10.1021/jm201301h Neuronal acetylcholine receptor; alpha3/beta2 1
23641311 10.1021/ml3002715 Unchecked 1
23641311 10.1021/ml3002715 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine