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Compound Detail

CHEMBL241098

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COc1cccc(C2NCCc3c2[nH]c2ccccc32)c1

Basic Information

ChEMBL ID CHEMBL241098
Phase Preclinical
Structure Type MOL
InChI Key LACQLKYZMSEMTM-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

278.4
MW (Da)
3.41
ALogP
2
HBA
2
HBD
37.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H18N2O
MW 278.36
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness 0.16

Activity Summary

IC50 2 meas. best 4.6
Ki 1 meas. best 5.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 5.77 5.77 1700.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.6 4.6 25100.0 1
Isocitrate lyase
CHEMBL5359
IC50 4.12 4.12 75000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21035332 10.1016/j.bmcl.2010.10.029 Isocitrate lyase 2
27280693 10.1021/acs.jmedchem.6b00035 Broad substrate specificity ATP-binding cassette transporter ABCG2 2
17317171 10.1016/j.bmcl.2007.01.093 5-hydroxytryptamine receptor 7 1
17317171 10.1016/j.bmcl.2007.01.093 Muscarinic acetylcholine receptor M4 1
17317171 10.1016/j.bmcl.2007.01.093 D(2) dopamine receptor 1
21035332 10.1016/j.bmcl.2010.10.029 Sortase A 1
21035332 10.1016/j.bmcl.2010.10.029 Staphylococcus aureus 1
21035332 10.1016/j.bmcl.2010.10.029 Bacillus subtilis 1
21035332 10.1016/j.bmcl.2010.10.029 Salmonella typhimurium 1
21035332 10.1016/j.bmcl.2010.10.029 Proteus vulgaris 1
21035332 10.1016/j.bmcl.2010.10.029 Micrococcus luteus 1
21035332 10.1016/j.bmcl.2010.10.029 Escherichia coli 1
27280693 10.1021/acs.jmedchem.6b00035 ATP-dependent translocase ABCB1 1
34058709 10.1016/j.ejmech.2021.113536 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine