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Compound Detail

CHEMBL2435435

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COc1cc2c(cc1C(C)NCC1CCCCC1)C=CC(C)(C)O2

Basic Information

ChEMBL ID CHEMBL2435435
Phase Preclinical
Structure Type MOL
InChI Key LWFWVRZBVMVNHA-UHFFFAOYSA-N
7
Targets
8
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

329.5
MW (Da)
5.11
ALogP
3
HBA
1
HBD
30.5
PSA (Ų)
0.81
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H31NO2
MW 329.48
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness 1.03

Activity Summary

IC50 6 meas. best 6.19
Ki 2 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL4153
Ki 8.62 8.62 2.4 1
Unchecked
CHEMBL612545
Ki 6.89 6.89 128.0 1
Leishmania tarentolae
CHEMBL612915
IC50 6.19 6.19 650.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 5.67 5.67 2160.0 1
Plasmodium falciparum
CHEMBL364
IC50 5.61 5.61 2460.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.89 4.89 12900.0 1
L6
CHEMBL614793
IC50 4.84 4.84 14500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23968432 10.1021/jm401007p Unchecked 3
24996139 10.1016/j.ejmech.2014.06.054 Unchecked 2
23968432 10.1021/jm401007p Leishmania tarentolae 1
23968432 10.1021/jm401007p Leishmania donovani 1
23968432 10.1021/jm401007p Trypanosoma cruzi 1
23968432 10.1021/jm401007p Trypanosoma brucei rhodesiense 1
23968432 10.1021/jm401007p Plasmodium falciparum 1
23968432 10.1021/jm401007p L6 1
24996139 10.1016/j.ejmech.2014.06.054 Sigma non-opioid intracellular receptor 1 1

Data from ChEMBL 36 via Core Engine