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Compound Detail

CHEMBL4294195

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COc1ccc2c(c1OC)C(OC)N(C)c1c-2ccc2cc3c(cc12)OCO3

Basic Information

ChEMBL ID CHEMBL4294195
Phase Preclinical
Structure Type MOL
InChI Key LVWAKZBZWYHYCJ-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

379.4
MW (Da)
4.35
ALogP
6
HBA
0
HBD
49.4
PSA (Ų)
0.67
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C22H21NO5
MW 379.41
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness 1.14

Activity Summary

IC50 3 meas. best 5.52
Ki 2 meas. best 5.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1A1
CHEMBL2231
IC50 5.52 5.52 3030.0 1
Cytochrome P450 1A1
CHEMBL2231
Ki 5.49 5.49 3250.0 1
Cytochrome P450 1B1
CHEMBL4878
IC50 5.11 5.11 7700.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 5.05 5.05 8930.0 1
Cytochrome P450 1A2
CHEMBL3356
Ki 5.04 5.04 9160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30108931 10.1039/C7MD00388A Cytochrome P450 1A1 4
30108931 10.1039/C7MD00388A Cytochrome P450 1A2 3
30108931 10.1039/C7MD00388A Cytochrome P450 2D6 2
30108931 10.1039/C7MD00388A Cytochrome P450 1B1 2
30108931 10.1039/C7MD00388A Cytochrome P450 3A4 2
30108931 10.1039/C7MD00388A Cytochrome P450 2C9 2
30108931 10.1039/C7MD00388A Cytochrome P450 2C19 2
35168150 10.1016/j.ejmech.2022.114173 Mycobacterium tuberculosis 1

Data from ChEMBL 36 via Core Engine