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Compound Detail

CHEMBL260185

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COc1ccc(OC)c2c1c(C(=O)/C=C(\O)C(=O)O)cn2Cc1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL260185
Phase Preclinical
Structure Type MOL
InChI Key IVCJOZWNBVIQMX-SXGWCWSVSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
3.56
ALogP
6
HBA
2
HBD
98.0
PSA (Ų)
0.36
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18FNO6
MW 399.37
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.34

Activity Summary

IC50 4 meas. best 7.52
EC50 2 meas. best 5.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 7.52 7.37 30.0 4
Human immunodeficiency virus 1
CHEMBL378
EC50 5.67 5.67 2130.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18417342 10.1016/j.bmcl.2008.03.089 Human immunodeficiency virus type 1 integrase 2
18541726 10.1128/aac.00210-08 Human immunodeficiency virus type 1 integrase 2
18417342 10.1016/j.bmcl.2008.03.089 Human immunodeficiency virus 1 1
18417342 10.1016/j.bmcl.2008.03.089 MT4 1
18417342 10.1016/j.bmcl.2008.03.089 Unchecked 1
18541726 10.1128/aac.00210-08 Human immunodeficiency virus 1 1
18541726 10.1128/aac.00210-08 MT4 1
18541726 10.1128/aac.00210-08 Unchecked 1

Data from ChEMBL 36 via Core Engine