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Compound Detail

CHEMBL454633

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O=S1(=O)CCCCN1c1nc(-c2nnc(Cc3ccc(F)cc3)o2)c(O)c2ncccc12

Basic Information

ChEMBL ID CHEMBL454633
Phase Preclinical
Structure Type MOL
InChI Key PKDXCDDPOQGIND-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

455.5
MW (Da)
3.05
ALogP
8
HBA
1
HBD
122.3
PSA (Ų)
0.50
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18FN5O4S
MW 455.47
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.66

Activity Summary

EC50 2 meas. best 7.89
IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 8.7 8.7 2.0 1
Unchecked
CHEMBL612545
IC50 8.7 8.7 2.0 1
Human immunodeficiency virus
CHEMBL613758
EC50 7.89 7.89 13.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19217284 10.1016/j.bmcl.2009.01.089 Unchecked 1
19217284 10.1016/j.bmcl.2009.01.089 Human immunodeficiency virus 1
19217284 10.1016/j.bmcl.2009.01.089 ADMET 1
19217781 10.1016/j.bmcl.2009.01.090 Human immunodeficiency virus type 1 integrase 1
19217781 10.1016/j.bmcl.2009.01.090 Human immunodeficiency virus 1

Data from ChEMBL 36 via Core Engine