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Compound Detail

CHEMBL4460705

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Cc1nc2cc(-c3ccccc3)nn2c(N2CCC(C)(C)CC2)c1C(OC(C)(C)C)C(=O)O

Basic Information

ChEMBL ID CHEMBL4460705
Phase Preclinical
Structure Type MOL
InChI Key YYAGFKRZXPZDJF-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
5.27
ALogP
6
HBA
1
HBD
80.0
PSA (Ų)
0.57
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H34N4O3
MW 450.58
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.86

Activity Summary

EC50 1 meas. best 6.26
Ki 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
Ki 7.22 7.22 60.0 1
Human immunodeficiency virus 1
CHEMBL378
EC50 6.26 6.26 550.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32081010 10.1021/acs.jmedchem.9b01681 Human immunodeficiency virus 1 1
32081010 10.1021/acs.jmedchem.9b01681 Human immunodeficiency virus type 1 integrase 1
32081010 10.1021/acs.jmedchem.9b01681 No relevant target 1
32081010 10.1021/acs.jmedchem.9b01681 ADMET 1

Data from ChEMBL 36 via Core Engine