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Compound Detail

CHEMBL12659

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CC1=C(C(O)CO)c2cc3nc(cc4[nH]c(cc5[nH]c(cc1n2)c(C)c5CCC(=O)O)c(CCC(=O)O)c4C)C(C(O)CO)=C3C

Basic Information

ChEMBL ID CHEMBL12659
Phase Preclinical
Structure Type MOL
InChI Key GAVJVYKTGGHFIM-LNKBXFQTSA-N
1
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

630.7
MW (Da)
3.53
ALogP
8
HBA
8
HBD
212.9
PSA (Ų)
0.16
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H38N4O8
MW 630.70
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness 0.34

Activity Summary

EC50 2 meas. best 4.26
IC50 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 4.26 4.26 54411.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus 1 EC50 = 54411.0 nM 4.26 Inhibition of HIV-1 P24 production. 8164251

Literature References

PubMed DOI Target Context # Activities
8164251 10.1021/jm00034a007 Human immunodeficiency virus 1 2
1527792 10.1021/jm00096a020 Human immunodeficiency virus type 1 protease 2
1527792 10.1021/jm00096a020 Human immunodeficiency virus type 2 pol protein 1
1527792 10.1021/jm00096a020 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine