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Compound Detail

CHEMBL4074049

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Cc1cc(C#N)cc(C)c1Oc1nc(NC2CCC(NCc3ccc(S(N)(=O)=O)cc3)CC2)nc2ccsc12

Basic Information

ChEMBL ID CHEMBL4074049
Phase Preclinical
Structure Type MOL
InChI Key WNZYHVDGZRQQIJ-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

562.7
MW (Da)
5.13
ALogP
9
HBA
3
HBD
143.0
PSA (Ų)
0.27
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30N6O3S2
MW 562.72
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.45

Activity Summary

EC50 3 meas. best 7.38
IC50 1 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 7.38 7.38 42.2 1
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
EC50 6.82 6.79 152.0 2
Unchecked
CHEMBL612545
IC50 5.4 5.4 4020.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28481112 10.1021/acs.jmedchem.7b00332 Unchecked 11
28481112 10.1021/acs.jmedchem.7b00332 Human immunodeficiency virus type 1 reverse transcriptase 7
28481112 10.1021/acs.jmedchem.7b00332 Human immunodeficiency virus 1 1
28481112 10.1021/acs.jmedchem.7b00332 Human immunodeficiency virus 2 1
28481112 10.1021/acs.jmedchem.7b00332 MT4 1

Data from ChEMBL 36 via Core Engine