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Compound Detail

CHEMBL5080087

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Cc1nc(C)c([C@H](OC(C)(C)C)C(=O)O)c(N2CCC(C)(C)CC2)c1-c1ccc(SCCc2ccc(F)cc2)cc1

Basic Information

ChEMBL ID CHEMBL5080087
Phase Preclinical
Structure Type MOL
InChI Key UQDIRJKAKJCBPZ-HKBQPEDESA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

578.8
MW (Da)
8.41
ALogP
5
HBA
1
HBD
62.7
PSA (Ų)
0.26
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H43FN2O3S
MW 578.79
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.59

Activity Summary

EC50 1 meas. best 7.81
IC50 1 meas. best 7.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 7.81 7.81 15.6 1
Unchecked
CHEMBL612545
IC50 7.01 7.01 98.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Rattus norvegicus
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35235334 10.1021/acs.jmedchem.1c02169 ADMET 2
35235334 10.1021/acs.jmedchem.1c02169 Unchecked 1
35235334 10.1021/acs.jmedchem.1c02169 Human immunodeficiency virus 1 1
35235334 10.1021/acs.jmedchem.1c02169 MT2 1

Data from ChEMBL 36 via Core Engine