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Compound Detail

CHEMBL5084138

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Cc1nc(C)c([C@H](OC(C)(C)C)C(=O)O)c(N2CCC(C)(C)CC2)c1-c1ccc(OCCc2ccc(F)c(F)c2)cc1

Basic Information

ChEMBL ID CHEMBL5084138
Phase Preclinical
Structure Type MOL
InChI Key MQOIECOWBIBICH-HKBQPEDESA-N
2
Targets
8
Activities
2
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

580.7
MW (Da)
7.83
ALogP
5
HBA
1
HBD
71.9
PSA (Ų)
0.28
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 C34H42F2N2O4
MW 580.72
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.52

Activity Summary

EC50 7 meas. best 8.74
IC50 1 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 8.74 8.2471 1.8 7
Unchecked
CHEMBL612545
IC50 8.17 8.17 6.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.8 mL.min-1.kg-1 Rattus norvegicus
T1/2 0.85 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 Human immunodeficiency virus 1 7
35235334 10.1021/acs.jmedchem.1c02169 ADMET 3
35235334 10.1021/acs.jmedchem.1c02169 Unchecked 1
35235334 10.1021/acs.jmedchem.1c02169 MT2 1

Data from ChEMBL 36 via Core Engine