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Compound Detail

CHEMBL78504

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CNc1cc(CN2C(=O)N(Cc3ccc4[nH]ncc4c3)[C@H](Cc3ccccc3)[C@H](O)[C@@H](O)[C@H]2Cc2ccccc2)ccc1F

Basic Information

ChEMBL ID CHEMBL78504
Phase Preclinical
Structure Type MOL
InChI Key RREYCVXDIYCIMA-WZJLIZBTSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

593.7
MW (Da)
5.13
ALogP
5
HBA
4
HBD
104.7
PSA (Ų)
0.19
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H36FN5O3
MW 593.70
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -0.60

Activity Summary

Ki 1 meas. best 10.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 protease
CHEMBL243
Ki 10.57 10.57 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 670.0 nM Canis lupus familiaris
F 14.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus type 1 protease Ki = 0.027 nM 10.57 Inhibitory activity against HIV protease 9632373

Literature References

PubMed DOI Target Context # Activities
9632373 10.1021/jm980103g Human immunodeficiency virus type 1 protease 1
9632373 10.1021/jm980103g MT2 1
9632373 10.1021/jm980103g ADMET 1
9632373 10.1021/jm980103g Canis familiaris 1

Data from ChEMBL 36 via Core Engine