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Compound Detail

CHEMBL2114369

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C[C@@H]1O[C@](C#CC2CC2)(C(F)(F)F)c2cc(Cl)ccc2NC1=O

Basic Information

ChEMBL ID CHEMBL2114369
Phase Preclinical
Structure Type MOL
InChI Key QCTDQQNLOPRRMO-VFZGTOFNSA-N
1
Targets
2
Activities
1
Assay Types
4
PK Parameters
4
Publications
0
Known Names

Molecular Properties

343.7
MW (Da)
3.87
ALogP
2
HBA
1
HBD
38.3
PSA (Ų)
0.73
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H13ClF3NO2
MW 343.73
Aromatic Rings 1
Heavy Atoms 23
NP-Likeness -0.10

Activity Summary

IC50 2 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 7.09 7.09 82.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 10311.9 ng.hr.mL-1 Macaca mulatta
Cmax 1670.0 nM -
T1/2 - - Macaca mulatta
Tmax 6.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11378361 10.1016/s0960-894x(01)00239-6 Human immunodeficiency virus type 1 reverse transcriptase 3
11378361 10.1016/s0960-894x(01)00239-6 Rhesus monkey 3
11378361 10.1016/s0960-894x(01)00239-6 ADMET 2
26708112 10.1016/j.ejmech.2015.11.025 Human immunodeficiency virus type 1 reverse transcriptase 1

Data from ChEMBL 36 via Core Engine