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Compound Detail

CHEMBL4160395

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COc1cc(C(=O)Nc2cc(OC(F)(F)F)ccc2-n2cncn2)ccc1OC1CC1

Basic Information

ChEMBL ID CHEMBL4160395
Phase Preclinical
Structure Type MOL
InChI Key NKFXNBZYAWFRIF-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

434.4
MW (Da)
3.97
ALogP
7
HBA
1
HBD
87.5
PSA (Ų)
0.61
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H17F3N4O4
MW 434.37
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.52

Activity Summary

IC50 2 meas. best 6.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 7
CHEMBL3879
IC50 6.15 6.15 708.0 2

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.052 - Rattus norvegicus
Fu 0.039 - Mus musculus
Fu 0.013 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29259756 10.1021/acsmedchemlett.7b00429 ADMET 5
29259756 10.1021/acsmedchemlett.7b00429 Metabotropic glutamate receptor 7 3

Data from ChEMBL 36 via Core Engine