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Compound Detail

CHEMBL3961834

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Cn1c(Nc2c(F)cccc2Cl)nc2cc(C(=O)Nc3ccc(C(F)(F)F)cc3)c3c(c21)CC(C)(C)O3

Basic Information

ChEMBL ID CHEMBL3961834
Phase Preclinical
Structure Type MOL
InChI Key KXJFMYSYPOZGGT-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

532.9
MW (Da)
7.09
ALogP
5
HBA
2
HBD
68.2
PSA (Ų)
0.28
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H21ClF4N4O2
MW 532.93
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.26

Activity Summary

IC50 4 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin E synthase
CHEMBL5658
IC50 8.59 7.9025 2.6 4

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29519738 10.1016/j.bmcl.2018.02.048 Prostaglandin E synthase 3
29519738 10.1016/j.bmcl.2018.02.048 ADMET 3
27865703 10.1016/j.bmcl.2016.10.079 Prostaglandin E synthase 1
29519738 10.1016/j.bmcl.2018.02.048 Cytochrome P450 1A2 1
29519738 10.1016/j.bmcl.2018.02.048 Cytochrome P450 2D6 1
29519738 10.1016/j.bmcl.2018.02.048 Cytochrome P450 3A4 1
29519738 10.1016/j.bmcl.2018.02.048 Cytochrome P450 2C9 1
29519738 10.1016/j.bmcl.2018.02.048 Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine