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Compound Detail

CHEMBL3978250

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COc1cccc(C(=O)N2CCC(F)(F)C(Oc3ccc4ccccc4n3)C2)c1

Basic Information

ChEMBL ID CHEMBL3978250
Phase Preclinical
Structure Type MOL
InChI Key QZXSVMSMRJTFPZ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

398.4
MW (Da)
4.17
ALogP
4
HBA
0
HBD
51.7
PSA (Ų)
0.66
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20F2N2O3
MW 398.41
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.01

Activity Summary

Ki 1 meas. best 8.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.04 8.04 9.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Ki = 9.1 nM 8.04 Displacement of (2S)-N-(2-phenylphenyl)-1-[2-[1-(tritritiomethyl)benzimidazol-2-... 27818110

Literature References

PubMed DOI Target Context # Activities
27818110 10.1016/j.bmcl.2016.10.019 Unchecked 2
27818110 10.1016/j.bmcl.2016.10.019 Voltage-dependent L-type calcium channel subunit alpha-1C 1
27818110 10.1016/j.bmcl.2016.10.019 Cytochrome P450 3A4 1
27818110 10.1016/j.bmcl.2016.10.019 Cytochrome P450 2C9 1
27818110 10.1016/j.bmcl.2016.10.019 No relevant target 1
27818110 10.1016/j.bmcl.2016.10.019 Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine