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Compound Detail

CHEMBL3981114

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O=C(c1cccc2[nH]cnc12)N1CCC(F)(F)[C@@H](Oc2ccc3ccccc3n2)C1

Basic Information

ChEMBL ID CHEMBL3981114
Phase Preclinical
Structure Type MOL
InChI Key RGCVWVPTCVUBJN-SFHVURJKSA-N
2
Targets
2
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

408.4
MW (Da)
4.04
ALogP
4
HBA
1
HBD
71.1
PSA (Ų)
0.56
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18F2N4O2
MW 408.41
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.98

Activity Summary

Ki 2 meas. best 8.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 8.42 8.42 3.8 1
Orexin receptor type 2
CHEMBL4792
Ki 5.85 5.85 1409.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 69.0 mL.min-1.kg-1 Rattus norvegicus
CL 829.0 mL.min-1.kg-1 Rattus norvegicus
F 10.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27818110 10.1016/j.bmcl.2016.10.019 Unchecked 3
27818110 10.1016/j.bmcl.2016.10.019 ADMET 3
27818110 10.1016/j.bmcl.2016.10.019 Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine