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Compound Detail

CHEMBL3913485

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COc1ccc(C(C)C)cc1C1=C(CN(Cc2cc(C(F)(F)F)cc(C(F)(F)F)c2)c2ncc(-c3cnn(C)c3)cn2)CC(C)(C)CC1

Basic Information

ChEMBL ID CHEMBL3913485
Phase Preclinical
Structure Type MOL
InChI Key UJEIOIFAOYONCD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

671.7
MW (Da)
9.72
ALogP
6
HBA
0
HBD
56.1
PSA (Ų)
0.17
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H39F6N5O
MW 671.73
Aromatic Rings 4
Heavy Atoms 48
NP-Likeness -0.61

Activity Summary

IC50 1 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholesteryl ester transfer protein
CHEMBL3572
IC50 7.16 7.16 70.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6994.4 ng.hr.mL-1 Rattus norvegicus
Cmax 1038.21 nM Rattus norvegicus
T1/2 11.1 hr Rattus norvegicus
Tmax 2.5 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27490022 10.1016/j.ejmech.2016.07.065 ADMET 4
27490022 10.1016/j.ejmech.2016.07.065 Syrian golden hamster 3
27490022 10.1016/j.ejmech.2016.07.065 Cholesteryl ester transfer protein 1

Data from ChEMBL 36 via Core Engine